title: Gestational changes in endothelin-1-induced receptors and myometrial contractions in rat.
abstract: The present experiments were performed to characterize the gestational changes in endothelin (ET)-1-induced myometrial contractions and ET receptors in rat. ET-1-induced contractions were composed of two types: increases in resting tone and rhythmic contractions. The increase in resting tone was decreased at 7 days of gestation, but increased at 20 days. The increase in amplitude and frequency of rhythmic contractions remained unchanged during days 7-14 of gestation. Continuous rhythmic contractions were not produced by ET-1 near the term. Both contractions were inhibited by the antagonists BQ 123 and Ro 46-2005 but not by RES 701-1 or BQ 788. In binding studies, total binding sites of [1251]-ET-1 were unchanged, however higher affinity binding sites appeared during pregnancy in addition to the lower affinity sites. The specific [125I]-ET-1 binding in non-pregnant and pregnant myometrium was completely inhibited by unlabelled ET-1 and Ro 46-2005. In contrast, the proportion which was inhibited by BQ 123 was decreased during pregnancy. In conclusion, characteristic gestational changes were the augmentation of ET-1-induced increased resting tone near term, and the appearance of high affinity ET-1 binding sites and an increase in BQ 123-resistant ET-1 binding sites during pregnancy. Further investigations are needed to understand the physiological role of these changes.
authors.affiliation: Department of Obstetrics and Gynecology, Faculty of Medicine, Tokyo Medical and Dental University, Japan.
authors.forename: S
authors.initials: S
authors.lastname: Sakamoto
authors.forename: T
authors.initials: T
authors.lastname: Aso
authors.forename: H
authors.initials: H
authors.lastname: Masuda
authors.forename: M
authors.initials: M
authors.lastname: Goto
authors.forename: S
authors.initials: S
authors.lastname: Tamaoki
authors.forename: H
authors.initials: H
authors.lastname: Azuma
mesh_terms: D000818:Animals; D019332:Endothelin-1 / Q000378:metabolism* / Q000494:pharmacology; D005260:Female; D007457:Iodine Radioisotopes; D019563:Mechanics; D009215:Myometrium / Q000378:metabolism*; D011247:Pregnancy; D011270:Pregnancy, Animal / Q000378:metabolism*; D051381:Rats; D017207:Rats, Sprague-Dawley; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin / Q000378:metabolism*; D014590:Uterine Contraction / Q000187:drug effects / Q000502:physiology*
chemical_list: D019332:Endothelin-1; D007457:Iodine Radioisotopes; D044022:Receptor, Endothelin A; D017466:Receptors, Endothelin