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

被引：275

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
BOUHELAL, R
SMOUNYA, L
BOCKAERT, J
[J]. EUROPEAN JOURNAL OF PHARMACOLOGY, 1988, 151 (02) : 189 - 196
[3] BRADFORD MM, 1976, ANAL BIOCHEM, V72, P248, DOI 10.1016/0003-2697(76)90527-3
[4] PROPOSALS FOR THE CLASSIFICATION AND NOMENCLATURE OF FUNCTIONAL RECEPTORS FOR 5-HYDROXYTRYPTAMINE
BRADLEY, PB
ENGEL, G
FENIUK, W
FOZARD, JR
HUMPHREY, PPA
MIDDLEMISS, DN
MYLECHARANE, EJ
RICHARDSON, BP
SAXENA, PR
[J]. NEUROPHARMACOLOGY, 1986, 25 (06) : 563 - 576
[5] BRANCHEK T, 1991, SEROTONIN : MOLECULAR BIOLOGY, RECEPTORS AND FUNCTIONAL EFFECTS, P21
[6] CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099
[7] A HUMAN SEROTONIN 1D RECEPTOR VARIANT (5HT1D-BETA) ENCODED BY AN INTRONLESS GENE ON CHROMOSOME-6
DEMCHYSHYN, L
SUNAHARA, RK
MILLER, K
TEITLER, M
HOFFMAN, BJ
KENNEDY, JL
SEEMAN, P
VANTOL, HHM
NIZNIK, HB
[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1992, 89 (12) : 5522 - 5526
[8] DEVIVO M, 1986, J PHARMACOL EXP THER, V238, P248
[9] THE GENOMIC CLONE G-21 WHICH RESEMBLES A BETA-ADRENERGIC-RECEPTOR SEQUENCE ENCODES THE 5-HT1A RECEPTOR
FARGIN, A
RAYMOND, JR
LOHSE, MJ
KOBILKA, BK
CARON, MG
LEFKOWITZ, RJ
[J]. NATURE, 1988, 335 (6188) : 358 - 360
[10] A TECHNIQUE FOR RADIOLABELING DNA RESTRICTION ENDONUCLEASE FRAGMENTS TO HIGH SPECIFIC ACTIVITY
FEINBERG, AP
VOGELSTEIN, B
[J]. ANALYTICAL BIOCHEMISTRY, 1983, 132 (01) : 6 - 13

← 1 2 3 4 →