Premium
Differential effects of BQ‐123 against endothelin‐1 and endothelin‐3 on the rat vas deferens: evidence for an atypical endothelin receptor
Author(s) -
Eglezos Anthony,
Cucchi Paola,
Patacchini Riccardo,
Quartara Laura,
Maggi Carlo Alberto,
Mizrahi Jacques
Publication year - 1993
Publication title -
british journal of pharmacology
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 2.432
H-Index - 211
eISSN - 1476-5381
pISSN - 0007-1188
DOI - 10.1111/j.1476-5381.1993.tb13635.x
Subject(s) - endothelin receptor , vas deferens , endocrinology , medicine , endothelin 1 , endothelin receptor antagonist , endothelin 3 , antagonist , receptor , endothelins , stimulation , receptor antagonist , chemistry
1 Endothelin‐1 and endothelin‐3 enhanced concentration‐dependently the rat vas deferens twitch response to electrical stimulation, endothelin‐1 being three times more potent. Sarafotoxin S6c was at least 200 times less active than endothelin‐1. 2 The response to endothelin was antagonized in a competitive manner by the supposedly selective ET A receptor antagonist, BQ‐123 (pA 2 :7.0 ± 0.1). In contrast, the endothelin‐1 concentration‐response curve was only shifted two fold in the presence of 10 μ m BQ‐123, while no effect was observed at 1 μ m . 3 This evidence suggests the rat vas deferens contains an endothelin receptor not conforming to the ET A /ET B receptor subtype classification so far proposed.