RS-102221: A novel high affinity and selective, 5-HT(2C) receptor antagonist

Neuropharmacology

Volumn 36, Issue 4-5, 1997, Pages 621-629

  Bonhaus, D W ^a   Weinhardt, K K ^a   Taylor, M ^a   Desouza, A ^a   Mcneeley, P M ^a   Szczepanski, K ^a   Fontana, D J ^a   Trinh, J ^a   Rocha, C L ^a   Dawson, M W ^a   Flippin, L A ^a   Eglen, R M ^a  

^a ROCHE BIOSCIENCE   (United States)

Author keywords

5 HT; 5 HT(2C) receptor; 5 HT(2C) receptor antagonist

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; 1 METHYL 3 INDOLECARBOXYLIC ACID [1 [2 (METHYLSULFONYLAMINO)ETHYL] 4 PIPERIDINYLMETHYL] ESTER; 5 METHOXYTRYPTAMINE; 8 [4 (5 AMINO 2,4 DIMETHOXYBENZOYL)BUTYL] 1,3,8 TRIAZASPIRO[4.5]DECANE 2,4 DIONE; BUSPIRONE; CLOZAPINE; CYPROHEPTADINE; ERGOTAMINE; FLUOXETINE; HALOPERIDOL; KETANSERIN; LISURIDE; METITEPINE; MIANSERIN; PAROXETINE; RADIOLIGAND; RAUWOLSCINE; RECEPTOR SUBTYPE; SEROTONIN; SEROTONIN 1C RECEPTOR; SEROTONIN 2 AGONIST; SEROTONIN 2 ANTAGONIST; SEROTONIN 2A RECEPTOR; SEROTONIN 2B RECEPTOR; SEROTONIN 2C ANTAGONIST; SEROTONIN AGONIST; SEROTONIN ANTAGONIST; SUMATRIPTAN; TRYPTAMINE; UNCLASSIFIED DRUG; UNINDEXED DRUG;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BEHAVIOR; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG SELECTIVITY; FOOD INTAKE; HUMAN; INTRAPERITONEAL DRUG ADMINISTRATION; LOCOMOTION; MALE; MOLECULAR CLONING; NONHUMAN; PRIORITY JOURNAL; PROTON TRANSPORT; RAT; RECEPTOR AFFINITY; RECEPTOR BINDING; WEIGHT GAIN;

ANIMALS; CELL MEMBRANE; CHO CELLS; CRICETINAE; FEEDING BEHAVIOR; FEMALE; GUINEA PIGS; HUMANS; HYDROGEN; LIGANDS; MALE; MOTOR ACTIVITY; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SEROTONIN; SEROTONIN ANTAGONISTS; SPIRO COMPOUNDS; SULFONAMIDES; WEIGHT GAIN;

EID: 0030903068     PISSN: 00283908     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0028-3908(97)00049-X     Document Type: Article

References (53)

1. 2C receptor protein in human and rat brain using specific antisera. Neuropharmacology 34: 1635-1645.
2. 2C receptors. Journal of Neurochemistry 64: 2473-2479.
3. 2B) contractile receptor in the rat stomach fundus. Journal of Medical Chemistry 39: 2773-2780.
4. 2 receptor stimulation on excessive grooming, penile erection and plasma oxytocin concentrations. European Journal of Pharmacology 229: 9-14.
5. Battey J. F. et al. (1994) The RBI Handbook of Receptor Classification (J. W. Kebabian and J. L. Neumeyer Eds) Research Biochemicals International, Natick, MA.
6. 2 receptor subtypes: a family re-united? Trends in Pharmacological Science 16: 105-110.
7. 2B receptors. Behavioural Brain Research 73: 149-152.
8. 1C-receptors in drug-induced penile erections in rats. Psychopharmacology 101: 57-61.
9. 2C receptors. British Journal of Pharmacology 115: 622-628.
10. Boyson S. J. and Alexander A. (1990) Net production of cerebrospinal fluid is decreased by SCH-23390. Annals of Neurology 27: 631-635.
11. Brewerton T. D., Murhpy D. L., Mueller E. A. and Jimerson D. C. (1988) Induction of migraine like headaches by the serotonin agonist m-chlorophenylpiperazine. Clinical and Pharmacological Therapeutics 43: 605-609.
12. 1C sites. European Journal of Pharmacology 191: 93-96.
13. 2C serotonin receptor to G proteins in Xenopus oocytes. Neuroscience Letters 179: 100-102.
14. 50) of an enzymatic reaction. Biochemistry of Pharmacology 92: 881-894.
15. Conn P. J., Sanders-Bush E., Hoffman B. J. and Hartig P. R. (1986) A unique serotonin receptor in choroid plexus is linked to phosphatidylinositol turnover. Proceedings of the National Academy of Science U.S.A. 83: 4086-4088.
16. Curzon G. (1991) Effects of tryptophan and of 5-hydroxytryptamine receptor subtype agonists on feeding. Advances in Experimental Medical Biology 294: 377-388.
17. 1C receptors. Trends in Pharmacological Science 11: 181-182.
18. 2/1C antagonist, and negative symptoms in schizophrenia. A placebo-controlled double-blind trial. British Journal of Psychiatry 163: 451-455.
19. 1C receptors in choroid plexus epithelium. Journal of Neuroscience 12: 4775-4782.
20. 2C receptor-mediated phosphoinositide turnover and the stimulus effects of m-chlorophenyl piperazine. Psychopharmacology 122: 237-243.
21. 2 and stomach fundus serotonin receptor genes. Neuroreport 3: 345-348.
22. 1C receptor antagonist. Journal of Medical Chemistry 36: 1104-1107.
23. 2B receptor antagonist with improved affinity, selectivity, and oral activity. Journal of Medical Chemistry 38: 2524-2530.
24. 1C receptor activation: a key step in the initiation of migraine? Trends in Pharmacological Science 10: 307-309.
25. Galanopoulou P., Giannacopoulos G., Theophanopoulos C., Couvaris M. K. and Varonos D. (1990) Behavioural changes on diet selection and serotonin (5-HT) turnover in rats under pizotifen treatment. Pharmacology and Biochemistry of Behaviour 37: 461-464.
26. 2A receptors expressed in fibroblasts. Journal of Pharmacology and Experimental Therapeutics 271: 1122-1126.
27. 1C receptor mRNA in adult rat brain. FEBS Letters 247: 453-462.
28. 2 recognition sites. Brain Research 376: 97-107.
29. Hoyer D., Clarke D. E., Fozard J. R., Hartig P. R., Martin G. R., Mylecharane E. J., Saxena P. R. and Humphrey P. A. (1994) International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacology Review 46: 157-203.
30. Kahn, R. S. and Wetzler, S. (1991) m-Chorophenylpiperazine as probe of serotonin function. Biological Psychiatry 30: 1139-1165.
31. 2C receptor stimulates cyclic GMP formation in choroid plexus. Journal of Neurochemistry 64: 199-205.
32. 2C receptors. Neuroscience Letters 206: 153-156.
33. 2C receptor antagonists are anxiolytic in the rat Geller-Seifter model of anxiety. Psychopharmacology 114: 90-96.
34. 2C/2B receptor antagonist. British Journal of Pharmacol. 111, 797-802.
35. 2B receptor antagonist, in two conflict models of anxiety. Psychopharmacology 118: 178-182.
36. 2B receptor antagonist with anxiolytic-like properties. British Journal of Pharmacology 117: 427-434.
37. 1C receptors. British Journal of Pharmacology 94: 137-147.
38. 1C receptors mediate 1-3(chlorophenyl)piperazine-mduced hypophagia. British Journal of Pharmacology 103: 2016-2020.
39. Klodzinska A., Jaros T., Chojnacka-Wojcik E. and Maj J. (1989) Exploratory hypoactivity induced by m-trifluoromethylphenylpiperazine (TFMPP) and m-chlorophenylpiperazine (m-CPP). Journal of Neural Transmission (Parkinsons Disease and Dementia Section) 1: 207-218.
40. 2F) from rat stomach fundus. Molecular Pharmacology 42: 549-557.
41. 2B receptor. Molecular Pharmacology 46: 227-234.
42. Martin G. R. and Humphrey P. P. A. (1994) receptors for 5-hydroxytryptamine: current perspectives on classification and nomenclature. Neuropharmacology 33: 261-273.
43. 2C receptors. Psychopharmacology 123: 333-339.
44. McConnell H. M., Owicki J. C., Parce J. W., Miller D. L., Baxter G. T., Wada H. G. and Pitchford S. (1992) The cytosensor microphysiometer: biological applications of silicon technology. Science 257: 1906-1912.
45. 1C receptor is a prominent serotonin receptor subtype in the central nervous system. Proceedings of the National Academy of Science U.S.A. 86: 6793-6797.
46. 2A receptor affinity. Journal of Medical Chemistry. 38, 28-33.
47. 1C receptor subtypes. Biochemistry and Biophysics Research Communications 181: 1469-1478.
48. Shih J. C., Yang W., Chen K. and Gallaher T. (1991) Molecular biology of serotonin (5-HT) receptors. Pharmacology and Biochemistry of Behaviour 40: 1053-1058.
49. 2c receptor gene. Neuroreport 7: 169-172.
50. 2c serotonin receptors. Nature 374: 542-546.
51. 2B receptor-mediated? British Journal of Pharmacology 116: 449P.
52. Ullmer C., Schmuck K., Kalkman H. O. and Lubbert H. (1995) Expression of serotonin receptor mRNAs in blood vessels. FEBS Letters 370: 215-221.
53. 2C receptor. Bioorganics and Medical Chemistry Letters 6: 2687-2692.