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- W2038831738 abstract "We have previously shown that endothelin-B (ETB) receptors mediate contraction in human and rat pulmonary resistance arteries (PRAs). Here we characterize the endothelin(ET) receptors in rabbits PRAs. PRAs (∼150 μm i.d.) were studied using wire myography. Vasoconstrictor effects to ET-1, ET-3, and the ETB-selective agonist sarafotoxin S6c (S6c) were studied in the presence and absence of the ETA receptor antagonist FR139317, the ETB-selective antagonist BQ788, and the mixed ETA/ETB antagonist SB209670. The effect of SB209670 was also studied in human PRAs (∼250 μm i.d.). Competitive ET-1 binding studies were also carried out on rabbit small pulmonary artery homogenates. The potencies of the agonists were in the following order: S6c>ET-3=ET-1. Concentration-response curves(CRCs) to ET-1 were biphasic, with a gradual slope up to ∼1 nM and a steeper component at higher concentrations of ET-1. Neither FR139317 (1 μM) nor BQ788 (1 μM) inhibited responses to ET-1. BQ788 inhibited S6c- and ET-3 induced contractions with pKb values of 6.8 ± 0.1 and 6.3 ± 0.2, respectively. SB209670 inhibited responses to ET-1 in the higher concentration component of the CRC and inhibited responses to S6c in a competitive fashion. pKb values for ET-1 and S6c were 6.8 ± 0.2 and 7.5 ± 1, respectively. SB209670 (0.1-1 μM) totally abolished responses to ET-1 in human PRAs. The binding assay established two ET binding sites in rabbit PRAs, one low affinity (Ki = 480 pM) and one high affinity (Ki = 64 fM). The study provides evidence for a heterogeneous population of ETB-like receptors in pulmonary resistance arteries, including an atypical ETB receptor sensitive to SB209670." @default.
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- W2038831738 date "1998-01-01" @default.
- W2038831738 modified "2023-09-23" @default.
- W2038831738 title "Heterogeneity of Endothelin-B Receptors in Rabbit Pulmonary Resistance Arteries" @default.
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- W2038831738 doi "https://doi.org/10.1097/00005344-199800001-00035" @default.
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