1992年11月
EFFECTS OF THE NEW THROMBOXANE-A2 ANTAGONIST VAPIPROST ON ISOLATED CANINE BLOOD-VESSELS
ARZNEIMITTEL-FORSCHUNG/DRUG RESEARCH
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- 巻
- 42-2
- 号
- 11
- 開始ページ
- 1318
- 終了ページ
- 1322
- 記述言語
- 英語
- 掲載種別
- 出版者・発行元
- ECV-EDITIO CANTOR VERLAG MEDIZIN NATURWISSENSCHAFTEN
Effects of the new thromboxane A2 antagonist vapiprost (SN-309, GR-32191B, CAS 85505-64-2) on isolated canine blood vessels were investigated. U46619 ((15S)-hy-droxy-11alpha,9alpha-(epoxymethano)prosta-5Z, 13E-dienoic acid) 10(-10)-10(-6) mol/l, a thromboxane A2 analogue, produced concentration-dependent contractions of oblong or ring preparations isolated from basilar, coronary, mesenteric and femoral arteries. Vapiprost 10(-8) and 10(-7) mol/l significantly and concentration-dependently shifted the concentration-contraction curves for U46619 of these arteries to the right. The pA2 values were 8.80 +/- 0.09 in basilar arteries, 8.67 +/- 0.12 in coronary arteries, 8.86 +/- 0.05 in mesenteric arteries and 9.01 +/- 0.07 in femoral arteries. On the other hand, oblong or ring preparations of basilar, coronary, mesenteric and femoral arteries showed sustained contractile responses to KCl 3 X 10(-2) mol/l, U46619 10(-7) mol/l or prostaglandin (PG) F2alpha 10(-5) mol/l.
Norepinephrine (NE) 3 x 10(-5) mol/l also produced sustained contractions in mesenteric and femoral arterial preparations, but not in basilar and coronary arterial preparations. Vapiprost 10(-10)-3 X 10(-6) mol/l relaxed these four arterial preparations constricted with U46619 10(-7) mol/l and PGF2alpha 10(-5) mol/l in a concentration-dependent fashion, but hardly affected them constricted with KCl 3 x 10(-2) mol/l. NE 3 x 10(-5) mol/l-induced contractures of mesenteric and femoral arterial preparations were not influenced by any concentrations of vapiprost. Results indicate that vapiprost has an antagonistic action on a so-called TP-receptor and/or a vasoconstrictive prostaglandin(s)-receptor and thus produces vasorelaxation.
Norepinephrine (NE) 3 x 10(-5) mol/l also produced sustained contractions in mesenteric and femoral arterial preparations, but not in basilar and coronary arterial preparations. Vapiprost 10(-10)-3 X 10(-6) mol/l relaxed these four arterial preparations constricted with U46619 10(-7) mol/l and PGF2alpha 10(-5) mol/l in a concentration-dependent fashion, but hardly affected them constricted with KCl 3 x 10(-2) mol/l. NE 3 x 10(-5) mol/l-induced contractures of mesenteric and femoral arterial preparations were not influenced by any concentrations of vapiprost. Results indicate that vapiprost has an antagonistic action on a so-called TP-receptor and/or a vasoconstrictive prostaglandin(s)-receptor and thus produces vasorelaxation.
- リンク情報
- ID情報
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- ISSN : 0004-4172
- Web of Science ID : WOS:A1992KB40900011