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.
MeSH terms
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Animals
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Dipeptides / pharmacology*
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Endothelin Receptor Antagonists
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Endothelin-1 / pharmacology
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Endothelin-2 / pharmacology
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Endothelin-3 / pharmacology
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Endothelins / pharmacology*
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Estrogens / pharmacology
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Female
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In Vitro Techniques
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Muscle Tonus / drug effects*
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Neprilysin / antagonists & inhibitors*
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Oligopeptides / pharmacology
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Peptides, Cyclic / pharmacology
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Piperidines / pharmacology
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Pregnancy
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Protease Inhibitors / pharmacology
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Rats
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Rats, Sprague-Dawley
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Receptors, Endothelin / agonists
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Uterus / drug effects*
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Viper Venoms / pharmacology
Substances
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Dipeptides
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Endothelin Receptor Antagonists
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Endothelin-1
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Endothelin-2
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Endothelin-3
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Endothelins
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Estrogens
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Oligopeptides
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Peptides, Cyclic
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Piperidines
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Protease Inhibitors
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Receptors, Endothelin
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Viper Venoms
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sarafotoxins s6
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Sch 39370
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BQ 788
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Neprilysin
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cyclo(Trp-Asp-Pro-Val-Leu)