Pharmacological characterisation of the human 5-HT(2B)and 5-HT(2C) receptors in functional studies

Pharmacology Reviews and Communications

Volumn 9, Issue 4, 1997, Pages 259-268

  Wood, Martyn D ^a   Thomas, David R ^a   Gager, Tracey L ^a   Browne, Michael J ^b   Carey, Janet E ^b   Chambers, Jon K ^b   Gale, Davina G ^b   Hastwell, Christopher ^b   Muir, Alison I ^b   Pritchard, Trudy R ^b   Robinson, Jeffery H ^b   Wilson, Shelagh ^b   Brown, Anthony M ^a  

^a Departments of Psychiatry Research   (United Kingdom)

^b Departments of Biotechnology   (United Kingdom)

Author keywords

5 HT(2B) and 5 HT(2C) receptors; 5 Hydroxytryptamine; Constitutive coupling; Inverse agonism; Phosphoinositide hydrolysis

Indexed keywords

INOSITOL PHOSPHATE; RECEPTOR SUBTYPE; SEROTONIN 2B RECEPTOR; SEROTONIN 2C RECEPTOR; SEROTONIN AGONIST; SEROTONIN ANTAGONIST;

ARTICLE; CONTROLLED STUDY; HUMAN; HUMAN CELL; MOLECULAR CLONING; PRIORITY JOURNAL; PROTEIN CONFORMATION; PROTEIN EXPRESSION; RECEPTOR AFFINITY; STRUCTURE ACTIVITY RELATION;

EID: 6844253869     PISSN: 10288945     EISSN: None     Source Type: Journal    
DOI: None     Document Type: Article

References (25)

1. 2C) receptors reveal novel inverse agonist activity of receptor ligands," J. Biol Chem , 269, 11687-11690.
2. 2 receptor subtypes: a family re-united?" TiPS, 105, 105-110.
3. 2B receptors," Third IUPHAR satellite meeting on Serotonin, Chicago, Illinois, U.S.A., p. 75.
4. Baxter, G. S. and Tilford, N. S. (1995) "Endogenous ligands and inverse agonism," TiPS, 16, 258-259.
5. 2C receptors," Br. J. Pharmacol., 115, 622-628
6. 2B receptor, using extracellular acidification rates as a rapid, sensitive measure of receptor functionality: a paradigm for 'orphan' receptors. In Genomes, Molecular Biology and Drug Discovery (eds.) M.J. Browne and P.L. Thurlby (Academic Press, London), pp. 187-188.
7. Cohen, M. L. and Fludzinski, L. A. (1987) "Contractile serotonergic receptor in rat stomach fundus," J. Pharmacol & Exp. Ther., 243, 264-269.
8. 2C receptor antagonist with improved affinity, selectivity and oral activity," J. Med Chem., 38, 2524-2530.
9. Gardner, B. (1995) "Molecular mechanism of agonism," TiPS, 16, 259-260.
10. Hoyer, D., Clarke, D. E., Fozard, J. R., Hartig, J. R., Martin, G. R., Mylecharane, E. J., Saxena, P. R. and Humphrey, P P. A. (1994) "International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (5-HT)," Pharmacol. Rev., 46, 157-203.
11. 1C receptor-mediated stimulation of inositol phosphate production in pig choroid plexus. A pharmacological characterization," Naunyn-Schmiedeberg's Arch Pharmacol., 339, 252-258.
12. Kenakin, T. (1993) Pharmacologic analysis of drug-receplor interaction. (Raven Press, New York).
13. Kenakin, T. (1995) "Pharmacological proteus?" TiPS, 16, 256-258.
14. 2B receptor antagonist with anxiolyric-like properties," Br. J. Pharmacol., 117, 427-434.
15. 2B) from rat stomach fundus," Mol. Pharmacol., 42, 549-557.
16. Labreque, J., Fargin, A., Bouvier, M., Chidiac, P and Dennis, M. (1995) "Serotonergic antagonists differentially inhibit spontaneous activity and decrease ligand binding capacity of the rat 5-hydroxytryptamme type 2C receptor in Sf9 cells," Mol. Pharmacol., 48, 150-159.
17. Leff, P. (1995) "The two-state model of receptor activation," TiPS, 16, 89-97.
18. Lefkowitz, R. J., Cotecchia, S., Samama, P. and Costa, T. (1993) "Constitutive activity of receptors couple to guanine nucleotide regulatory proteins," TiPS, 14, 303-307.
19. 2A receptor expressed in the human neuroblastoma cell line SH-SY5Y," Br. J. Pharmacol., 112, 97P.
20. 2) subfamily of receptors: pharmacological challenges," Med. Chem. Res., 3, 306-316.
21. 1C receptors," Biochem. Biophys. Res. Commun., 181, 1469-1478.
22. 1D receptor subtypes," J. Rec. & Sig. Trans. Res., 15, 199-211.
23. 2B receptor," NeuroReport, 7, 1457-1460.
24. Westphal, R. S. and Sanders-Bush, E. (1994) "Reciprocal binding properties of 5-hydroxytryptamine type 2C receptor agonists and inverse agonists," Mol Pharmacol., 46, 937-942.
25. 2A receptor," Pharmacol. Comm., 5, 109-116.