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
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
收藏
页码:1953 / 1958
页数:6
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