Functional characterization of agonists at recombinant human 5-HT(2A), 5-HT(2B) and 5-HT(2C) receptors in CHO-K1 cells

British Journal of Pharmacology

Volumn 128, Issue 1, 1999, Pages 13-20

  Porter, R H P ^a   Benwell, K R ^a   Lamb, H ^a   Malcolm, C S ^a   Allen, N H ^a   Revell, D F ^a   Adams, D R ^a   Sheardown, M J ^a  

^a NONE

Author keywords

5 HT(2A); 5 HT(2B); 5 HT(2C); Calcium; FLIPR; Fluorescence; Receptors; Ro 60 0175; Serotonin

Indexed keywords

(3 CHLOROPHENYL)PIPERAZINE; 1 [5 (2 THIENYLMETHOXY) 3 INDOLYL] 2 PROPANAMINE; 2 (6 CHLORO 5 FLUORO 1 INDOLYL) 1 METHYLETHYLAMINE; 6 CHLORO 2 (1 PIPERAZINYL)PYRAZINE; NORFENFLURAMINE; ORG 12962; ORG 37684; PIPERAZINE DERIVATIVE; SEROTONIN 2 RECEPTOR; SEROTONIN 2A AGONIST; SEROTONIN 2B RECEPTOR; SEROTONIN 2C AGONIST; SEROTONIN AGONIST; TRYPTAMINE; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CALCIUM CELL LEVEL; CHO CELL; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; DRUG RECEPTOR BINDING; DRUG STRUCTURE; FLUOROMETRY; NONHUMAN; PRIORITY JOURNAL; REVERSE TRANSCRIPTION POLYMERASE CHAIN REACTION;

ANIMALS; CALCIUM; CALCIUM SIGNALING; CHO CELLS; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; FLUORESCENT DYES; HUMANS; RECEPTOR, SEROTONIN, 5-HT2A; RECEPTOR, SEROTONIN, 5-HT2B; RECEPTOR, SEROTONIN, 5-HT2C; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; REVERSE TRANSCRIPTASE POLYMERASE CHAIN REACTION; SEROTONIN AGONISTS; TIME FACTORS; TRANSFECTION;

EID: 0032858740     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0702751     Document Type: Article

References (43)

1. 2C receptors. J. Neurochem., 64, 2473-2479.
2. 2B receptors. Behav. Brain Res., 73, 149-152.
3. 2B) in rat stomach fundus longitudinal muscle. Br. J. Pharmacol., 112, 323-331.
4. Berg, K.A., Maayani, S., Goldfarb, J., Scaramellini, C., Leff, P. & Clarke, W.P. (1998). Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors: Evidence for agonist-directed trafficking of receptor stimulus. Mol. Pharmacol., 54, 94-104.
5. 2C Receptors. Synthesis and biological evaluation of substituted 2-(Indol-1-yl)-1-methylethylamines and 2-(Indeno[1,2-b]pyrrol-1-yl)-1-methylethylamines. Improved therapeutics for obsessive compulsive disorder. J. Med. Chem., 40, 2762-2769.
6. 2C receptors. Br. J. Pharmacol., 115, 622-628.
7. Burns, C.M., Chu, H., Rueter, S.M., Hutchinson, L.K., Canton, H., Sanders-Bush, E. & Emeson, R.B. (1997). Regulation of serotonin-2C receptor G-protein coupling by RNA editing. Nature, 387, 303-308.
8. Conklin, D.S., Krause, C.M., Marshall, A.P., Patterson, J.P., Iyer, G., Tran, D.P., Largent, B.L., Jonak, G.J., Hartig, P.R. & Fitzgerald, L.W. (1998). Functional differences between edited isoforms of the human serotonin 5-HT2C receptor are accompanied by commensurate changes in agonist binding affinities. Soc. Neurosci. Abstr., 24, p. 1098.
9. Conn, P.J. & Sanders-Bush, E. (1987). Relative efficacies of piperazines at the phosphoinositide hydrolysis-linked serotonergic (5-HT-2 and 5-HT-1C) receptors. J. Pharmacol. Exp. Ther., 242, 552-557.
10. Dourish, C.T. (1995). Multiple serotonin receptors: opportunities for new treatment for obesity? Obes. Res., 3, 449S-462S.
11. Duxon, M.S., Flanigan, T.P., Reavley, A.C., Baxter, G.S., Blackburn, T.P. & Fone, K.C.F. (1997). Evidence for expression of the 5-hydroxytryptamine-2B receptor protein in the rat central nervous system. Neuroscience, 76, 323-329.
12. 2C receptors. Psychopharmacol., 136, 409-414.
13. 1B receptor on CHO cells: functional responses in the absence of radioligand binding. Br. J. Pharmacol., 117, 1119-1126.
14. Hoyer, D., Clarke, D.E., Fozard, J.R., Hartig, P.R., Martin, G.R., Mylecharane, E.J., Saxena, P.R. & Humphrey, P.P.A. (1994). International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (serotonin). Pharmacol. Rev., 46, 157-203.
15. Humphrey, P.P.A., Hartig, P. & Hoyer, D. (1993). A proposed new nomenclature for 5-HT receptors. Trends Pharmacol. Sci., 14, 233-236.
16. Iyer, G., Tran, D.P., Conklin, D.S., Patterson, J., Krause, C., Fitzgerald, L.W., Hartig, P. & Jonak, G.J. (1998). Identification and characterisation of 5-HT2C receptor edited isoforms in human brain. Soc. Neurosci. Abstr., 24, 1098.
17. 2 receptor. Eur. J. Pharmacol., 239, 111-118.
18. Johnson, M.P., Loncharich, R.J., Baez, M. & Nelson, D.L. (1994). Species variations in transmembrane region V of the 5-hydroxtryplamine type 2A receptor alter the structure-activity relationship of certain ergolamines and tryptamines. Mol. Pharmacol., 45, 277-286.
19. 1C Receptors and their therapeutic relevance. Curr. Opin. Invest. Drugs, 2, 317-362.
20. 2B receptor agonist, causes hyperphagia and reduced grooming in rats. Neuropharmacology, 36, 233-239.
21. 2B receptor agonist, BW 723C86, on three rat models of anxiety. Br. J. Pharmacol., 117, 1443-1448.
22. 2B receptor. Mol. Pharmacol., 46, 227-234.
23. 2C receptor as potential antidepressants and anxiolytics. Trends in Drug Res II., pp 49-61.
24. 2 receptor subfamily. Life Sci., 59, 1081-1095.
25. 2A receptors on interneurons in rat piriform cortex. J. Pharmacol. Exp. Ther., 278, 1373-1382.
26. Martin, G.R. & Humphrey, P.P.A. (1994). Receptors for 5-hydroxytryptamine: Current perspectives on classification and nomenclature. Neuropharmacology, 33, 261-273.
27. 2C Receptor agonists: Pharmacological characteristics and therapeutic potential. J. Pharmacol. Exp. Ther., 286, 913-924.
28. 2 receptor: Structurally specific differentiation by crgolamines and tryptamines. J. Pharmacol. Exp. Ther., 265, 1272-1279.
29. 2C receptors expressed in the human neuroblastoma cell line SH-SY5Y: Comparative stimulation by hallucinogenic drugs. J. Neurochem., 67, 2521-2531.
30. Niswender, C.M., Copeland, S.C., Herrick-Davis, K., Emeson, R.B. & Sanders-Bush, E. (1999). RNA editing of the human serotonin 5-hydroxytrptamine 2C receptor silences constitutive activity. J. Biol. Chem., 274, 9472-9478.
31. 2C receptor. Ann. N.Y. Acad Sci., 861, 38-48.
32. 2C receptors. Mol. Brain Res., 23, 163-178.
33. 2C): where structure meets function. Pharmacol. Ther., 79, 231-257.
34. 2A receptor in NIH-3T3 cells: Agonist induced down-regulation involves decreases in receptor RNA and number. J. Neurochem., 68, 1998-2011.
35. Saucier, C., Morris, S.J. & Albert, P.R. (1998). Endogenous serotonin - 2A and - 2C receptors in Balb/c-3T3 cells revealed in serotonin-free medium. Biochem. Pharmacol., 56, 1347-1357.
36. 2 serotonin receptor. FEBS Lett., 342, 85-90.
37. Schroeder, K.S. & Neagle, B.D. (1996). FLIPR: A new instrument for accurate, high throughput optical screening. J. Biomol. Screening, 1, 75-80.
38. 2B receptor. NeuroReport, 7, 1457-1460.
39. 2 receptor as a site of action for LSD and phenylisopropylamine hallucinogens. Psychopharmacology, 94, 213-216.
40. 2B receptor: evidence for species differences. J. Pharmacol. Exp. Ther., 276, 720-727.
41. Westphal, R.S. & Sanders-Bush, E. (1994). Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists. Mol. Pharmacol., 46, 937-942.
42. 2C receptors in functional studies. Pharmacol. Rev. Commun., 9, 259-268.
43. 2C receptor. Soc. Neurosci. Abstr., 24, 1371.