Constriction to ETB receptor agonists, BQ-3020 and sarafotoxin S6c, in human resistance and capacitance vessels in vivo

被引:10
作者
Strachan, FE [1 ]
Crockett, TR
Mills, NL
Gray, GA
Webb, DJ
机构
[1] Univ Edinburgh, Western Gen Hosp, Dept Med Sci, Clin Pharmacol Unit, Edinburgh EH4 2XU, Midlothian, Scotland
[2] Univ Edinburgh, Western Gen Hosp, Dept Med Sci, Res Ctr, Edinburgh EH4 2XU, Midlothian, Scotland
[3] Univ Edinburgh, Dept Biomed Sci, Edinburgh EH8 9J2, Midlothian, Scotland
关键词
endothelin-1; ETB receptor agonist; vasoconstriction;
D O I
10.1046/j.1365-2125.2000.00213.x
中图分类号
R9 [药学];
学科分类号
1007 ;
摘要
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.
引用
收藏
页码:27 / 30
页数:4
相关论文
共 20 条
[1]   A NEW TECHNIQUE FOR RECORDING COMPLIANCE OF HUMAN HAND VEINS [J].
AELLIG, WH .
BRITISH JOURNAL OF CLINICAL PHARMACOLOGY, 1981, 11 (03) :237-243
[2]   CLONING AND EXPRESSION OF A CDNA-ENCODING AN ENDOTHELIN RECEPTOR [J].
ARAI, H ;
HORI, S ;
ARAMORI, I ;
OHKUBO, H ;
NAKANISHI, S .
NATURE, 1990, 348 (6303) :730-732
[3]   ENDOTHELIN IS A POTENT LONG-LASTING VASOCONSTRICTOR IN MEN [J].
CLARKE, JG ;
BENJAMIN, N ;
LARKIN, SW ;
WEBB, DJ ;
DAVIES, GJ ;
MASERI, A .
AMERICAN JOURNAL OF PHYSIOLOGY, 1989, 257 (06) :H2033-H2035
[4]   THE ENDOTHELIN ET(B) RECEPTOR MEDIATES BOTH VASODILATION AND VASOCONSTRICTION INVIVO [J].
CLOZEL, M ;
GRAY, GA ;
BREU, V ;
LOFFLER, BM ;
OSTERWALDER, R .
BIOCHEMICAL AND BIOPHYSICAL RESEARCH COMMUNICATIONS, 1992, 186 (02) :867-873
[5]  
DAVENPORT AP, 1993, J CARDIOVASC PHAR S8, V22, P22
[6]   ETB receptor and nitric oxide synthase blockade induce BQ-123-sensitive pressor effects in the rabbit [J].
Gratton, JP ;
Cournoyer, G ;
Loffler, BM ;
Sirois, P ;
DOrleansJuste, P .
HYPERTENSION, 1997, 30 (05) :1204-1209
[7]   ENDOTHELIN ET(A) AND ET(B) AND RECEPTORS CAUSE VASOCONSTRICTION OF HUMAN RESISTANCE AND CAPACITANCE VESSELS IN-VIVO [J].
HAYNES, WG ;
STRACHAN, FE ;
WEBB, DJ .
CIRCULATION, 1995, 92 (03) :357-363
[8]  
IHARA M, 1992, LIFE SCI, V51, P47
[9]   BIOCHEMICAL AND PHARMACOLOGICAL PROFILE OF A POTENT AND SELECTIVE ENDOTHELIN B-RECEPTOR ANTAGONIST, BQ-788 [J].
ISHIKAWA, K ;
IHARA, M ;
NOGUCHI, K ;
MASE, T ;
MINO, N ;
SAEKI, T ;
FUKURODA, T ;
FUKAMI, T ;
OZAKI, S ;
NAGASE, T ;
NISHIKIBE, M ;
YANO, M .
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA, 1994, 91 (11) :4892-4896
[10]   Vasodilator effects of endothelin-converting enzyme inhibition and endothelin ET(A) receptor blockade in chronic heart failure patients treated with ACE inhibitors [J].
Love, MP ;
Haynes, WG ;
Gray, GA ;
Webb, DJ ;
McMurray, JJV .
CIRCULATION, 1996, 94 (09) :2131-2137