GR127935 acts as a partial agonist at recombinant human 5-HT(1Dα) and 5-HT(1Dβ) receptors

European Journal of Pharmacology

Volumn 314, Issue 3, 1996, Pages 365-372

  Watson, Jeannette M ^a   Burton, Melanie J ^a   Price, Gary W ^a   Jones, Brian J ^a   Middlemiss, Derek N ^a  

^a GLAXOSMITHKLINE   (United Kingdom)

Author keywords

5 HT(1D ) receptor; 5 HT(1D ) receptor; 35S GTP S binding; CAMP accumulation; GR127935; Receptor reserve

Indexed keywords

CYCLIC AMP; GUANINE NUCLEOTIDE BINDING PROTEIN; METITEPINE; N [4 METHOXY 3 (4 METHYL 1 PIPERAZINYL)PHENYL] 2' METHYL 4' (5 METHYL 1,2,4 OXADIAZOL 3 YL)[1,1' BIPHENYL] 4 CARBOXAMIDE; RECEPTOR SUBTYPE; SEROTONIN; SEROTONIN 1D RECEPTOR;

ANIMAL CELL; ARTICLE; BINDING AFFINITY; CELL LINE; CHO CELL; CONTROLLED STUDY; DRUG RECEPTOR BINDING; GENE EXPRESSION; HUMAN; NONHUMAN; PRIORITY JOURNAL; TECHNIQUE;

ADENYLATE CYCLASE; ALKYLATING AGENTS; ANIMALS; CHO CELLS; CRICETINAE; CYCLIC AMP; GTP-BINDING PROTEINS; GUANOSINE 5'-O-(3-THIOTRIPHOSPHATE); HUMANS; LOGISTIC MODELS; OXADIAZOLES; PIPERAZINES; QUINOLINES; RECEPTORS, SEROTONIN; RECOMBINANT PROTEINS; SEROTONIN AGONISTS; SEROTONIN ANTAGONISTS;

EID: 0030608352     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(96)00579-1     Document Type: Article

References (30)

1. 1B receptor expression system, Mol. Pharmacol. 43, 427.
2. 1B receptors are negatively coupled with adenylate cyclase in rat substantia nigra, Eur. J. Pharmacol. 151, 189.
3. Crocker, A.D. and D.L. Cameron, 1989, Receptor alkylating agents: novel tools for the study of receptor function in the central nervous system of the rat, Clin. Exp. Pharmacol. Physiol. 16, 545.
4. 2-adrenergic receptors to two G-proteins with opposing effects, J. Biol. Chem. 267, 15795.
5. 1D type serotonin receptor, Mol. Pharmacol. 40, 43.
6. 1D receptors mediate SKF 99101H-induced hypothermia in the guinea-pig, J. Psychopharmacol. 93, 234.
7. Hoyer, D. and D.N. Middlemiss, 1989, Species differences in the pharmacology of terminal 5-HT autoreceptors in mammalian brain, Trends Pharmacol. Sci. 13, 130.
8. Hoyer, D., D.E. Clarke, J.R. Fozard, P.R. Hartig, G.R. Martin, E.J. Mylecharane, P.R. Saxena and P.P. Humphrey, 1994, International union of pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin), Pharmacol. Rev. 46, 157.
9. Jones, S.V.P., C.J. Heilman and M.R. Brann, 1991, Functional responses of cloned muscarinic receptors expressed in CHO-K1 cells, Mol. Pharmacol, 40, 242.
10. Lazareno, S., T. Farries and N.J.M. Birdsall, 1993, Pharmacological characterisation of guanine-nucleotide exchange reactions in membranes from CHO cells stably transfected with human muscarinic receptors M1-M4, Life Sci. 52, 449.
11. 1D serotonin receptor, Biochem. Biophys. Res. Commun. 180, 1460.
12. Manuel, N.A., D.I. Wallis and H. Crick, 1995, Ketanserin-sensitive depressant actions of 5-HT receptor agonists in the neonatal rat spinal cord, Br. J. Pharmacol. 116, 2647.
13. Matesic, D.F. and G.R. Luthin, 1991, Atropine dissociates complexes of muscarinic acetylcholine receptor and guanine nucleotide-binding protein in heart membranes, FEBS Lett. 284, 184.
14. Murphy, T.J. and D.B. Bylund, 1989, Characterisation of serotonin-1B receptor negatively coupled to adenylate cyclase in OK cells, a renal epthelial cell line from the opossum, J. Pharmacol. Exp. Ther. 249, 535.
15. 1B receptors, Eur. J. Pharmacol. Mol. Pharmacol. Sect. 290, 95.
16. 1D receptor antagonist, GR127935, on in vivo 5-HT release, synthesis and turnover in the guinea-pig frontal cortex, Br. J. Pharmacol. 112, 489P.
17. Roberts, C., J. Watson, M. Burton, G.W. Price, D.N. Middlemiss and B.J. Jones, 1996, Functional characterisation of the 5-HT terminal autoreceptor in the guinea-pig brain cortex, Br. J. Pharmacol. 117, 384.
18. Samama, P., P. Gang, T. Costa, S. Cotecchia and R.J. Leftkowitz, 1994, Negative antagonists promote an inactive conformation of the β-2 adrenergic receptor, Mol. Pharmacol. 45, 390.
19. 1D receptor subtype, Naunyn-Schmied. Arch. Pharmacol. 340, 45.
20. 1D receptor antagonist, Br. J. Pharmacol. 110, 9P.
21. 1D receptor antagonist GR127935 on extracellular levels of 5-HT in the guinea-pig frontal cortex as measured by microdialysis, Neuropharmacology 34, 377.
22. 1D autoreceptors modulate stimulated 5-HT release in the guinea-pig dorsal raphe nucleus, Br. J. Pharmacol. 110, C102.
23. 1A autoreceptors modulate 5-HT release in the guinea-pig dorsal raphe nucleus, Neuropharmacology 33, 393.
24. 1D receptor subtypes, J. Rec. Sig. Trans, Res. 15, 199.
25. 1D receptor can both activate and inhibit adenylate cyclase in transfected cells, Eur. J. Pharmacol. 247, 177.
26. 1Dβ receptors, Eur. J. Pharmacol, 287, 79.
27. Watson, J., 1995, In vitro measurement of the second messenger cAMP: ria vs flashplates, Biotech Update 10, 11.
28. 1Dα receptor is positively coupled to adenylyl cyclase in transfected CHO cells, Br. J. Pharmacol. 112, 301P
29. 1Dβ, Proc. Natl. Acad. Sci. USA 89, 3630.
30. 1D subtypes, Naunyn-Schmied. Arch. Pharmacol. 354, 226.