ALTERATIONS IN PHARMACOLOGICAL RECEPTOR ACTIVITIES OF RABBIT ARTERIES BY SULFHYDRYL REAGENTS
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概要
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The addition of 1×10<SUP>-3</SUP> M or 1×10<SUP>-2</SUP> M 2-mercaptoethanol (2-MEt), a sulfhydryl reagent, produced a leftward displacement (potentiation) of the dose-response curves of mesenteric arterial strips for histamine, norepinephrine, serotonin, angiotensin II, prostaglandin F<SUB>2α</SUB> and KCl. N-ethyl maleimide abolished the 2-MEt-induced potentiation of the arterial responses. Dithiothreitol (DTT) and cysteine also potentiated the contraction by these agonists in mesenteric arterial strips, suggesting that the sulfhydryl group plays a role in the arterial responses to various contractile agonists. In contrast to the mesenteric arterial strips, 2-MEt abolished the contraction by angiotensin II without greatly affecting contraction by norepinephrine in the thoracic aorta, femoral, renal and carotid arterial strips. These data suggest that there are regional differences in the responsiveness of rabbit arteries to sulfhydryl reagents. In mesenteric arterial strips treated with 1×10<SUP>-6</SUP> M histamine, 6×10<SUP>-8</SUP> M norepinephrine or 1×10<SUP>-9</SUP> M angiotensin II after exposure to Ca<SUP>2+</SUP>-free Krebs bicarbonate solutions containing 0.1 mM EGTA, the addition of 2.5 mM CaCl<SUB>2</SUB> caused a contraction (agonist-induced Ca<SUP>2+</SUP>-contraction). Sulfhydryl reagents potentiated each agonist-induced Ca<SUP>2+</SUP>-contraction in this artery. Moreover, in thoracic aortic strips, sulfhydryl reagents enhanced only histamine-induced Ca<SUP>2+</SUP>-contraction and attenuated norepinephrine- and angiotensin II-induced Ca<SUP>2+</SUP>-contractions. It is concluded that the reduction of a disulfide bond of the arterial strips to a sulfhydryl group affects the pharmacological receptor activities of the strips and that the changes in the receptor activities may be related to the changes in the transmembrane influx of calcium.
- 社団法人 日本薬理学会の論文
著者
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Asano Masahisa
Department Of Pharmacology Nagoya City University Medical School
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Hidaka Hiroyoshi
Department Of Pharmacology Nagoya University School Of Medicine
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Hidaka Hiroyoshi
Department Of Pharmacology Mie University
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