CLONING OF ANOTHER HUMAN SEROTONIN RECEPTOR (5-HT1F) - A 5TH 5-HT1 RECEPTOR SUBTYPE COUPLED TO THE INHIBITION OF ADENYLATE-CYCLASE

被引：276

作者：

ADHAM, N ^{[1
]}

KAO, HT ^{[1
]}

SCHECHTER, LE ^{[1
]}

BARD, J ^{[1
]}

OLSEN, M ^{[1
]}

URQUHART, D ^{[1
]}

DURKIN, M ^{[1
]}

HARTIG, PR ^{[1
]}

WEINSHANK, RL ^{[1
]}

BRANCHEK, TA ^{[1
]}

机构：

[1] SYNAPT PHARMACEUT CORP,215 COLL RD,PARAMUS,NJ 07652

来源：

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA | 1993年 / 90卷 / 02期

关键词：

D O I：

10.1073/pnas.90.2.408

中图分类号：

O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];

学科分类号：

07 ; 0710 ; 09 ;

摘要：

An intronless gene encoding an additional human serotonin (5-HT) 5-HT1-like receptor subtype was isolated from a human genomic library with probes obtained from degenerate PCR primers used to amplify 5-HT-receptor-specific sequences. The highest degree of homology was found with the 5-HT1E subtype (70%) and the 5-HT1Dalpha (63%) and 5-HT1Dbeta (60%) receptors. RNA for this gene was detected in the human brain but was not detected in kidney, liver, spleen, heart, pancreas, and testes. High-affinity (K(d) = 9.2 nM) H-3-labeled 5-HT binding was detected. Competition studies revealed the following rank order of potencies for serotonergic ligands: 5-HT > sumatriptan >> 5-carboxyamidotryptamine > 8-hydroxy-2(di-1-propylamino)tetralin > spiperone. 5-HT produced a dose-dependent inhibition of forskolin-stimulated cAMP accumulation (EC50 = 7.9 nM) in transfected cells. These properties distinguish this receptor from any previously characterized and establish a fifth 5-HT1-like receptor subtype (5-HT1F) coupled to the inhibition of adenylate cyclase.

引用

页码：408 / 412

页数：5

共 32 条

[1]

ADHAM N, 1992, MOL PHARMACOL, V41, P1

[2] 5-HT1B RECEPTORS ARE NEGATIVELY COUPLED WITH ADENYLATE-CYCLASE IN RAT SUBSTANTIA NIGRA [J].