The putative <> 5-HT(1A) receptor antagonist, WAY 100635, has inverse agonist properties at cloned human 5-HT(1A) receptors

European Journal of Pharmacology

Volumn 401, Issue 1, 2000, Pages 9-15

  Cosi, Cristina ^a   Koek, Wouter ^a  

^a INSTITUT DE RECHERCHE PIERRE FABRE   (France)

Author keywords

5 HT(1A) receptor; 35S GTP S binding; Inverse agonist; WAY 100635

Indexed keywords

GUANINE NUCLEOTIDE BINDING PROTEIN; N [2 [4 (2 METHOXYPHENYL) 1 PIPERAZINYL]ETHYL] N (2 PYRIDYL)CYCLOHEXANECARBOXAMIDE; SEROTONIN 1A ANTAGONIST; SPIPERONE;

AGONIST; ARTICLE; CHO CELL; CONTROLLED STUDY; DRUG PROTEIN BINDING; HELA CELL; HUMAN; HUMAN CELL; MEMBRANE; PRIORITY JOURNAL;

BINDING, COMPETITIVE; CELL MEMBRANE; DNA, RECOMBINANT; DOSE-RESPONSE RELATIONSHIP, DRUG; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HELA CELLS; HUMANS; PIPERAZINES; PYRIDINES; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; SODIUM CHLORIDE; SPIPERONE; SULFUR RADIOISOTOPES;

EID: 0034726024     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(00)00410-6     Document Type: Article

References (18)

1. 1A receptor antagonists on hippocampal 5-hydroxytryptamine levels: (s)-WAY 100135, but not WAY 100635, has partial agonist properties. Eur. J. Pharmacol. 304:1996;15-21.
2. 1A receptor co-expressed in Spodoptera frugiperda cells: distinguishing inverse agonists from neutral antagonists. J. Biol. Chem. 272(52):1997;32979-32987.
3. Costa T., Lang J., Gless C., Herz A. Spontaneous association between opioid receptors and GTP-binding regulatory proteins in native membranes: specific regulation by antagonists and sodium ions. Mol. Pharmacol. 37:1990;383-394.
4. Costa T., Ogino T.Y., Munson P.J., Onaran H.O., Rodbard D. Drug efficacy at guanine nucleotide-binding regulatory protein-linked receptors: thermodynamic interpretation of negative antagonism and of receptor activity in absence of ligand. Mol. Pharmacol. 41:1992;549-560.
5. 1A receptor. J. Biol.Chem. 264:1989;14848-14852.
6. 1A receptor agonist. Behav. Brain Res. 73:1996;337-353.
7. 1A receptor antagonist, WAY 100635. Eur. J. Pharmacol. 281:1995;81-88.
8. 1Dα/1Dβ receptors. Ann. N. Y. Acad. Sci. 812:1997;236-239.
9. +, 5′-guanylylimido-diphosphate, amiloride and ethylisopropylamiloride: evidence for receptor-G protein precoupling. J. Pharmacol. Exp. Ther. 252:1990;1184-1196.
10. 1A receptors. J. Neurochem. 74:2000;347-357.
11. 1A receptors by the inverse agonist, spiperone but not the neutral antagonist, WAY 100635. Br. J. Pharmacol. 120:1997;737-739.
12. 35S]GTPγS binding study. Eur. J. Pharmacol. 355:1998;245-256.
13. 1A and histamine H1 receptors in HeLa cells stimulate phosphoinositide hydrolysis and phosphate uptake via distinct G protein pools. J. Biol. Chem. 266:1991;372-379.
14. 1A receptor-mediated hyperpolarization of the rat isolated superior cervical ganglion. Naunyn-Schmiedeberg's Arch. Pharmacol. 348:1993;225-227.
15. 35S]GTPγS binding. Eur. J. Pharmacol. 320:1997;267-275.
16. Tallarida R.J., Murray R.B. Manual of Pharmacological Calculations. 1987;Springer, New York.
17. o-linked receptors and its allosteric regulation by monovalent cations. Life Sci. 52:1993;1899-1907.
18. Tian W.-N., Duzic E., Lanier S.M., Deth C.R. Determinations of α2-adrenergic receptor activation of G proteins: evidence for a precoupled receptor/G protein state. Mol. Pharmacol. 45:1994;524-531.