Endothelins and their inhibition in the human skin microcirculation: ET[1-31], a new vasoconstrictor peptide.

摘要: Aims  Endothelin-1 (ET-1[1−21]) is an extremely potent vasoconstrictor in the human skin microcirculation and generated from larger precursor peptides. The aims of present study were to assess vasoactive effects these precursors as well endothelin blockade microcirculation, vivo. Methods  Six healthy volunteers received intradermal injections a range doses big ET-1[1−38], ET-1[1−31], ET-1[1−21], BQ-123 (ETA receptor antagonist), BQ-788 (ETB phosphoramidon [endothelin converting enzyme (ECE) inhibitor] or saline control (0.9%). Skin blood flow (SBF) was measured using standard laser Doppler flowmetry. Results  Big ET-1[1−31] ET-1[1−21] reduced SBF when compared with (P < 0.01 for all). ET-1[1−38] less than defined by vasoconstriction. Phosphoramidon, BQ-788, given alone, all caused vasodilatation all). Conclusions  In are vasoconstrictors ET-1[1−21]. suggest presence endogenous ECE activity skin. contrast skeletal muscle resistance vessels, contributes maintenance microvascular tone through both ETA ETB receptor-mediated