RADIOLIGAND BINDING-STUDIES REVEAL MARKED SPECIES-DIFFERENCES IN THE VASOPRESSIN-V(1) RECEPTOR OF RAT, RHESUS AND HUMAN TISSUES

被引：72

作者：

PETTIBONE, DJ ^{[1
]}

KISHEL, MT ^{[1
]}

WOYDEN, CJ ^{[1
]}

CLINESCHMIDT, BV ^{[1
]}

BOCK, MG ^{[1
]}

FREIDINGER, RM ^{[1
]}

VEBER, DF ^{[1
]}

WILLIAMS, PD ^{[1
]}

机构：

[1] MERCK SHARP & DOHME LTD,DEPT MED CHEM,W POINT,PA 19486

来源：

LIFE SCIENCES | 1992年 / 50卷 / 25期

关键词：

D O I：

10.1016/0024-3205(92)90524-S

中图分类号：

R-3 [医学研究方法]; R3 [基础医学];

学科分类号：

1001 ;

摘要：

The [H-3]arginine-vasopressin ([H-3]AVP) binding site in rat, rhesus and human liver and nonpregnant human uterus was characterized and contrasted. [H-3]AVP bound with high affinity (K(i) values, 0.2-0.6 nM) to preparations of all tissues studied. Competition binding studies using a series of compounds from three structural classes indicate a marked species difference between the rat and primate liver AVP-V1 site. This site in rhesus and human liver however, is essentially identical, indicating that the rhesus liver is an appropriate surrogate for human tissue. These studies also indicate that the AVP-V1 site of nonpregnant human uterus and human liver is equivalent.

引用

页码：1953 / 1958

页数：6

共 24 条

[1] INHIBITION OF UTERINE CONTRACTIONS OF PREMATURE LABOR WITH AN OXYTOCIN ANALOG - RESULTS FROM A PILOT-STUDY [J].

AKERLUND, M ;

STROMBERG, P ;

HAUKSSON, A ;

ANDERSEN, LF ;

LYNDRUP, J ;

TROJNAR, J ;

MELIN, P .

BRITISH JOURNAL OF OBSTETRICS AND GYNAECOLOGY, 1987, 94 (11) :1040-1044

[2] VASOTOCIN ANALOGS WHICH COMPETITIVELY INHIBIT VASOPRESSIN STIMULATED UTERINE ACTIVITY IN HEALTHY WOMEN [J].

AKERLUND, M ;

HAUKSSON, A ;

LUNDIN, S ;

MELIN, P ;

TROJNAR, J .

BRITISH JOURNAL OF OBSTETRICS AND GYNAECOLOGY, 1986, 93 (01) :22-27

[3] RECEPTOR LIGANDS WHICH BIND THE OXYTOCIN RECEPTOR WITH SELECTIVITY AND HIGH-AFFINITY - CHEMICAL MODIFICATION OF A STREPTOMYCES-SILVENSIS DERIVED CYCLIC HEXAPEPTIDE [J].

BOCK, MG ;

DIPARDO, RM ;

WILLIAMS, PD ;

PETTIBONE, DJ ;

CLINESCHMIDT, BV ;

BALL, RG ;

VEBER, DF ;

FREIDINGER, RM .

JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (09) :2321-2323

[4]

CHAN WY, 1986, J PHARMACOL EXP THER, V239, P84

[5]

CHENG Y, 1973, BIOCHEM PHARMACOL, V22, P3099

[6]

CLINESCHMIDT BV, 1991, J PHARMACOL EXP THER, V256, P827

[7]

Embrey M P, 1967, J Obstet Gynaecol Br Commonw, V74, P648

[8] CYCLIC HEXAPEPTIDE OXYTOCIN ANTAGONISTS - POTENCY-ENHANCING, SELECTIVITY-ENHANCING, AND SOLUBILITY-ENHANCING MODIFICATIONS [J].

FREIDINGER, RM ;

WILLIAMS, PD ;

TUNG, RD ;

BOCK, MG ;

PETTIBONE, DJ ;

CLINESCHMIDT, BV ;

DIPARDO, RM ;

ERB, JM ;

GARSKY, VM ;

GOULD, NP ;

KAUFMAN, MJ ;

LUNDELL, GF ;

PERLOW, DS ;

WHITTER, WL ;

VEBER, DF .

JOURNAL OF MEDICINAL CHEMISTRY, 1990, 33 (07) :1843-1845

[9] OXYTOCIN AND VASOPRESSIN - DISTINCT RECEPTORS IN MYOMETRIUM [J].

GUILLON, G ;

BALESTRE, MN ;

ROBERTS, JM ;

BOTTARI, SP .

JOURNAL OF CLINICAL ENDOCRINOLOGY & METABOLISM, 1987, 64 (06) :1129-1135

[10] CHARACTERIZATION OF THE HUMAN LIVER VASOPRESSIN RECEPTOR - PROFOUND DIFFERENCES BETWEEN HUMAN AND RAT VASOPRESSIN-RECEPTOR-MEDIATED RESPONSES SUGGEST ONLY A MINOR ROLE FOR VASOPRESSIN IN REGULATING HUMAN HEPATIC-FUNCTION [J].

HOWL, J ;

ISMAIL, T ;

STRAIN, AJ ;

KIRK, CJ ;

ANDERSON, D ;

WHEATLEY, M .

BIOCHEMICAL JOURNAL, 1991, 276 :189-195

← 1 2 3 →