NEUROPHARMACOLOGICS

ADRENERGICS

AR-100
Bopindolol malonate
99%, MW=484.6 [62658-64-4] Storage: RT
A slowly dissociating b1-adrenergic receptor antagonist^1,2. Antihypertensive. Antioxidant (IC₅₀=1.8 µM) and free radical scavenging activity³.
100 mg
500 mg

AR-105
(-)-Cyanopindolol hemifumarate
99%, MW=345.4 [81608-27-7] Storage: RT
b-Adrenergic receptor antagonist^4,5. Serotonin 5HT1A/1B antagonist^6,7.
10 mg
50 mg

AR-102
Guanfacine HCl
99%, MW=282.5 [29520-14-7] Storage: RT
Centrally acting ₂-adrenergic receptor agonist. In the guinea pig cerebral cortex, the K_ds are 20 and 880 nM for a_2A- and the a_2C-adrenoceptor, respectively⁸. Antihypertensive agent⁹.
100 mg
500 mg

AR-104
ICI-118,551
98%, MW=313.9 [72795-19-8] Storage: 4°C
A highly selective b₂-adrenergic receptor antagonist^10,11.
10 mg
50 mg

Phenoxybenzamine·HCl
99%, MW=340.3 [63-92-3] Storage: RT
Selective a-adrenergic receptor antagonist. Irreversibly inhibits calmodulin.

Propranolol
(?1-(Isopropylamino)-3-(1-naphthyloxy)-2-propanol·HCl
98%, MW=295.8 [3506-09-0] Storage: 0°C
Selective b-adrenergic receptor antagonist.

AR-107
S(-)-Propranolol HCl
98%, MW=295.8 [4199-10-4] Storage: RT
b-Adrenergic receptor antagonist. Active enantiomer of (?-propranolol¹².
100 mg

AR-106
Rauwolscine HCl (a-Yohimbine HCl)
98%, MW=390.9 [6211-32-1] Storage: RT
a₂-Adrenergic receptor antagonist^13,14.
200 mg
500 mg

AR-103
Tizanidine HCl
99%, MW=290.2 [51322-75-9] Storage: RT
₂-Adrenergic receptor agonist. Displays affinity for the I₁-imidazoline receptor¹⁵. Spasmolytic activity¹⁶.
100 mg
500 mg

REFERENCES

1. Y. Hosohata et al. Biol. Pharm. Bull. 1995 18 1066

2. Y. Hosohata et al. Gen. Pharmacol. 1995 26 743

3. Y. Aniya et al. Jpn. J. Pharmacol. 1995 68 323

4. D. Bojanic et al. Eur. J. Pharmacol. 1983 93 235

5. Y. Cui et al. J. Mol. Cell. Cardiol. 1996 28 1307

6. G. Engel et al. Naunyn Schmied. Arch. Pharmacol. 1986 332 1

7. H. Giles et al. Br. J. Pharmacol. 1996 117 1119

8. S. Uhlen et al. Pharmacol.Toxicol. 1995 76 353

9. P.A. van Zwieten J. Cardiovasc. Pharmacol. 1996 27 S5

10. A.J.Bilski et al. J. Cardiovasc. Pharmacol. 1983 5 430

11. R.A. Bond et al. Nature 1995 374 214

12. R. Howe and R.G. Shanks Nature 1966 210 1336

13. J.P. Hieble et al. J. Med. Chem. 1995 38 3415

14. L.C. Rump et al. J. Cardiovasc. Pharmacol. 1995 26 462

15. J. E. Piletz et al. J. Pharmacol. Exp. Ther. 1996 279 694

16. D.M. Coward Neurology 1994 44 S6

BENZODIAZEPINES

W-100
Chlordiazepoxide HCl (Ro 5-0690)
99%, MW=336.2 [438-41-5] Storage: RT
Benzodiazepine agonist¹. Anxiolytic.
Controlled substance. Schedule 4.
10 g
50 g

W-120
4'-Chlorodiazepam (Ro 5-4864)
99%, MW=319.2 [14439-61-3] Storage: RT
Peripheral benzodiazepine agonist^2,3,4. Relaxes airway smooth muscle⁵. Blocks GABA_A chloride channels, binding to a site different from that of picrotoxin⁶.
Controlled substance. Schedule 4. information.
5 mg
25 mg

W-105
Desmethyldiazepam (Nordiazepam, Ro 5-2180)
99%, MW=270.7 [1088-11-5] Storage: RT
Benzodiazepine agonist. Major, biologically active metabolite of diazepam. Anxiolytic^7,8.
Controlled substance. Schedule 4. information.
10 mg
100 mg

W-110
Diazepam (Ro 5-2807)
99%, MW=284.8 [439-14-5] Storage: RT
Benzodiazepine agonist⁹. Anxiolytic
Controlled substance. Schedule 4.
1 g
10 g

B-102
Ethyl -carboline-3-carboxylate (-CCE)
98%, MW=240.3 [74214-62-3] Storage: RT
Benzodiazepine inverse agonist¹⁰. Antagonizes some of the actions of benzodiazepines in vivo. Lowers seizure threshold and reverses the sedative effect of flurazepam¹¹. Anxiogenic and convulsant activity¹². SAR studies^13,14.
Methyl, propyl, and butyl ester analogs are also available. Please inquire.
100 mg
500 mg

B-100
Flumazenil (Ro 15-1788)
MW=303.3 [78755-81-4]
Benzodiazepine antagonist. Reverses all the effects of benzodiazepine agonists and inverse agonists^15,16.
Inquire

W-115
Flunitrazepam (Ro 5-4200)
99%, MW=313.3 [1622-62-4] Storage: RT
Benzodiazepine agonist. Hypnotic^17,18.
Controlled substance. Schedule 4. See page X3 for ordering information.
50 mg
250 mg

B-103
3-Hydroxymethyl--carboline
98%, MW=198.2 [65474-79-5] Storage: RT
Benzodiazepine inverse agonist. Antagonizes the anxiolytic and anticonvulsant actions of diazepam^19,20 and reverses the sedative action of flurazepam²¹.
20 mg
100 mg

WB-104
Zolpidem
N,N,6-Trimethyl-2-(4-methylphenyl)-imidazo[1,2-a]pyridine-3-acetamide
99%, MW=307.4 [82626-48-0] Storage: RT
Benzodiazepine agonist selective for the BZ₁ subtype associated with the GABA_A receptor^22,16.
Controlled substance. Schedule 4. See page X3 for ordering information.
5 mg
25 mg

REFERENCES

1. E. Van der Kleijn Psychopharmacol. 1977 2 997

2. A.J. Eshleman et al. J. Neurochem. 1989 53 494

3. M. Holck and W. Osterreider Eur. J. Pharmacol. 1985 118 293

4. P. Marangos et al. Mol. Pharmacol. 1982 22 26

5. D. Raeburn et al. J. Pharmacol. Exp. Ther. 1988 245 557

6. I. Izquierdo and J.H. Medina Trends Pharmacol. Sci. 1991 12 260

7. A.N. Nicholson et al. Br. J. Clin. Pharmacol. 1976 3 429

8. U. Traversa et al. J. Pharm. Pharmacol. 1977 29 504

9. R.F. Squires and C. Braestrup Nature 1977 266 732

10. M. Cain et al. J. Med. Chem. 1982 25 1081

11. P.J. Cowan et al. Nature 1981 290 54

12. L. Prado de Carvalho et al. Nature 1983 301 64

13. K.P. Lippke et al. J. Med. Chem. 1983 26 449

14. G. Neef et al. Heterocycles 1983 20 1295

15. S.E. File Neuropharmacol. 1986 89 113

16. G. Mereu et al. Eur. J. Pharmacol. 1990 179 339

17. M.A.K. Matila and H.M. Larni Drugs 1980 20 353

18. M. Viukari et al. Curr. Ther. Res. 1983 33 828

19. P. Skolnick et al. Prog. Clin. Biol. Res. 1982 90 122

20. P.A. Borea et al. Biochem. Pharmacol. 1988 37 3953

21. W.B. Mendelson et al. Science 1983 219 414

22. J. Benavides et al. Brain Res. 1993 604 240

CANNABINOIDS

ANANDAMIDES AND RELATED AMIDES

FA-017
Anandamide
Arachidonylethanolamide
98%, Solution in methylene chloride, MW=347.6 [94421-68-8] Storage: -70°C.
Endogenous cannabinoid ligand¹. Inhibits the binding of [³H]HU-243 to synaptosomal membranes (K_i=52 nM)². Binds to brain² and peripheral³ cannabinoid receptors. Cannabimimetic activity^4,5.
5 mg
25 mg

FA-026
Anandamide (18:2, n-6)
Linoleylethanolamide
98%, Solution in methylene chloride, MW=323.6, Storage: -70°C.
Anandamide analog.
5 mg
25 mg

FA-019
Anandamide (20:3, n-6)
Dihomo--linolenylethanolamide
98%, Solution in methylene chloride, MW=349.6, Storage: -70°C
Endogenous cannabinoid ligand⁶. Inhibits the binding of [³H]HU-243 to synaptosomal membranes (K_i=53 nM)⁷.
5 mg
25 mg

FA-020
Anandamide (22:4, n-6)
Docosatetraenylethanolamide
98%, Solution in methylene chloride, MW=375.6, Storage: -70°C
Endogenous cannabinoid ligand^6,7. Inhibits the binding of [³H]HU-243 to synaptosomal membranes (K_i=34 nM)7.
5 mg
25 mg

FA-022
Arachidonamide
98%, Solution in methylene chloride, MW=303.5, Storage: -70°C
A weak cannabinoid CB₁ and CB₂ agonist⁸.
10 mg
50 mg

FA-023
Linoleamide
98%, MW=279.5, Storage: -20°C
Unsaturated analog of endogenous sleep inducing lipid⁹.
10 mg
50 mg

FA-027
Mead acid ethanolamide
Eicosa-5Z,8Z,11Z-trienylethanolamide
98%, Solution in methylene chloride, MW=349.6, Storage: -70°C
A cannabinoid CB₁ and CB₂ agonist equipotent with anandamide¹⁰.
1 mg
10 mg

FA-021
(R)-Methanandamide
(R)-Arachidonic acid propan-1-ol-2-amide
98%, MW=361.6 [150314-39-9] Storage: -20°C
A potent analog of anandamide with improved metabolic stability and selectivity for the CB₁ receptor¹¹. K_i=20 nM in rat forebrain membranes¹². Inhibits motor behavior resembling the effects of THC rather than anandamide¹³.
5 mg
25 mg

FA-025
9,10-Octadecenoamide
99%, MW=281.5 Storage: -20°C
Endogenous sleep inducing lipid⁹. Substrate for anandamide amidohydrolase¹⁴.
10 mg
50 mg

FA-018
Palmitylethanolamide
98%, MW=299.5 Storage: -20°C
Inactive negative control for anandamide at CB₁ receptors². Endogenous agonist at the CB₂ receptor¹⁵.
10 mg
50 mg

OTHER CANNABINOIDS

CR-104
BML-190
Indomethacin morpholinylamide
98%, MW=426.9, Storage: RT
A potent and selective ligand for the human cannabinoid CB₂ receptor¹⁶.
10 mg
50 mg

CR-103
HU-210
98%, MW=386.6 [112924-45-5] Storage: -20°C
A potent cannabinoid CB₁¹⁷ and CB₂¹⁸ receptor agonist.
5 mg
25 mg

L-126
Tetrahydrocannabinol-7-oic acid
11-Nor-D⁸-tetrahydrocannabinol-9-carboxylic acid
98%, MW=344.4 [39690-06-7] Storage: 0°C.
A nonpsychoactive metabolite of tetrahydrocannabinol with potent bronchodilatory, antiinflammatory and analgesic activity^19,20.

REFERENCES

1. W.A. Devane Trends Pharmacol. Sci. 1994 15 40

2. W.A. Devane et al. Science 1992 258 1946

3. S. Munro et al. Nature 1993 365 61

4. E. Fride et al. Eur. J. Pharmacol. 1993 231 313

5. J.N. Crawley et al. Pharmacol. Biochem. Behav. 1993 46 967

6. J. Barg et al. Eur. J. Pharmacol. 1995 287 145

7. L. Hanus et al. J. Med. Chem. 1993 36 3032

8. J.C. Pinto et al. Mol. Pharmacol. 1994 46 516

9. B.F. Cravatt et al. Science. 1995 268 1506

10. J. Priller et al. Mol. Pharmacol. 1995 48 288

11. A.D. Khanolkar et al. J. Med. Chem. 1996 39 4515

12. V. Abadji et al. J. Med. Chem. 1994 37 1889

13. J. Romero et al. Life Sci. 1996 58 1249

14. S. Maurelli et al. FEBS Lett. 1995 377 82

15. L. Facci et al. Proc. Natl. Acad. Sci. USA 1995 92 3376

16. M. Gallant et al. Bioorg. Med. Chem. Letters 1996 6 2263

17. A.C. Howlett et al. Neuropharmacology 1990 29 161

18. D.M. Slipetz et al. Mol. Pharmacol. 1995 48 352

19. S. Burstein et al. FASEB J. 1988 2 3024

20. S. Burstein et al. J. Med. Chem. 1992 35 3135

CHOLINERGICS

C-100
(+)-Anatoxin A
2-Acetyl-9-azabicyclo[4.2.1]non-2-ene·HCl
99% MW=165.2 [64314-16-5] Storage: -20°C
Anatoxin is an alkaloidal toxin produced by the filamentous freshwater cyanophyte Anabaena flos-aquae¹. It is a potent agonist at neuronal nicotinic acetylcholine receptors². At low concentrations (20-200 nM) it acts as an agonist³. At higher concentrations (>800 nM) it blocks the AChR ion channel, desensitizes the receptor and blocks neuromuscular transmission⁴.
250 µg
1 mg

C-102
BMCP
1-Benzyl-1-methyl-4-cyclopentylmethoxycarbonylpiperidinium bromide
98%, MW=396.4, Storage: RT
A potent inhibitor of the active transport of acetylcholine by synaptic vesicles.⁵
20 mg
100 mg

C-103
Dexetimide·HCl (R 16470)
98%, MW=398.9 [21888-98-2] Storage: RT
A high affinity muscarinic receptor antagonist^6,7,8.
50 mg

C-104
4-Diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP)
98%, MW=451.4 [1952-15-4] Storage: RT
M₃ muscarinic receptor antagonist^9,10.
20 mg
100 mg

C-114
(?-Epibatidine
99%, MW=208.7 [140111-52-0] Storage: -20°C
Epibatidine is an analgesic alkaloid isolated from the skin of the poison frog Epipedobates tricolor¹¹. It is the most potent nicotinic acetylcholine receptor agonist known¹². The natural (+) enantiomer is only 2-fold more potent than the (-) enantiomer with respect to analgesic activity in mice. Both enantiomers bind with high affinity (K_i=0.045 and 0.058 nM respectively) to rat brain membrane nicotinic receptors¹³.
1 mg
5 mg

C-115
Galanthamine·HBr
98% MW=368.3 [1953-04-4] Storage: -20°C
Inhibits acetylcholinesterase from human brain frontal cortex (IC₅₀=3.2 µM) and is 10-fold more active for human erythrocyte acetylcholinesterase¹⁴. Possible Alzheimer's disease therapeutic^15,16.
20 mg
100 mg

C-112
Gallamine triethiodide
98%, MW=891.5 [65-29-2] Storage: RT
M₂ muscarinic antagonist with pronounced cardioselectivity^17,18,19. Acts via allosteric modulation of receptor binding²⁰. For a review of allosteric antagonists of the muscarinic acetylcholine receptor see reference .
1 g
5 g

C-116
Himbacine
98%, MW=345.5 [6879-74-9] Storage: -20°C
Himbacine is an alkaloid isolated from Galbulimima baccata. It is a potent muscarinic M₂/M₄ receptor antagonist^22,23.
1 mg
5 mg

C-105
(?-Huperzine A
98%, MW=242.3 [102518-79-6] Storage: 0°C
A potent acetylcholinesterase inhibitor²⁴. Nootropic agent. Improves memory and learning in animal models^25,26.
1 mg
5 x 1 mg

C-106
Hydroxytacrine maleate
98%, MW=330.3 [112964-99-5] Storage: RT
Cholinesterase inhibitor. Potential Alzheimer's Disease therapeutic²⁷.
200 mg
1 g

C-108
1-Methyl-4-[2-(2-naphthyl)-ethenyl]-pyridinium iodide
98%, MW=373.2, Storage: RT
Choline acetyltransferase inhibitor²⁸.
20 mg
100 mg

C-113
2-(-Naphthoyl)-ethyltrimethylammonium iodide (-NETA)
98%, MW=369.2 Storage: RT
Potent and selective inhibitor of choline acetyltransferase²⁹
20 mg
100 mg

C-109
Oxotremorine sesquifumarate
98%, MW=380.4 [17360-35-9] Storage: 0°C
Muscarinic agonist³⁰. Combinations of oxotremorine and other muscarinic agonists display supra-additive memory enhancement³¹. For recent reviews of muscarinic agonists and antagonists see references32 and 33.
100 mg
500 mg

C-110
Tacrine·HCl
98%, MW=234.7 [1684-40-8] Storage: 0°C
Cholinesterase inhibitor. Alzheimer's disease therapeutic^34,35.
1 g
5 g

C-111
(?-Vesamicol·HCl (AH-5183)
98%, MW=295.5 [120447-62-3] Storage: RT
Potent inhibitor of acetylcholine storage^36,37.
200 mg
1 g

REFERENCES

1. O.E. Edwards et al. Can. J. Chem. 1977 55 1367

2. P. Thomas et al. J. Neurochem. 1993 60 2308

3. K.L. Swanson et al. Mol. Pharmacol. 1986 29 250

4. P. Kofuji et al. J. Pharmacol. Exp. Ther. 1990 252 517

5. G.A. Rodgers and S.M. Parsons Mol. Pharmacol. 1989 36 333

6. P.M. Laduron et al. J. Neurochem. 1979 33 1223

7. P.M. Laduron et al. Drug Dev. Res. 1986 8 15

8. P.A.J. Janssen et al. Arzneim. Forsch. 1971 21 1365

9. R.B. Barlow and M.K. Shepherd Br. J. Pharmacol. 1986 89 837

10. A.D. Michel et al. Eur. J. Pharmacol. 1989 166 459

11. T.F. Spande et al. J. Am. Chem. Soc. 1992 114 3475

12. C. Qian et al. Eur. J. Pharmacol. 1993 250 R13

13. B. Badio and J.W. Daly Mol. Pharmacol. 1994 45 563

14. T. Thomsen et al. Eur. J. Clin. Chem. Clin. Biochem. 1991 29 487

15. P. Dal-Bianco et al. J. Neural. Transm. Suppl. 1991 33 59

16. P. Chopin and M. Briley Psychopharmacology. 1992 106 26

17. R. Hammer et al. Life Sci. 1986 38 1653

18. J. Nedoma et al. J. Pharmacol. Exp. Ther. 1986 236 219

19. A.D. Michel et al. Eur. J. Pharmacol. 1990 182 335

20. T. Kenakin et al. J. Pharmacol. Exp. Ther. 1989 250 944

21. N.H. Lee and E.E. El-Fakahany Biochem. Pharmacol. 1991 42 199

22. J.H. Miller et al. J. Pharmacol. Exp. Ther. 1992 263 663

23. P.M. Kerr et al. Br. J. Pharmacol. 1995 115 1518

24. H. Xu and X.-C. Tang Acta Pharm. Sin. 1987 8 18

25. X.-C. Tang et al. Acta Pharm. Sin. 1986 7 507

26. S.-L. Zhang New Drugs Clin. Remedies 1986 5 260

27. G.M. Shutske et al. J. Med. Chem. 1988 31 1278

28. C.J. Cavalito et al. J. Med. Chem. 1969 12 134

29. B.V.R. Sastry et al. J. Pharmacol. Exp. Ther. 1988 245 72

30. S.K. Fisher et al. Mol. Pharmacol. 1987 32 81

31. J.F.Flood et al. Psychopharmacology 1985 86 61

32. G. Mihm and B. Wetzel Annu. Rev. Med. Chem. 1988 23 81

33. V.P. Whittaker Trends Pharmacol. Sci.1990 11 8

34. W.K. Summers et al. N. Engl. J. Med. 1986 315 1241

35. W.K. Summers et al. Clin. Toxicol. 1980 16 269

36. G.A. Rodgers et al. J. Med. Chem. 1989 32 1217

37. I.G. Marshall and S.M. Parsons Trends Neurosci. 1987 10 174

DOPAMINERGICS

D-100
6,7-ADTN·HBr
(?-2-Amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene·HBr
98%, MW=260.1 [73304-33-3] Storage: RT
Dopamine agonist^1,2.
25 mg

D-101
AJ-76
(1S,2R)-cis-5-Methoxy-1-methyl-2-(n-propylamino)-tetralin·HCl
98%, MW=269.8 [85379-09-5] Storage: RT
A selective dopamine autoreceptor antagonist^3,4. Antagonizes the pharmacological effects of cocaine⁵.
10 mg
50 mg

D-102
Bromocriptine mesylate
(+)-2-Bromo-12'-hydroxy-2'-(1-methylethyl)-5'-(2-methylpropyl)-ergotaman-3',6',18-trione methanesulfonate
98% MW=750.7 [22260-51-1] Storage: -20°C
Dopamine agonist⁶.
100 mg
500 mg

D-103
BTCP
1-[1-(2-Benzo[b]thienyl)cyclohexyl)]piperidine·maleate
98%, MW=415.6 [112726-66-6] Storage: RT
Dopamine uptake inhibitor^7,8,9.
10 mg
50 mg

D-108
Clothiapine
99%, MW=343.9 [2058-52-8] Storage: RT
Atypical neuroleptic agent related to clozapine.
20 mg
100 mg

D-107
Clozapine
99%, MW=326.8 [5786-21-0] Storage: RT
Dopamine D₄ and D₂ receptor antagonist. High affinity for the cloned rat dopamine D₄ receptor (K_i<20 nM)²⁰. Atypical neuroleptic agent¹⁰.
20 mg
100 mg

D-104
GBR-12909
1-(2-bis-(4-Fluorophenyl)methoxy)ethyl)-4-(3-phenyl-2-propyl)piperazine·HCl
98%, MW=523.5 [67469-78-7] Storage: RT
Dopamine uptake inhibitor^11,12,13.
5 mg
25 mg

D-105
7-Hydroxy-DPAT·HBr
(?-7-Hydroxy-2-dipropylaminotetralin·HBr
98%, MW=329.3 [94938-11-7] Storage: RT
Selective D₃ dopamine agonist^14-17 (K_i=0.99 nM)¹⁸.
10 mg
50 mg

D-106
trans-7-Hydroxy-PIPAT maleate
trans-7-Hydroxy-2-[N-propyl-N(3'-iodo-2'-propenyl)amino]tetralin maleate
98%, MW=487.3, Storage: -20°C
A selective, high affinity D₃ dopamine receptor ligand (K_i=0.99 nM)^18,19.
5 mg
25 mg

NS-531
Mesoridazine besylate
99% MW=544.7 [32672-69-8] Storage: RT
Dopamine receptor antagonist. High affinity for the cloned rat dopamine D₄ receptor (K_i<20 nM)²⁰. Antipsychotic agent.
1 g

NS-835
Thioridazine HCl
99%, MW=406.0 [130-61-0] Storage: RT
Dopamine D₄ receptor antagonist. High affinity for the cloned rat dopamine D₄ receptor (K_i<20 nM)²⁰.
5 g

REFERENCES

1. S.J. List et al. J. Neurosci. 1982 2 895

2. G.N. Woodruff et al. Neuropharmacology 1984 23 243

3. F. Hefti Neuropharmacology 1987 26 1239

4. N. Waters et al. Eur. J. Pharmacol. 1994 251 181

5. M.F. Piercey et al. Brain Res. 1992 588 217

6. B. Hokfelt and S.J. Nillius Acta Endocrinol. 1978 Suppl. 216 88

7. J. Vignon et al. Eur. J. Pharmacol. 1988 148 427

8. W. Koek et al. J. Pharmacol. Exp. Therap. 1989 250 1019

9. T. Maurice et al. J. Neurochem. 1991 56 553

10. H.Y. Meltzer Clin. Neurosci. 1995 3 64

11. R.E. Heikkila et al. Eur. J. Pharmacol. 1984 103 241

12. M.H. Teicher et al. Dev. Brain Res. 1986 30 124

13. K.F. Melia et al. J. Pharmacol. Exp. Therap. 1991 258 626

14. S.B. Freedman et al. J. Pharmacol. Exp. Therap. 1994 268 417

15. R.G. MacKenzie et al. Eur. J. Pharmacol. 1994 266 79

16. D. Levesque et al. Proc. Natl. Acad. Sci. USA 1992 89 8155

17. S.A. Daly et al. Neuropharmacol. 1993 32 509

18. Z.P. Zhuang et al. J. Med. Chem. 1993 36 1499

19. M.-P. Kung et al. Eur. J. Pharmacol. 1993 235 165

20. B.L. Roth et al. Neuropsychopharmacol. 1995 120 365

DRUG METABOLITES

NS-105
Clozapine N-oxide
99%, MW=342.8 [34233-69-7] Storage: RT
Major metabolite of clozapine¹. Possesses little or no activity at 5-HT receptors².
5 mg
25 mg

NS-106
N-Desmethylclozapine
99%, MW=312.8 [6104-71-8] Storage: RT
Major metabolite of clozapine^3,4. Potent serotonin 5-HT_1c receptor antagonist⁵ and ligand for 5-HT₆ and 5-HT₇ receptors².
5 mg
25 mg

J-110
Despropionylfentanyl
99%, MW=280.4, Storage: RT
Major urinary metabolite of the narcotic analgesic fentanyl⁶.
1 mg
10 mg

J-115
Despropionyl-3-methylfentanyl
99%, MW=294.4, Storage: RT
Major urinary metabolite of 3-methylfentanyl⁷.
1 mg
10 mg

J-125
a-Hydroxy-alprazolam
98%, MW=324.8, Storage: RT
Metabolite of alprazolam⁸.
5 mg
25 mg

J-126
4-Hydroxy-alprazolam
98%, MW=324.8, Storage: RT
Metabolite of alprazolam⁸.
5 mg
25 mg

EI-169
(?4-Hydroxydebrisoquin
99%, MW=191.2 [59333-79-8] Storage: RT
Major metabolite of debrisoquin⁹. Useful indicator for cytochrome P-450 polymorphism^6,1. For analytical methods see references 11 and 12.
10 mg
50 mg

J-130
a-Hydroxy-triazolam
98%, MW=359.2, Storage: RT
Metabolite of triazolam⁸.
1 mg
5 mg

J-131
4-Hydroxy-triazolam
98%, MW=359.2, Storage: RT
Metabolite of triazolam⁸.
5 mg
25 mg

J-100
Norfentanyl
99%, MW=232.3 Storage: RT
Major urinary metabolite of the narcotic analgesic fentanyl⁷.
1 mg
10 mg

REFERENCES

1. G. Lin et al. J. Pharm. Sci. 1994 83 1412

2. B.L. Roth et al. J. Pharmacol. Exp. Ther. 1994 268 1403

3. O.V. Olesen and B. Poulsen J. Chromatog. 1993 622 39

4. M. Pirmohamed et al. J. Pharmacol. Exp. Ther. 1995 272 984

5. M. Kuoppamaki et al. Eur. J. Pharmacol. 1993 245 179

6. H. Van Rooy et al. J. Chromatography 1981 223 85

7. W.R. Hammargren and G.L. Henderson J. Anal. Toxicol. 1988 12 183

8. W. Huang and D.E. Moody J. Anal. Toxicol. 1995 19 333

9. J.R. Idle et al. Br. J. Clin. Pharmacol. 1979 7 257

10. M.R. Law et al. Brit. J. Cancer 1989 59 686

11. D.A.P. Evans et al. J. Med. Genet. 1980 17 102

12. L. Daumas et al. J. Chromatography 1991 570 89

ENZYME INHIBITORS

EI-265
S(-)-Carbidopa
S--Hydrazino-3,4-dihydroxy--methylbenzenepropanoic acid
99%, MW=244.2 [28860-95-9] Storage: -20°C
Peripheral decarboxylase inhibitor. Used with L-DOPA as a Parkinson's disease therapeutic¹.
20 mg
100 mg

EI-165
Benserazide·HCl (Ro 4-4602)
99%, MW=293.7 [322-35-0] Storage: RT
Peripheral decarboxylase inhibitor^2,3. Also inhibits tryptophan hydroxylase⁴ and tyrosine hydroxylase. Used with L-DOPA as a Parkinson's disease therapeutic.
100 mg
1 g

EI-240
R(-)-Deprenyl·HCl
98%, MW=223.8 [14611-52-0] Storage: RT
Selective MAO-B inhibitor. Parkinson's disease therapeutic^6,7.
100 mg
500 mg

EI-241
Ro 16-6491
N-(2-Aminoethyl)-4-chlorobenzamide hydrochloride
98%, MW=235.1 [94319-79-6] Storage: RT
Selective, reversible MAO-B inhibitor^8,9,10.
200 mg
1 g

EI-217
Tranylcypromine
Monoamine oxidase inhibitor¹¹.

EI-242
U-0521
3',4'-Dihydroxy-2-methylpropiophenone
98%, MW=180.2 [5466-89-7] Storage: RT
Catechol-O-methyltransferase (COMT) inhibitor^12,13,14.
20 mg
100 mg

REFERENCES

1. A.M. Watanabe et al. Clin. Pharmacol. Ther. 1970 11 740

2. R.M. Pinder et al. Drugs 1976 11 329

2. M.-H. Marion et al. Adv. Neurol. 1987 45 493

4 P.A. Johansen et al. Biochem. Pharmacol. 1991 41 625

5. J.F. Reinhard, Jr. and M.D. Shearin Biochem. Pharmacol. 1990 39 1489

6. J.W. Tetrud and J.W. Langston Science 1989 245 519

7. R. Lewin Science 1985 230 527

8. A.M. Cesura et al. J. Neurochem. 1988 50 1037

9. A.M. Cesura et al. Pharmacol. Res. Commun. 1988 20 (S.4) 51

10. A.M. Cesura et al. Biochem. Pharmacol. 1990 39 216

11. R.B. Silverman and P.A. Zieske Biochemistry 1985 24 2128

12. L.J. Bryan et al. Naunyn Schmiedeberg's Arch. Pharmacol. 1983 322 6

13. A. Reches and S. Fahn Adv. Neurol. 1984 40 1716

14. P.G. Duncan et al. Eur. J. Pharmacol. 1985 108 39

HISTAMINERGICS

NH-100
Amthamine
2-Amino-4-methylthiazole-5-ethanamine?HBr
99%, MW=319.1 [142437-67-0] Storage: RT
Highly selective histamine H₂ agonist, devoid of stimulatory activity at H₁ and H₃ receptors^1,2. It induces a dose-dependent increase in gastric acid secretion and is a superior alternative to other H₂ agonists for the study of gastric acid secretion³.
5 mg
25 mg

NH-101
Astemizole
1-[(4-Fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]-4-piperidinyl]-1H-benzimidazol-2-amine
99%, MW=458.6 [68844-77-9] Storage: RT
Selective histamine H₁ receptor antagonist^4,5.
100 mg
500 mg

NH-102
Dimaprit?HCl
S-(3-Dimethylaminopropyl)isothiourea?HCl
98%, MW=234.2 [23256-33-9] Storage: -20°C
Selective histamine H₂ agonist^6,7.
50 mg
250 mg

NH-106
Ketotifen fumarate
99%, MW=425.5 [34580-14-8] Storage: RT
Selective histamine H₁ antagonist⁸. Anti-allergic and anti-asthmatic agent. Mast cell stabilizer. Inhibits ionophore-induced leukotriene generation in human leukocytes, IC₅₀=80 µM⁹. Inhibits histamine release from monocytes and lymphocytes at 0.1-10 µM¹⁰.
1 g

NH-103
HTMT
6-[2-(4-Imidazolyl)ethylamino]-N-(4-trifluoromethylphenyl)heptanecarboxamide·dimaleate
98%, MW=614.6, Storage: RT
Histamine H₁ receptor agonist^11,12.
10 mg
50 mg

NH-107
Levocabastine HCl
99%, MW=457.0 [79547-78-7] Storage: RT
Histamine H₁ receptor antagonist¹³. Anti-allergic agent¹⁴. An antagonist of low affinity neurotensin receptors.
50 mg
250 mg

NH-104
R(-)--Methylhistamine?HBr
99%, MW=287.0, Storage: RT
Potent and selective histamine H₃ agonist^16,17.
10 mg
50 mg

NH-105
Thioperamide·maleate
N-Cyclohexyl-4-(imidazol-4-yl)-1-piperidinecarbothioamide·maleate
99%, MW=408.5 [106243-16-7] Storage: RT
Potent and selective histamine H₃ antagonist^16,18.
10 mg
50 mg

REFERENCES

1. J.C. Eriks et al. J. Med. Chem. 1992 35 3239

2. E. Poli et al. Agents Actions 1993 40 44

3. G. Coruzzi et al. Naunyn Schmeidebergs Arch. Pharmacol. 1993 348 77

4. P.M. Laduron et al. Mol. Pharmacol. 1982 21 294

5. D.M. Richards et al. Drugs 1984 28 38

6. S.J. Hill Pharmacol. Rev. 1990 42 45

7. T.E. Tenner Pharmacology 1981 22 227

8. U. Martin and D. Roemer Arzneim. Forsch. 1978 28 770

9. H. Mita and T. Shida Arzneim. Forsch. 1995 45 36

10. W. Schmutzler et al. Int. Arch. Allergy Immunol. 1995 107 194

11. M.M. Khan et al. J. Immunol. 1986 137 308

12. R. Qui et al. J. Pharmacol. Exp. Therap. 1990 253 1245

13. I.M. Garrelds et al. Ann. Allergy Asthma. Immunol. 1996 76 327

14. S. Noble and D. McTavish et al.Drugs 1995 50 1032

15. P. Chalon et al. FEBS Lett. 1996 386 91

16. J.-M. Arrang et al. Nature 1987 327 117

17. R.W.S. Hew et al. Brit. J. Pharmacol. 1990 101 621

18. F.S. LaBelle et al. Brit. J. Pharmacol. 1992 107 161

NEUROACTIVE AMINO ACIDS

EA-138
N-Acetylglycyl-D-glutamic acid
99%, MW=246.2, Storage: RT
Excitatory peptide, more potent than L-glutamic acid¹.
5 mg
25 mg

EA-108
(?-4-Amino-3-(5-chloro-2-thienyl)-butanoic acid
98%, MW=219.7 [133933-81-0] Storage: RT
Potent and selective GABA_B agonist².
10 mg
50 mg

EA-112
1-Aminocyclobutane-cis-1,3-dicarboxylic acid
trans-1-Aminocyclobutane-1,3-dicarboxylic acid
99%, MW=159.1 [117488-23-0] Storage: RT
The most potent and selective synthetic NMDA agonist known^3,4.
5 mg
25 mg

EA-100
D(-)-2-Amino-4-phosphonobutanoic acid (D-AP4)
98%, MW=183.1 [78739-01-2] Storage: RT
NMDA antagonist⁵.
5 mg
5 x 5 mg

EA-101
DL-2-Amino-4-phosphonobutanoic acid (AP4)
99%, MW=183.1 [20263-07-4] Storage: RT
NMDA agonist/antagonist⁵. Synaptic depressant⁶.
50 mg
250 mg

EA-102
L(+)-2-Amino-4-phosphonobutanoic acid (L-AP4)
99%, MW=183.1 [23052-81-5] Storage: RT
NMDA agonist5. Potent synaptic depressant⁶.
5 mg
5 x 5 mg

EA-103
DL-2-Amino-3-phosphonopropionic acid (AP3)
98%, MW=169.1 [20263-06-3] Storage: RT
Potent and selective quisqualate metabotropic receptor antagonist⁷. The L-isomer is the active form⁸. For reviews of the quisqualate metabotropic receptor see references 9 and 10.
50 mg
250 mg

EA-104
D(-)-2-Amino-5-phosphonovaleric acid (D-AP5)
99%, MW=197.1 [79055-68-8] Storage: RT
Active form of AP5^11,12.
5 mg
5 x 5 mg

CA-400
DL-2-Amino-5-phosphonovaleric acid (AP5)
99%, MW=197.1 [76326-31-3] Storage: RT
Potent NMDA antagonist^11,12
10 mg
50 mg

EA-105
L(+)-2-Amino-5-phosphonovaleric acid (L-AP5)
99%, MW=197.1 [79055-67-7] Storage: RT
Less active form of AP5^11,12
5 mg
5 x 5 mg

EA-110
AMPA
(?--Amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid
98%, MW=186.2 [74341-63-2] Storage: 0°C
Potent and selective glutamate agonist¹³.
5 mg
5 x 5 mg

EA-136
Arcaine sulfate
N,N'-1,4-Butanediyl-bis(guanidine)·sulfate
99%, MW=270.3 [14923-17-2] Storage: RT
Competitive antagonist of the NMDA receptor polyamine site^14,15.
20 mg
100 mg

EA-128
(?-Baclofen
98%, MW=213.7 [1134-47-0] Storage: RT
GABA_B agonist^16,17.
1 g
5 g

EA-109
(-)-Bicuculline methobromide
98%, MW=462.3 [73604-30-5] Storage: 0°C
GABA_A antagonist¹⁸.
100 mg
500 mg

EA-113
5,7-Dichlorokynurenic acid
98%, MW=258.1 [131123-76-7] Storage: RT
Potent antagonist at the NMDA receptor glycine site^19,20.
10 mg
50 mg

EA-114
6,7-Dichloroquinoxaline-2,3-dione (DCQX)
98%, MW=231.0 [25983-13-5] Storage: RT
Selective antagonist at the NMDA receptor glycine site^21,22.
10 mg
50 mg

EA-115
Dihydrokainic acid
98%, MW=215.3 [52497-36-6] Storage: RT
Excitatory amino acid uptake inhibitor¹¹.
10 mg
50 mg

EA-116
6,7-Dinitroquinoxaline-2,3-dione (DNQX)
98%, MW=252.1 [2379-57-9] Storage: RT
Selective non-NMDA receptor antagonist²³.
10 mg
50 mg

EA-117
Domoic acid
98%, MW=311.3 [14277-97-5] Storage: 0°C
More potent and selective than kainate at kainate electrophysiological receptors^24,25,26.
1 mg
5 x 1 mg

EA-135
Gabaculine
(?3-Amino-2,3-dihydrobenzoic acid·HCl
98%, MW=175.6 [59556-17-1] Storage: 0°C
A potent, irreversible inhibitor of GABA transaminase^27,28.
10 mg
50 mg

EA-118
-D-Glutamylaminomethylsulphonic acid (GAMS)
98%, MW=240.2 [90237-02-8] Storage: RT
Selective kainate/quisqualate antagonist²⁹. Anticonvulsant³⁰.
10 mg
50 mg

EA-119
Guvacine·HCl
98%, MW=163.6 [498-96-4] Storage: RT
Specific GABA uptake inhibitor³¹.
10 mg
50 mg

EA-124
Homoquinolinic acid
98%, MW=181.2 [490-75-5] Storage: RT
Potent NMDA agonist^32,33.
5 mg
25 mg

EA-131
N-(4-Hydroxyphenylacetyl)-spermine
MW=336.5 [130210-32-1]
Analog of naturally occurring PhTX-433^34,35. Potent glutamate antagonist^36,37.
Inquire

EA-120
Ibotenic acid
98%, MW=158.1 [2552-55-8] Storage: RT
Potent glutamate agonist^38,39.
1 mg
5 mg

EA-121
Isoguvacine·HCl
98%, MW=163.6 [64603-90-3] Storage: RT
GABA agonist³¹.
10 mg
50 mg

EA-122
Joro Spider Toxin (JSTX-3)
98%, MW=565.7 [112163-33-4] Storage: 0°C
Potent and selective quisqualate/kainate receptor antagonist. For reviews of polyamine spider toxins see references 34 and 35.
100 µg
5 x 100 µg

EA-123
Kainic acid
98%, MW=231.3 [487-79-6] Storage: RT
Selective agonist at the kainate receptor subtype¹¹.
100 mg
500 mg

EA-143
L-701,252
7-Chloro-3-(cyclopropylcarbonyl)-4-hydroxy-2(1H)-quinoline
99%, MW=263.7, Storage: RT
NMDA receptor antagonist acting at the glycine site⁴⁰. Anticonvulsant.
10 mg
50 mg

EA-125
N-Methyl-D-Aspartic acid (NMDA)
99%, MW=147.1 [6384-92-5] Storage: RT
Excitatory amino acid¹¹.
50 mg
250 mg

EA-126
Muscimol
99%, MW=114.1 [2763-96-4] Storage: 0°C
Potent GABA_A receptor agonist⁴¹.
5 mg
25 mg

EA-127
Phaclofen
3-Amino-2-(4-chlorophenyl)-propylphosphonic acid
98%, MW=249.6 [114012-12-3] Storage: RT
Selective GABA_B receptor antagonist⁴².
5 mg
25 mg

EA-129
Philanthotoxin 343 3HCl (PhTX-343)
98%, MW=530.1 [115976-93-7] Storage: -20°C
Analog of naturally occurring PhTX-433^34,35. Potent glutamate antagonist⁴³.
250 µg
5 x 250 µg

EA-139
L-trans-Pyrrolidine-2,4-dicarboxylic acid
98%, MW=159.1 [64769-66-0] Storage: RT
Potent and selective glutamate uptake inhibitor^44,45>.
5 mg
25 mg

EA-132
Quisqualic acid
99%, MW=189.1 [52809-07-1] Storage: RT
Glutamate agonist⁴⁶.
5 mg
25 mg

EA-133
SK&F 97541
3-Aminopropyl-(methyl)phosphinic acid
98%, MW=106.2 [127729-35-5] Storage: RT
GABA_B agonist, 10-fold more potent than baclophen⁴⁷.
5 mg
25 mg

EA-137
Synthalin sulfate
N,N'-1,10-Decanediyl-bis(guanidine)·sulfate
99%, MW=354.5 [111-23-9] Storage: RT
Competitive antagonist of the NMDA receptor polyamine site^48,49.
10 mg
50 mg

EA-144
U-54494A
cis (?-3,4-Dichloro-N-methyl-N-[2-(1-pyrrolidinyl)cyclohexyl]benzamide·HCl
98%, MW=391.8 [92953-41-8] Storage: RT
NMDA antagonist⁵⁰.
5 mg
25 mg

EA-134
ZAPA H₂SO₄
Z-3-(Amidinothio)propenoic acid
98%, MW=244.2 [92138-10-8] Storage: RT
More potent than either GABA or muscimol as an agonist at low affinity GABA_A receptors⁵¹.
5 mg
25 mg

REFERENCES

1. A.P. Garyaev et al Eur. J. Pharmacol. 1991 187 157

2. P. Berthelot et al. J. Med. Chem. 1991 34 2557

3. T.H. Lanthorn et al. Eur. J. Pharmacol. 1990 182 397

4. R.D. Allen et al. J. Med. Chem. 1990 33 2905

5. J. Davies and J.C. Watkins Brain Res. 1982 235 378

6. J.F. Koerner and C.W. Cotman Brain Res. 1981 216 192

7. D.D. Schoepp and B.G. Johnson J. Neurochem. 1989 53 273

8. A.J. Irving et al. Eur. J. Pharmacol. 1990 186 363

9. D.T. Monaghan et al. Ann. Rev. Pharmacol. Toxicol. 1989 29 365

10. C.R.J. Miller Trends Pharmacol. Sci. 1991 12 365

11. J.C. Watkins et al. Ann. Rev. Pharmacol. Toxicol. 1981 21 165

12. J.J. Hansen and P. Krogsgaard-Larsen Med. Res. Rev. 1990 10 55

13. P. Krogsgaard-Larson et al. Nature 1980 284 64

14. I.J. Reynolds et al J. Pharmacol. Exp. Therap. 1990 255 1001

15. I.J. Reynolds et al Eur. J. Pharmacol. 1990 177 215

16. N. Bowery Trends Pharmacol. Sci. 1989 10 401

17. U. Wullner and T. Klockgether Trends Pharmacol. Sci. 1990 11 103

18. D.R. Hill and N.G. Bowery Nature 1981 290 149

19. B.M. Baron et al. Mol. Pharmacol. 1990 38 554

20. P.D. Leeson et al. J. Med. Chem. 1991 34 1243

21. Y. Yoneda and A. Agita Biochem. Biophys. Res. Commun. 1989 164 841

22. A. Agita et al. J. Neurochem. 1990 54 699

23. T. Honore et al. Science 1988 241 701

24. S.G. Agarwal and R.H. Evans Br. J. Pharmacol. 1986 87 345

25. T.J. Biscoe et al. Br. J. Pharmacol. 1976 58 373

26. G. Debonnel et al. Can. J. Physiol. Pharmacol. 1989 67 29

27. B.W. Metcalf Biochem. Pharmacol. 1979 28 1705

28. W. Loscher Naunyn-Schmiedeberg's Arch. Pharmacol. 1980 315 119

29. J. Davies and J.C. Watkins Brain Res. 1985 327 113

30. M.J. Croucher et al. Brain Res. 1984 322 111

31. P. Krogsgaard-Larson et al. J. Neurochem. 1978 30 1377

32. H.J. Olverman et al. Neuroscience 1988 26 17

33. T.W. Stone Br. J. Pharmacol. 1984 81 175

34. H. Jackson and P.N.R. Usherwood Trends Neuroscience 1988 11 278

35. N.A. Saccomano et al. Annu. Rev. Med. Chem. 1989 24 287

36. B.W. Bycroft et al. Eur. J. Pharmacol. 1990 183 470

37. T.W. Smith et al. Eur. J. Pharmacol. 1990 183 472

38. C. Kohler et al. Neuroscience Lett. 1979 15 223

39. G.L. Colingridge et al. Pharmacological Rev. 1989 40 143

40. M. Rowley et al J. Med. Chem. 1993 36 3386

41. F.V. DeFeudis Neurochem. Res. 1980 5 1047

42. D.I.B. Kerr et al. Brain Res. 1987 405 150

43. I.S. Blagbrough et al. J. Pharm. Pharmac. 1989 41 95P

44. R.J. Bridges et al J. Med. Chem. 1991 34 717

45. V.J. Balcar et al FEBS Lett. 1992 300 203

46. P. Boden et al. Brain Res. 1986 385 205

47. G.R. Seabrook et al. Br. J. Pharmacol. 1990 101 949

48. I.J. Reynolds et al J. Pharmacol. Exp. Therap. 1992 259 626

49. I.J. Reynolds et al J. Pharmacol. Exp. Therap. 1992 263 632

50. V.H. Sethy and G.P. Sage Neuropharmacology 1992 31 111

51. R.D. Allan et al. Br. J. Pharmacol. 1986 88 379

OPIOIDS

NO-100
BRL-52537
(?-1-(3,4-Dichlorophenyl)acetyl-2-(1-pyrrolindinyl)-methylpiperidine·HCl
99%, MW=391.8 Storage: RT
Potent and selective -opioid agonist ¹
10 mg
50 mg

NO-101
Naloxone·HCl
99%, MW=363.8 [357-08-4] Storage: RT
Opioid antagonist^2,3.
100 mg
500 mg

NO-102
Naloxonazine?HCl
bis-[5--4,5-Epoxy-3-14-dihydroxy-17-(2-propenyl)morphan-6-ylidene]hydrazine?HCl
98%, MW=723.7 [82824-01-9] Storage: RT
Selective ?sub>1 opioid receptor antagonist^4,5.
10 mg
50 mg

N-701
U-50,488H
99%, MW=465.4 [67198-13-4] Storage: 0°C
Selective -opioid agonist^6,7,8. Inhibits P-type Ca²⁺ channel at 10 µM⁹.
10 mg
50 mg

N-705
U-69,593
99%, MW=356.1 [96744-75-1] Storage: 0°C
Selective -opioid agonist^8,10.
5 mg
25 mg

REFERENCES

1. V. Vecchietti et al. J. Med. Chem. 1991 34 397

2. B.L. Roth et al. J. Neurochem. 1984 42 1677

3. L.F. McNicholas and W.R. Martin Drugs 1984 27 81

4. R.A. Cruciani et al. J. Pharmacol. Exp. Ther. 1987 242 15

5. D. Paul. et al. Eur. J. Pharmacol. 1988 149 403

6. P.F. Von Voigtlander et al. J. Pharmacol. Exp. Ther. 1983 224 7

7. R.A. Lahti et al. Life Sci. 1982 31 2257

8. M.J. Millan Trends Pharmacol. Sci. 1990 11 70

9. T. Kanemasa et al. Brain Res. 1995 702 207

10. R.B. Rothman et al. Eur. J. Pharmacol. 1989 167 345

SIGMA LIGANDS

NO-103
Carbetapentane citrate
99%, MW=525.6 [77-23-6] Storage: RT
Sigma receptor ligand selective for the ₁ receptor^1,2.
100 mg
500 mg

NO-108
L-695,845
3,4-Dihydro-1'-(3-methylbut-2-enyl)spiro[1H-indene-1,4'-piperidine]
99%, MW=255.4 [137730-58-6] Storage: RT
High affinity sigma ligand (pIC₅₀=8.93) with 10,000-fold selectivity over the dopamine D₂ receptor³.
10 mg
50 mg

NO-105
BD 1008
N-[2-(3,4-Dichlorophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylamine?HBr
99%, MW=463.1, Storage: RT
Sigma ligand K_i=0.34 nM⁴.
10 mg
50 mg

NO-490
1-(4-Iodophenyl)-3-(1-adamantyl)-guanidine
99%, MW=395.3, Storage: RT
Sigma receptor ligand (IC₅₀ 2.8 nM vs. [³H]1,3-ditolylguanidine)⁵.
10 mg
50 mg

NO-550
cis-(?-N-Methyl-N-[2-(3,4-dichlorophenyl)ethyl]-2-(1-pyrrolidinyl)cyclohexamine?HBr
99%, MW=517.2, Storage: 0°C
Potent and selective sigma receptor ligand⁶.
10 mg
50 mg

NO-104
4-Phenyl-1-(4-phenylbutyl)piperidine·maleate
98, MW=409.5, Storage: RT
Sigma ligand K_i=0.8 nM⁷.
10 mg
50 mg

NO-107
PRE-084
2-(4-Morpholinethyl)-1-phenylcyclohexanecarboxylate·HCl
99%, MW=353.9, Storage: RT
Sigma ligand⁸.
10 mg
50 mg

REFERENCES

1. R.B. Rothman et al. Mol. Pharmacol. 1991 39 222

2. R. Quirion et al. Trends Pharmacol. Sci. 1992 13 85

3. M.S. Chambers et al. J. Med. Chem. 1992 35 2033

4. B.R. de Costa et al. J. Med. Chem. 1992 35 38

5. A.A. Wilson et al. J. Med. Chem. 1991 34 1867

6. B.R. de Costa et al. J. Med. Chem. 1990 33 3100

7. R.A. Glennon et al. J. Med. Chem. 1991 34 3360

8. T.P. Su et al. J. Pharmacol. Exp. Therap. 1992 259 543

SEROTONERGICS

NS-101
3-(4-Allylpiperazin-1-yl)-2-quinoxalinecarbonitrile·maleate
98%, MW=415.4, Storage: RT
A selective serotonin 5-HT₃ antagonist¹.
5 mg
25 mg

NS-104
AMI-193
8-[3-(4-Fluorophenoxy)propyl-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
99%, MW=383.5, Storage: RT
Selective serotonin 5-HT₂ antagonist (K_i=2 nM)².
10 mg
50 mg

NS-100
Anpirtoline (D-16949)
6-Chloro-2-[piperidinyl-4-thio]pyridine·HCl
99%, MW=265.2 [98330-05-3] Storage: RT
Serotonin 5-HT_1B receptor agonist^3,4.
5 mg
25 mg

NS-085
CGS 12066B dimaleate
99%, MW=566.5 [109028-10-6] Storage: RT
Serotonin 5-HT_1B agonist⁵.
10 mg
50 mg

NS-102
Cinanserin
N-[2-[[3-(Dimethylamino)propyl]thio]phenyl]-3-phenyl-2-propenamide
99%, MW=340.5 [1166-34-3] Storage: -20°C
Serotonin 5-HT₂ antagonist^6,7.
10 mg
50 mg

NS-107
Dibenzepine HCl
99%, MW=331.8 [315-80-0] Storage: RT
Antipsychotic. Antidepressant.
100 mg
500 mg

NS-108
Dihydroergocristine mesylate
98%, MW=707.8 [24730-10-7] Storage: RT
Serotonin antagonist. Dopaminergic and adrenergic partial agonist⁸. Cognition enhancer⁹.
200 mg
1 g

NS-109
Fluperlapine
99%, MW=309.4 [67121-76-0] Storage: RT
Serotonin 5-HT₆/5-HT₇ receptor ligand¹⁰. Atypical antipsychotic agent¹¹.
100 mg
500 mg

NS-103
5-HTQ (N,N,N-Trimethylserotonin iodide)
2-(5-Hydroxy-3-indolyl)ethyltrimethylammonium iodide
98%, MW=346.2, Storage: RT
Quaternary salt of serotonin. Serotonin 5-HT₃ agonist¹².
10 mg
50 mg

NS-150
8-Hydroxy-DPAT HBr
(?-8-Hydroxydipropylaminotetralin·HBr
99%, MW=328.3 [87394-87-4] Storage: RT
Serotonin 5-HT_1A agonist¹³.
20 mg
100 mg

NS-515
Ketanserin tartrate
99%, MW=545.5 [74050-98-9] Storage: RT
Serotonin 5-HT₂/5-HT_1C antagonist¹⁴.
50 mg
250 mg

NS-530
MDL-72222
3-Tropanyl-3,5-dichlorobenzoate
99%, MW=314.2 [40796-97-2] Storage: RT
Serotonin 5-HT₃ antagonist¹⁵.
100 mg
500 mg

EI-167
Methiothepin maleate (Ro 8-6837)
98%, MW=472.6 [19728-88-2] Storage: RT
Serotonin 5-HT₁/5-HT₂ antagonist¹⁶. Potent 5-HT autoreceptor antagonist. It inhibits spontaneous as well as electrical and/or potassium evoked 5-HT release from various brain structures^17,18,19.
100 mg
500 mg

NS-490
(?-5-Methoxy-3-dipropylaminochroman·HCl
99%, MW=299.8, Storage: RT
Selective serotonin 5-HT_1A agonist²⁰.
5 mg
25 mg

NS-550
N-Methylquipazine dimaleate
99%, MW=459.4, Storage: RT
Serotonin 5-HT₃ agonist (more selective than quipazine)²¹.
20 mg
100 mg

NS-560
(?-Methylserotonin maleate
99%, MW=306.3 [304-52-9] Storage: 0°C
Serotonin 5-HT₂ agonist^22,23.
10 mg
50 mg

NS-570
2-Methylserotonin maleate
98%, MW=244.7 [78263-90-8] Storage: 0°C
Serotonin 5-HT₃ agonist^22,23.
10 mg
50 mg

NS-640
NAN-190
98%, MW=474.4 [115338-32-4] Storage: RT
Serotonin 5-HT_1A antagonist^24,25.
50 mg
250 mg

NS-660
1-(1-Naphthyl)piperazine·HCl
98%, MW=248.7 [57536-86-4] Storage: RT
Serotonin 5-HT₁ agonist²⁶. 5-HT₂ antagonist²⁷.
20 mg
100 mg

NS-700
6-Nitroquipazine maleate
98%, MW=374.3, Storage: RT
Serotonin uptake inhibitor^28,29.
10 mg
50 mg

NS-740
Pizotifen malate
99%, MW=429.6 [5189-11-7] Storage: RT
Serotonin receptor antagonist. 5-HT₃, K_i=42 nM³⁰. 5-HT₂, K_i=1-10 nM³¹. Antimigraine agent³².
100 mg
500 mg

NS-780
Quipazine dimaleate
98%, MW=445.4 [4774-24-7] Storage: 0°C
Serotonin 5-HT₃ agonist³³.
50 mg
250 mg

NS-820
Serotonin HCl
98%, MW=212.7 [153-98-0] Storage: 0°C
100 mg
1 g

NS-830
Spiroxatrine (R 5188)
99%, MW=379.4 [1054-88-2] Storage: RT
Serotonin 5-HT_1A antagonist³⁴.
20 mg
100 mg

NS-901
Y-25130
N-(1-Azabicyclo[2.2.2]oct-3-yl)-6-chloro-4-methyl-3-oxo-3,4-dihydro-2H-1,4-benzoxazine-8-carboxamide·HCl
99%, MW=386.3 [123040-16-4] Storage: RT
Potent and selective serotonin 5-HT₃ antagonist^35,36.
5 mg
25 mg

REFERENCES

1. A. Monge et al. J. Med. Chem. 1993 36 2745

2. A.M. Ismaiel et al. J. Med. Chem. 1993 36 2519

3. M.D. Swedberg et al. J. Pharmacol. Exp. Therap. 1992 263 1015

4. E. Schlicker et al. Brit. J. Pharmacol. 1992 105 732

5. R.F. Neale et al. Eur. J. Pharmacol. 1987 136 1

6. J.E. Leysen et al. Life. Sci. 1981 28 1015

7. P.J. Pauwels et al. Life. Sci. 1990 47 2009

8. Coppi et al. Arzneim. Forsch. 1990 42 1381

9. F. Drago et al. Pharmacol. Biochem. Behav. 1988 30 961

10. B.L. Roth et al. J. Pharmacol. Exp. Ther. 1994 268 1403

11. M. Matejcek et al. Arzneim. Forsch. 1984 34 114

12. B.P. Richardson et al. Nature 1985 316 126

13. D.N. Middlemiss et al. Eur. J. Pharmacol. 1983 90 151

14. J.E. Leysen et al. Mol. Pharmacol. 1982 21 301

15. B.P. Richardson et al. Trends Neuroscience 1986 9 424

16. A. Pazos et al. Eur. J. Pharmacol. 1985 106 539

17. C. Ennis and B. Cox Neuropharmacology 1982 21 41

18. M. Raiteri et al. J. Pharmacol. Exp. Ther. 1986 237 644

19. G.V. Rebec et al. Brain Res. 1982 251 374

20. J.M. Cossery Eur. J. Pharmacol. 1987 140 143

21. R.A. Glennon et al. Eur. J. Pharmacol. 1989 168 387

22. A.M. Ismaiel et al. J. Med. Chem. 1990 33 755

23. H.Wilson et al. J. Pharmacol. Exp. Ther. 1990 252 683

24. R.A. Glennon et al. J. Med. Chem. 1988 31 1968

25. R.A. Glennon et al. Eur. J. Pharmacol. 1988 154 339

26. R.A. Glennon et al. J. Med. Chem. 1987 30 1

27. M.L. Cohen et al. J. Pharmacol. Exp. Ther. 1985 233 75

28. K. Hashimoto and T. Goromaru Eur. J. Pharmacol. 1990 180 273

29. K. Hashimoto and T. Goromaru Biochem. Pharmacol. 1991 41 1679

30. A.W. Schmidt et al. Mol. Pharmacol. 1989 36 505

31. S.J. Peroutka et al. Ann. Neurol. 1988 23 500

32. E.J. Mylecharane et al. J. Neurol. 1991 238 S45

33. R.A. Glennon et al. J. Med. Chem. 1986 29 2375

34. P. Schoeffter and D. Hoyer Br. J. Pharmacol. 1988 95 975

35. T. Fukuda et al. Eur. J. Pharmacol. 1991 196 299

36. Y. Kagami-ishi et al. Eur. J. Pharmacol. 1992 224 51

SUBSTANCE P/NEUROKININS

P-501
Substance P
Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Gly-Leu-Met-NH₂
>97%, MW=1347.8 [12769-48-1] Storage: -20°C
Substance P (SP) was first discovered in 1931 by von Euler and Gaddum¹, and is the best characterized member of the neurokinins. This class of peptide neurotransmitters includes neurokinin A (NK-A) and B (NK-B)[see products below], and are characterized by the common C-terminal sequence Phe-X-Gly-Leu-Met-NH₂². The receptors for SP, NK-A and NK-B, designated NK₁, NK₂ and NK₃ respectively, are members of the G-protein coupled receptor superfamily³. All three receptors have been shown to stimulate inositol phospholipid hydrolysis. SP is involved in pain, smooth muscle contraction, secretion from exocrine and endocrine glands, inflammatory response including vasodilation, plasma extravasation and mobilization of immune system cells⁴.
1 mg
5 x 1 mg

P-505
Neurokinin A
His-Lys-Thr-Asp-Ser-Phe-Val-Gly-Leu-Met-NH₂
>97%, MW=1133.5 [86933-74-6] Storage: -20°C
Endogenous ligand for NK₂ receptor. Identical to substance K and neuromedin L⁵.
1 mg
5 x 1 mg

P-508
Neurokinin B
Asp-Met-His-Asp-Phe-Phe-Val-Gly-Leu-Met-NH₂
>97%, MW=1210.6 [86933-75-7] Storage: -20°C
Endogenous ligand for NK₃ receptor. Identical to neuromedin K.
1 mg
5 x 1 mg

EI-125
Capsaicin
99%, MW=305.4 [404-86-4] Storage: RT
Induces release of substance P from afferent nociceptive specific neurons^6,7.
200 mg
1 g

NK-101
Capsazepine
N-[2-(4-Chlorophenyl)ethyl]-1,3,4,5-tetrahydro-7,8-dihydroxy-2H-2-benzazepine-2-carbothioamide
98% MW=376.9 [138977-28-3] Storage: -20°C
Capsaicin antagonist^8,9. Inhibits resiniferatoxin and capsaicin-induced contractions of guinea pig trachea¹⁰. Inhibits C-fiber-smooth muscle contractions induced by capsaicin, bradykinin and neurokinin A¹¹.
5 mg
25 mg

NK-102
FK-888
98%, MW=588.7 [138449-07-7] Storage: -20°C
A potent nonpeptide neurokinin NK₁ receptor antagonist. IC₅₀ for displacement of [³H]-substance P is 6.9 nM in guinea pig lung. Blocks airway edema in the guinea pig induced by substance P (ED₅₀=4.2 mg/kg)^12,13.
1 mg
5 x 1 mg

NEW LOWER PRICE

NK-100
Resiniferatoxin
99%, MW=628.7 [57444-62-9] Storage: -20°C
Induces release of substance P from afferent nociceptive specific neurons^14,15. 1,000 to 10,000-fold more potent than capsaicin¹⁶.
1 mg
5 mg

P-502
[Sar-9, Met(O₂)-11]-Substance P
Arg-Pro-Lys-Pro-Gln-Gln-Phe-Phe-Sar-Leu-Met(O₂)-NH₂
>97%, MW=1392.7 [110880-55-2] Storage: -20°C
Highly selective NK₁ neurokinin receptor agonist¹⁷.
1 mg
5 x 1 mg

P-510
Sendide
[Tyr-6, D-Phe-7, D-His-9]-Substance P (6-11)
Tyr-D-Phe-Phe-D-His-Leu-Met-NH₂
>97%, MW=856.2, Storage: -20°C
Potent NK₁ neurokinin receptor antagonist¹⁸.
1 mg
5 x 1 mg

P-503
Spantide II
N--Nicotinoyl-D-Lys-Pro-3-Pyridyl-Ala-Pro-D-Cl₂Phe-Asn-D-Trp-Phe-D-Trp-Leu-Nle-NH₂
>97%, MW=1670.2, Storage: -20°C
Potent substance P antagonist¹⁹.
1 mg
5 mg

P-504
Spantide III
N--Nicotinoyl-D-Lys-Pro-3-Pyridyl-Ala-Pro-D-Cl₂Phe-Asn-D-Trp-Phe-D-3-Pyridyl-Ala-Leu-Nle-NH₂
A superior substance P antagonist with high potency and negligible neurotoxicity. More effective than spantide II¹⁹.
1 mg
5 mg

P-506
[-Ala-8]-Neurokinin A (4-10)
Asp-Ser-Phe-Val--Ala-Leu-Met-NH₂
>97%, MW=780.9, Storage: -20°C
Highly selective NK₂ neurokinin receptor agonist²⁰.
1 mg
5 mg

P-507
MEN10376
Asp-Tyr-D-Trp-Val-D-Trp-D-Trp-Lys-NH₂
>97%, MW=1081 [135306-85-3] Storage: -20°C
Highly selective NK₂ neurokinin receptor antagonist²¹.
1 mg
5 x 1 mg

P-509
Senktide
[Succinyl-Asp-6,N-Me-Phe-8]-Substance P (6-11)
Succinyl-Asp-Phe-(N-Me)Phe-Gly-Leu-Met-NH₂
>97%, MW=842.1 [106128-89-6] Storage: -20°C
Highly selective NK₃ neurokinin receptor agonist²².
1 mg
5 mg

REFERENCES

1. U.S. von Euler and J.H. Gaddum J. Physiol. (London) 1931 72 74

2. M.E. Logan et al. Ann. Reports Med. Chem. 1991 26 43

3. S. Guard and S.P. Watson Neurochem. Int. 1991 18 149

4. C.A. Maggi et al. J. Auton. Pharmacol. 1993 13 23

5. H.R. Eistetter et al. J. Cell. Biochem. 1993 52 84

6. S. Bevan and J. Szolcsanyi Trends Pharmacol. Sci. 1990 11 330

7. B. Pernow et al. J. Immunol. 1985 135 8125

8. C.A. Maggi et al. Br. J. Pharmacol. 1993 108 801

9. C.S.J. Walpole et al. J. Med. Chem. 1994 37 1942

10. J.L. Ellis and B.J. Undem J. Pharmacol. Exp. Therap. 1994 268 85

11. Z.Y. Wang and R. Hakanson Br. J. Pharmacol. 1993 110 1073

12. T. Fuji et al. Br. J. Pharmacol. 1992 107 785

13. Z.Y. Wang et al. Br. J. Pharmacol. 1994 111 1342

14. S. Bevan and J. Szolcsanyi Trends Pharmacol. Sci. 1990 11 330

15. J. Szolcsanyi et al. J. Pharmacol. Exp. Ther. 1990 255 923

16. A. Szallasi and P. Blumberg Neuroscience 1989 30 515

17. R. Quirion and T.V. Dam Regulatory Peptides 1988 22 18

18. T. Sakurada et al. Brain Res. 1992 593 319

19. K. Folkers et al. Amino Acids 1993 5 233

20. S. Evangelista et al. Peptides 1990 11 293

21. C.A. Maggi et al. J. Pharmacol. Exp. Therap. 1991 257 1172

22. R. Laufer et al. J. Biol. Chem. 1986 261 10257

MISCELLANEOUS

W-075
Benzphetamine·HCl (U-0441)
99%, MW=275.8 [5411-22-3] Storage: RT
Anorexic.
Controlled substance. Schedule 3.
100 mg
500 mg

N-140
Bilobalide
98%, MW=326.3 [33570-04-6] Storage: -20?
Bilobalide is a terpenoid isolated from Ginkgo biloba. It has been proposed to exert trophic and protective effects on neurons¹. It increases the sensitivity of mouse pancreatic beta cells to glucose² and displays protective effects during hypoxia³.
10 mg
50 mg

N-150
Chlorphenesin carbamate (U-19646)
99%, MW=245.7 [886-74-8] Storage: RT
Skeletal muscle relaxant.
1 g
5 g

EI-166
Debrisoquin sulfate (Ro 5-3307)
3,4-Dihydro-2(1H)-isoquinolinecarboxamidine ½H₂SO₄
99%, MW=224.3 [581-88-4] Storage: RT
Antihypertensive⁴. Metabolized to 4-hydroxydebrisoquin (See EI-169) by debrisoquin 4-hydroxylase⁵. Useful indicator for cytochrome P-450 polymorphism⁶.
50 mg
500 mg

J-120
(S)-Mephenytoin
98%, MW=218.2 [50-12-4] Storage: RT
Substrate for determination of cytochrome P-450 polymorphism^7,8. Anticonvulsant.
5 mg
25 mg

AD-100
PD 116,948
8-Cyclopentyl-1,3-dipropylxanthine
99%, MW=304.4 [102146-07-6] Storage: RT
Potent and selective adenosine A₁ receptor antagonist^9-13.
20 mg
100 mg

REFERENCES

1. C. Bruno et al. Planta Med. 1993 59 302

2. M. Vasseur et al. Gen. Pharmacol. 1994 25 31

3. D. Janssens et al. Biochem. Pharmacol. 1995 50 991

4. M.A. Medina et al. Biochem. Pharmacol. 1969 18 891

5. F.J. Gonzalez et al. DNA 1987 6 149

6. F.P. Guengerich Trends Pharmacol. Sci. 1989 10 107

7. F.P. Guengerich Trends Pharmacol. Sci. 1989 10 107

8. S.M. de Morais et al. Clin. Pharmacol. Ther. 1995 58 404

9. S.J. Haleen et al. Life Sci. 1987 40 555

10. M.G. Collis Trends Pharmacol. Sci. 1989 10 340

11. R.J. Knight et al. J. Pharm. Pharmacol. 1993 45 979

12. P.L. Martin and J.M. May J. Pharmacol. Exp. Therap. 1994 269 1228

13. R.S. Redman and E.M. Silinsky Mol. Pharmacol. 1993 44 835