NEW ANTAGONISTS OF THE VASOPRESSIN RECEPTOR MEDIATED CONTRACTION IN RAT TAIL ARTERY

被引：1
|
作者：
PETRUSEWICZ, J [1 ]
DAMASIEWICZ, B [1 ]
KALISZAN, R [1 ]
JUZWA, W [1 ]
LAMMEK, B [1 ]
DERDOWSKA, I [1 ]
机构：
[1] UNIV GDANSK, INST CHEM, PL-80952 GDANSK, POLAND
来源：
PHARMACOLOGICAL RESEARCH | 1992年 / 25卷 / 02期
关键词：
RAT TAIL ARTERY; VASOPRESSIN ANTAGONISTS; V1-RECEPTOR; VASOPRESSOR/OXYTOCINERGIC SELECTIVITY;
D O I：
10.1016/1043-6618(92)91384-S
中图分类号：
R9 [药学];
学科分类号：
1007 ;
摘要：
A perfused isolated rat tail artery preparation was employed to study antagonistic properties of four newly synthesized arginine-vasopressin (AVP) analogues against the V1 receptor. The activity of the agents SCATyr(Me)AVP, OCATyr(Me)AVP, OCAAVP and SCAAVP was related to that of a recognized antagonist d(CH2)5Tyr(Me)AVP. SCATyr(Me)AVP elicited outstanding antagonistic properties by blocking at concentration of 10-7m nearly completely the constrictory activity of AVP. At concentration of 10-9m the agent inhibited the AVP-induced constriction of artery about 40 times more effectively than the oxytocin (OXT)-induced constriction. The results obtained prove the validity of the structure-activity relationship based search for new potent V1 receptor antagonists. © 1992.
引用
收藏
页码：167 / 172
页数：6
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