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РЖ ВИНИТИ 34 (BI48) 95.11-04Т1.293

Grotewiel, Michael S.
m-Chlorophenylpiperazine and m-trifluoromethylphenylpiperazine are partial agonists at cloned 5-HT[2A] receptors expressed in fibroblasts [Text] / Michael S. Grotewiel, Hsin Chu, Elaine Sanders-Bush // J. Pharmacol. and Exp. Ther. - 1994. - Vol. 271, N 2. - P1122-1126 . - ISSN 0022-3565
Перевод заглавия: м-Хлорфенилпиперазин и м-трифторметилфенилпиперазин являются частичными агонистами клонированных 5-HT[2A]-рецепторов, экспрессированных в фибробласты
Аннотация: Serotonin[2A] (5-HT[2C]) receptors share numerous pharmacological properties. Two compounds thought to discriminate between these two receptor subtypes are m-chlorophenylpiperazine (mCPP) and m-trifluoromethylphenylpiperazine (TFMPP). These two drugs have been classified as antagonists at 5-HT[2A] receptors but as agonists at 5-HT[2C] receptors on the basis of phosphoinositide hydrolysis studies in cerebral cortex and choroid plexus, respectively. To determine more fully the properties of mCPP and TFMPP at 5-HT[2A] receptors, NIH 3T3 fibroblasts transfected with the 5-HT[2A] receptor complementary DNA (GF6 cells) were used as a model system of receptor function. These cells express approximately 15-fold higher 5-HT[2A] receptor density than is found in cerebral cortex. In GF6 cells, mCPP and TFMPP dose-dependently stimulated phosphoinositide hydrolysis with maximal effects less than that of 5-HT. This agonist activity was blocked by 5-HT[2A] receptor antagonists but not by prior treatment with pertussis toxin. Partial inactivation of 5-HT[2A] receptors with phenoxybenzamine decreased the maximal effects of mCPP and TFMPP but did not eliminate agonist activity. Thus mCPP and TFMPP are partial agonists at 5-HT[2A] receptors in GF6 cells, and these agonist properties are retained even under conditions where receptor density is comparable to that of cerebral cortex. Although it has not yet been demonstrated that mCPP and TFMPP are agonists at central 5-HT[2A] receptors, this possibility should be considered when evaluating in vivo effects of these drugs. США, Vanderbilt Univ. Sch. of Med., Nashville, TN 37232-6600. Библ. 25

ГРНТИ	34.45.21

ВИНИТИ 341.45.21.23.27
Рубрики: СЕРОТОНИНОВЫЕ РЕЦЕПТОРЫ
ПОДТИП 5-НТ 2А
ЧАСТИЧНЫЕ АГОНИСТЫ
ХЛОРФЕНИЛПИПЕРАЗИН * М-
ТРИФТОРМЕТИЛФЕНИЛПИПЕРАЗИН * М-
ЭКСПРЕССИЯ
ФИБРОБЛАСТЫ

Доп.точки доступа:
Chu, Hsin; Sanders-Bush, Elaine

"Электронные каталоги и базы данных библиотек СО РАН"

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