Correlation between low/high affinity ratios for 5-HT(1A) receptors and intrinsic activity

European Journal of Pharmacology

Volumn 386, Issue 1, 1999, Pages 97-103

  Assié, Marie Bernadette ^a   Cosi, Cristina ^a   Koek, Wouter ^a  

^a INSTITUT DE RECHERCHE PIERRE FABRE   (France)

Author keywords

5 HT(1A) receptor ligand; Affinity; Dihydroergotamine; Efficacy; Gpp(NH)p shift; Intrinsic activity; S 14506

Indexed keywords

1 [2 (4 FLUOROBENZAMIDO)ETHYL] 4 (7 METHOXY 1 NAPHTHYL)PIPERAZINE; DIHYDROERGOTAMINE; G PROTEIN COUPLED RECEPTOR; GUANINE NUCLEOTIDE BINDING PROTEIN; GUANYLYLIMIDODIPHOSPHATE; PIPERAZINE DERIVATIVE; SEROTONIN 1A RECEPTOR; TETRALIN DERIVATIVE;

ANIMAL TISSUE; ARTICLE; BINDING AFFINITY; DRUG RECEPTOR BINDING; LIGAND BINDING; MALE; MOLECULAR INTERACTION; NONHUMAN; PRIORITY JOURNAL; RAT; RECEPTOR BLOCKING; RECEPTOR INTRINSIC ACTIVITY;

8-HYDROXY-2-(DI-N-PROPYLAMINO)TETRALIN; AMINOPYRIDINES; ANIMALS; FORSKOLIN; GTP-BINDING PROTEIN ALPHA SUBUNITS, GI-GO; GUANYLYL IMIDODIPHOSPHATE; HELA CELLS; HIPPOCAMPUS; HUMANS; MALE; MEMBRANES; PERTUSSIS TOXIN; PIPERAZINES; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, SEROTONIN; RECEPTORS, SEROTONIN, 5-HT1; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS; VIRULENCE FACTORS, BORDETELLA;

EID: 0033452903     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(99)00738-4     Document Type: Article

References (26)

1. Birdsall N.J., Lazareno S. To what extend can binding studies allow the quantification of affinity and efficacy? Ann. N. Y. Acad. Sci. 812:1997;41-47.
2. 1A agonist and potential anxiolytic agent. Drug Dev. Res. 26:1992;21-48.
3. 1A binding sites with G regulatory proteins. Biochem. Pharmacol. 39:1990;7-18.
4. 1A receptor. J. Biol. Chem. 264:1989;14848-14852.
5. 2C receptors: evidence favoring the ternary complex and two-state models of agonist action. J. Neurochem. 72:1999;2127-2134.
6. 1A receptors. Eur. J. Pharmacol. 237:1993;283-291.
7. 1A receptor antagonist, WAY 100635. Eur. J. Pharmacol. 281:1995;81-88.
8. 3H-PAT. Nature. 305:1983;140-142.
9. 1A receptors in rat brain membranes. Eur. J. Pharmacol., Mol. Pharmacol. Sect. 288:1995;173-186.
10. 3H]8-Hydroxy-2-(di-n-propylamino)tetralin binding to pre- and postsynaptic 5-hydroxytryptamine sites in various regions of the rat brain. J. Neurochem. 44:1985;1685-1696.
11. 1A receptors from bovine hippocampus. Cell. Mol. Neurobiol. 18:1998;535-553.
12. Kenakin T.P. Efficacy. Pharmacologic Analysis of Drug-Receptor Interaction. 2nd edn. 1993;249-277 Raven Press, New York.
13. Kobilka B. Adrenergic receptors as models for G protein-coupled receptors. Annu. Rev. Neurosci. 15:1992;87-114.
14. 1A receptor agonist with marked anxiolytic and antidepressant potential. J. Pharmacol. Exp. Ther. 287:1998;266-283.
15. 3H]p-MPPF. Synapse. 23:1996;344-346.
16. 2 guanine nucleotide-binding protein-coupled receptor-utilization of receptor state binding affinities. Mol. Pharmacol. 42:1992;432-438.
17. 3H-antagonists. Evidence for the presence of high and low affinity agonist-binding states. Mol. Pharmacol. 27:1985;171-183.
18. 1A receptors. J. Neural Transm. 104:1997;1059-1075.
19. McPherson G.A. Analysis of radioligand binding experiments. A Collection of Computer Programs for IBM PC. J. Pharmacol. Methods. 14:1985;213-228.
20. 3H]hydroxydipropylaminotetralin. J. Neurochem. 62:1994;1822-1834.
21. 35S]GTPγS binding study. Eur. J. Pharmacol. 355:1998;245-256.
22. 1A receptor agonists in recombinant cell lines - modulation of apparent efficacy by G protein activation state. Naunyn-Schmiedeberg's Arch. Pharmacol. 356:1997;551-561.
23. 1A receptors: intrinsic activity and modulation by G protein activation state. Naunyn-Schmiedeberg's Arch. Pharmacol. 357:1998;490-499.
24. 3H]-5-hydroxytryptamine binding sites in brain. Mol. Pharmacol. 34:1988;527-536.
25. 3H]lisuride labels free receptor and receptor coupled to G protein. J. Neurochem. 65:1995;1909-1916.
26. Thielen R.J., Fangon N.B., Frazer A. 4-(2′-Methoxyphenyl)-1-[2′-[N-(2″-pyridinyl)-p-iodobenzamido] ethyl]piperazine and 4-(2′-methoxyphenyl)-1-[2′-[N-(2″-pyridinyl)-p- fluorobenzamido]ethyl]piperazine, two new antagonists at pre- and postsynaptic serotonin-1A receptors. J. Pharmacol. Exp. Ther. 277:1996;661-670.