Binding of Four Oxytocin Analogues to Myometrial Oxytocin and Arginine-Vasopressin Binding Sites in Pregnant Women
作者:
G. Rydén,
R.G.G. Andersson,
G. Berg,
S.-G. Karlsson,
Y. Oscarsson,
期刊:
Gynecologic and Obstetric Investigation
(Karger Available online 1990)
卷期:
Volume 29,
issue 1
页码: 6-9
ISSN:0378-7346
年代: 1990
DOI:10.1159/000293289
出版商: S. Karger AG
关键词: Oxytocin;Vasopressin;Oxytocin analogues;Myometrium;Oxytocin receptor sites;Vasopressin receptor sites
数据来源: Karger
摘要:
The binding of 3H-oxytocin (3H-OT) and 3H-arginine-vasopressin (3H-AVP) and the displacement from binding sites by four oxytocin analogues were studied in myometrial membrane preparations from full-term pregnant women. Specific 3H-OT binding was saturable with a maximal binding capacity of 76.1 fmol/mg DNA, and a dissociation constant of 0.5 pM. Corresponding values regarding 3H-AVP was 148.6 fmol/mg DNA and 0.7 pM. The oxytocin analogues tested demonstrated a high specific binding to the OT and AVP receptor sites; in fact, the affinity of the analogues to the 3H-AVP binding sites was higher than to the 3H-OT binding sites. The order of potency between the analogues was CAU > CAM > CAP > CAO and CAP > CAU > CAO > CAM for the OT and AVP binding sites, respectively. The displacement of oxytocin and arginine-vasopressin, respectively, from the myometrial receptor sites indicate partly separate binding sites for oxytocin and AVP and might implicate that AVP can be of importance in regulating myometrial activity in pregnancy. The results on oxytocin analogues imply that other pharmacological tests must be performed for quantification of the relaxing effects on the uterus and to determine the optimal analogue for clinical trials in preterm labor and dysmenorrhoea.
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