An innovative method for rapid characterisation of phospholipase C activity: SB242,084 competitively antagonises 5-HT(2C) receptor-mediated [3H]phosphatidylinositol depletion

Naunyn-Schmiedeberg's Archives of Pharmacology

Volumn 361, Issue 2, 2000, Pages 221-223

  Cussac, Didier ^a   Newman Tancredi, Adrian ^a   Quentric, Yann ^a   Millan, Mark J ^a  

^a INSTITUT DE RECHERCHES SERVIER   (France)

Author keywords

5 HT(2C) receptors; Phosphatidylinositol; Phospholipase C; SB242,084

Indexed keywords

6 CHLORO 5 METHYL 1 [6 (2 METHYLPYRIDIN 3 YLOXY) PYRIDIN 3 YLCARBAMOYL]INDOLINE; 6 CHLORO 5 METHYL 1 [[2 [(2 METHYL 3 PYRIDYL)OXY] 5 PYRIDYL]CARBAMOYL]INDOLINE; MESULERGINE; PHOSPHATIDYLINOSITOL; PHOSPHOLIPASE C; SEROTONIN; SEROTONIN 2C ANTAGONIST; SEROTONIN 2C RECEPTOR; TRITIUM; UNCLASSIFIED DRUG;

ANIMAL CELL; ARTICLE; CELL MEMBRANE; CHO CELL; COMPETITIVE INHIBITION; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG EFFECT; ENZYME ACTIVITY; NONHUMAN; PROTEIN CONTENT; PROTEIN DEPLETION; PROTEIN EXPRESSION; RECEPTOR AFFINITY; RECEPTOR BLOCKING;

AMINOPYRIDINES; ANIMALS; CHO CELLS; CRICETINAE; ERGOLINES; HUMANS; INDOLES; PHOSPHATIDYLINOSITOLS; PHOSPHOLIPASE C; RECEPTOR, SEROTONIN, 5-HT2C; RECEPTORS, SEROTONIN; SEROTONIN; SEROTONIN ANTAGONISTS;

EID: 0033984746     PISSN: 00281298     EISSN: None     Source Type: Journal    
DOI: 10.1007/s002109900178     Document Type: Article

References (10)

1. Berg KA, Maayani S, Goldfarb J, Scaramellini C, Leff P, Clarke WP (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
2. 2C receptor systems. Mol Pharmacol 55:863-872
3. Berridge MJ (1993) Inositol triphosphate and calcium signalling. Nature 361:315-325
4. 2C receptors. Br J Pharmacol 115:622-628
5. Burns CM, Chu H, Rueter SM, Hutchinson LK, Canton H, Sanders-Bush E, Emerson RB (1997) Regulation of serotonin-2C receptor G-protein coupling by RNA editing. Nature 387:303-308
6. 2A receptor-mediated phosphoinositide (PI) turnover by clozapine in the rat: a comparison to other antipsychotics. Neurosci Lett 181:65-68
7. 2C receptor agonist, RO 60-0175: a pharmacological analysis. Neuropharmacology 38: 415-423
8. Dickenson JM, Hill SJ (1996) Synergistic interactions between human transfected adenosine A1 receptors and endogenous cholecystokinin receptors in CHO cells. Eur J Pharmacol 302:141-151
9. Gerhardt CC, Heerikhuizen H (1997) Functional characteristics of heterologously expressed 5-HT receptors. Eur J Pharmacol 334: 1-23
10. Kennett GA, Wood MD, Bright F, Trail B, Riley G, Holland V, Avenell KY, Stean T, Upton N, Bromidge S, Forbes IT, Brown AM, Middlemiss DN, Blackburn TP (1997) SB242,084, a selective and brain penetrant 5-HT2C receptor antagonist. Neuropharmacology 36:609-620