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Titolo:
THE SEROTONIN 5-HT2C RECEPTOR IS A PROMINENT SEROTONIN RECEPTOR IN BASAL GANGLIA - EVIDENCE FROM FUNCTIONAL-STUDIES ON SEROTONIN-MEDIATED PHOSPHOINOSITIDE HYDROLYSIS
Autore:
WOLF WA; SCHUTZ LJ;
Indirizzi:
EDWARD HINES VET ADM MED CTR,RES SERV HINES IL 60141 EDWARD HINES VET ADM MED CTR,BIOL PSYCHIAT & RES SERV HINES IL 60141 LOYOLA UNIV,STRITCH SCH MED,DEPT PHARMACOL & EXPT THERAPEUT MAYWOOD IL 60153
Titolo Testata:
Journal of neurochemistry
fascicolo: 4, volume: 69, anno: 1997,
pagine: 1449 - 1458
SICI:
0022-3042(1997)69:4<1449:TS5RIA>2.0.ZU;2-9
Fonte:
ISI
Lingua:
ENG
Soggetto:
NEONATAL 6-OHDA-LESIONED RATS; PHARMACOLOGICAL CHARACTERIZATION; BRAIN MEMBRANES; ANTIPSYCHOTIC-DRUGS; RECOGNITION SITES; ARACHIDONIC-ACID; PHOSPHOLIPASE-C; H-3 MESULERGINE; HIGH-AFFINITY; ANTAGONIST;
Keywords:
SEROTONIN RECEPTOR; PHOSPHOLIPASE C; PHOSPHOINOSITIDE HYDROLYSIS; BRAIN; RAT;
Tipo documento:
Article
Natura:
Periodico
Settore Disciplinare:
Science Citation Index Expanded
Science Citation Index Expanded
Citazioni:
54
Recensione:
Indirizzi per estratti:
Citazione:
W.A. Wolf e L.J. Schutz, "THE SEROTONIN 5-HT2C RECEPTOR IS A PROMINENT SEROTONIN RECEPTOR IN BASAL GANGLIA - EVIDENCE FROM FUNCTIONAL-STUDIES ON SEROTONIN-MEDIATED PHOSPHOINOSITIDE HYDROLYSIS", Journal of neurochemistry, 69(4), 1997, pp. 1449-1458

Abstract

Serotonin (5-hydroxytryptamine; 5-HT) 5-HT2A and 5-HT2C receptors belong to the class of phosphoinositide-specific phospholipase C (PLC)-linked receptors. Conditions were established for measuring 5-HT2A-linked and 5-HT2C-linked PLC activity in membranes prepared from previouslyfrozen rat frontal cortex and caudate. In the presence of Ca2+ (300 nM) and GTP gamma S (1 mu M), 5-HT increased PLG activity in caudate membranes. Pharmacological analysis using the selective 5-HT2A antagonist, spiperone, and the nonselective 5-HT2A/2C antagonist, mianserin, demonstrated that over half of the 5-HT-stimulated PLC activity was due to stimulation of 5-HT2C receptors as opposed to 5-HT2A receptors. Radioligand binding assays with [H-3]RP 62203 and [H-3]-mesulergine were used to quantify 5-HT2A and 5-HT2C sites, respectively, in caudate. From these data, the B-max for caudate 5-HT2A sites and 5-HT2C sites was165.4 +/- 9.7 fmol/mg of protein and 49.7 +/- 3.3 fmol/mg of protein,respectively. In contrast to that in caudate, PLC activity in frontalcortex was stimulated by 5-HT in a manner that was inhibited by the 5-HT2A-selective antagonists, spiperone and ketanserin. Taken together,the results indicate that 5-HT2A- and 5-HT2C-linked PLC activity can be discerned in brain regions possessing both receptor subtypes using membranes prepared from previously frozen tissue. More importantly, significant 5-HT2C-mediated phosphoinositide hydrolysis was observed in caudate, despite the relatively low density of 5-HT2C sites. The significance of these observations with respect to the physiological function of 5-HT2C receptors is discussed.

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Documento generato il 06/07/20 alle ore 08:36:26