Characterization of a rat kidney thromboxane A(2) receptor: High affinity for the agonist ligand I-BOP

被引：12

作者：

DAngelo, DD ^{[1
]}

Terasawa, T ^{[1
]}

Carlisle, SJ ^{[1
]}

Dorn, GW ^{[1
]}

Lynch, KR ^{[1
]}

机构：

[1] UNIV VIRGINIA,DEPT PHARMACOL,CHARLOTTESVILLE,VA 22903

来源：

PROSTAGLANDINS | 1996年 / 52卷 / 04期

关键词：

thromboxane A2 receptor; radioligand binding; I-BOP; molecular cloning; oocyte expression (Xenopus laevis); HEK293; cells;

D O I：

10.1016/S0090-6980(96)00091-3

中图分类号：

Q5 [生物化学]; Q7 [分子生物学];

学科分类号：

071010 ; 081704 ;

摘要：

We have cloned a rat kidney thromboxane A(2) receptor (TP) cDNA. This receptor was shown to be functional in that the thromboxane A(2) mimetics, U46619 and I-BOP, elicited calcium transients in Xenopus oocytes and HEK293 cells expressing the TP receptor, respectively. Comparison of the affinities of the rat and human TP sites for the agonist radioligand [I-125]BOP showed that the rat TP site has about a ten-fold higher affinity for this drug (K-D approximate to 0.5 vs. 4.4 nM) while the affinities of the two sites for other compounds (U46619, I-PTH-OH) were the same. Our results are significant in that they identify a cloned TP as having a picomolar affinity for [I-125]BOP.

引用

页码：303 / 316

页数：14

共 26 条

[1] RAT KIDNEY THROMBOXANE RECEPTOR - MOLECULAR-CLONING, SIGNAL-TRANSDUCTION, AND INTRARENAL EXPRESSION LOCALIZATION [J].

ABE, T ;

TAKEUCHI, K ;

TAKAHASHI, N ;

TSUTSUMI, E ;

TANIYAMA, Y ;

ABE, K .

JOURNAL OF CLINICAL INVESTIGATION, 1995, 96 (02) :657-664

[2] MOLECULAR-CLONING OF RAT RENIN CDNA AND ITS GENE [J].

BURNHAM, CE ;

HAWELUJOHNSON, CL ;

FRANK, BM ;

LYNCH, KR .

PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1987, 84 (16) :5605-5609

[3]

DANGELO DD, 1994, J PHARMACOL EXP THER, V271, P1034

[4]

DORN GW, 1992, J BIOL CHEM, V267, P24897

[5] TISSUE-SPECIFIC AND SPECIES-SPECIFIC DIFFERENCES IN LIGAND-BINDING TO THROMBOXANE-A2 RECEPTORS [J].

DORN, GW .

AMERICAN JOURNAL OF PHYSIOLOGY, 1991, 261 (01) :R145-R153

[6] DISTINCT PLATELET THROMBOXANE-A2 PROSTAGLANDIN-H2 RECEPTOR SUBTYPES - A RADIOLIGAND BINDING STUDY OF HUMAN-PLATELETS [J].

DORN, GW .

JOURNAL OF CLINICAL INVESTIGATION, 1989, 84 (06) :1883-1891

[7] HUMAN PLATELET-AGGREGATION AND SHAPE CHANGE ARE COUPLED TO SEPARATE THROMBOXANE-A2-PROSTAGLANDIN-H2 RECEPTORS [J].

DORN, GW ;

DEJESUS, A .

AMERICAN JOURNAL OF PHYSIOLOGY, 1991, 260 (02) :H327-H334

[8]

DORN GW, 1991, J PHARMACOL EXP THER, V259, P228

[9] LYSOPHOSPHATIDIC ACID INDUCES A PERTUSSIS TOXIN-SENSITIVE CA2+-ACTIVATED CL- CURRENT IN XENOPUS-LAEVIS OOCYTES [J].

DURIEUX, ME ;

SALAFRANCA, MN ;

LYNCH, KR ;

MOORMAN, JR .

AMERICAN JOURNAL OF PHYSIOLOGY, 1992, 263 (04) :C896-C900

[10] LYSOPHOSPHATIDIC ACID INDUCES INWARD CURRENTS IN XENOPUS-LAEVIS OOCYTES - EVIDENCE FOR AN EXTRACELLULAR SITE OF ACTION [J].

FERNHOUT, BJH ;

DIJCKS, FA ;

MOOLENAAR, WH ;

RUIGT, GSF .

EUROPEAN JOURNAL OF PHARMACOLOGY, 1992, 213 (02) :313-315

← 1 2 3 →