title: Endopeptidase 24.11 inhibition does not modify uterotonic effects of endothelins in rat uterus.
abstract: We investigated effects of the endopeptidase 24.11 inhibitor, SCH 39370, on uterotonic effects of endothelins (ETs) and sarafotoxin S6b. Responses of uteri from non-pregnant rats were inhibited by the ETA receptor antagonist, BQ123 (1 microM) but not the ETB receptor antagonist, BQ 788 (1 microM). ET-1, sarafotoxin S6b and ET-2 were more potent than ET-3 in tissues from non-pregnant and pregnant rats. SCH 39370 (10 microM) did not affect uterotonic responses to these peptides in either group, but inhibited those of big ET-1 in non-pregnant rat tissues, indicating inhibition of conversion of big ET-1 to ET-1. These data indicate that endopeptidase 24.11 does not inactivate the endothelin peptides in the rat uterus.
authors.affiliation: Department of Pharmacology, Monash University, Clayton, Victoria, Australia.
authors.forename: M
authors.initials: M
authors.lastname: Kousides
authors.forename: M E
authors.initials: ME
authors.lastname: Story
authors.forename: J N
authors.initials: JN
authors.lastname: Pennefather
mesh_terms: D000818:Animals; D004151:Dipeptides / Q000494:pharmacology*; D065128:Endothelin Receptor Antagonists; D019332:Endothelin-1 / Q000494:pharmacology; D019333:Endothelin-2 / Q000494:pharmacology; D019334:Endothelin-3 / Q000494:pharmacology; D016232:Endothelins / Q000494:pharmacology*; D004967:Estrogens / Q000494:pharmacology; D005260:Female; D066298:In Vitro Techniques; D009129:Muscle Tonus / Q000187:drug effects*; D015260:Neprilysin / Q000037:antagonists & inhibitors*; D009842:Oligopeptides / Q000494:pharmacology; D010456:Peptides, Cyclic / Q000494:pharmacology; D010880:Piperidines / Q000494:pharmacology; D011247:Pregnancy; D011480:Protease Inhibitors / Q000494:pharmacology; D051381:Rats; D017207:Rats, Sprague-Dawley; D017466:Receptors, Endothelin / Q000819:agonists; D014599:Uterus / Q000187:drug effects*; D014757:Viper Venoms / Q000494:pharmacology
chemical_list: D004151:Dipeptides; D065128:Endothelin Receptor Antagonists; D019332:Endothelin-1; D019333:Endothelin-2; D019334:Endothelin-3; D016232:Endothelins; D004967:Estrogens; D009842:Oligopeptides; D010456:Peptides, Cyclic; D010880:Piperidines; D011480:Protease Inhibitors; D017466:Receptors, Endothelin; D014757:Viper Venoms; C057354:sarafotoxins s6; C060631:Sch 39370; C086539:BQ 788; D015260:Neprilysin; C072247:cyclo(Trp-Asp-Pro-Val-Leu)