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Constriction to ETB Receptor Agonists, BQ-3020 and Sarafotoxin s6c, in Human Resistance and Capacitance Vessels in Vivo

Constriction to ETB Receptor Agonists, BQ-3020 and Sarafotoxin s6c, in Human Resistance and Capacitance Vessels in Vivo

F E Strachan, T R Crockett, N L Mills, G A Gray, D J Webb

Br J Clin Pharmacol. 2000 Jul;50(1):27-30.

PMID: 10886114

Abstract:

Aims:
The aim of the study was to examine the effects of the ETB receptor selective agonists sarafotoxin S6c (SFTX6c) and BQ-3020 on the forearm resistance and capacitance vessels in healthy subjects in vivo.
Methods:
The local response to intra-arterial or intravenous infusion of SFTX6c (5 pmol min-1) or BQ-3020 (50 pmol min-1) was assessed, on separate occasions, in eight healthy men (aged 20-28 years). Data (mean +/- s.e.mean) were examined by ANOVA. Results are expressed as percentage change from baseline at 90 min.
Results:
SFTX6c and BQ-3020 reduced forearm blood flow, following local intra-arterial infusion (-25 +/- 7% and -27 +/- 7%, respectively; P < 0.001) and reduced hand vein diameter, following local intravenous infusion (-30 +/- 8% and -16 +/- 7%, respectively; P < 0.001).
Conclusions:
We have shown that locally active infusions of the selective ETB receptor agonists SFTX6c and BQ-3020 cause arterial constriction and venoconstriction in healthy human blood vessels in vivo. These results indicate that ETB receptor stimulation may mediate vasoconstriction in humans.

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP143113455	BQ-3020		143113-45-5	Price

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