D-精氨酸[Hyp3-硫代5-D-噻吨7-噻吨8]-缓激肽，一种平滑肌BK2受体和BK3受体的强效拮抗剂。
D-Arg[Hyp3-Thi5-D-Tic7-Tic8]-bradykinin, a potent antagonist of smooth muscle BK2 receptors and BK3 receptors.
作者信息
Farmer S G, Burch R M, Kyle D J, Martin J A, Meeker S N, Togo J
机构信息
Nova Pharmaceutical Corporation, Baltimore, Maryland 21224.
出版信息
Br J Pharmacol. 1991 Apr;102(4):785-7. doi: 10.1111/j.1476-5381.1991.tb12251.x.
Abstract
D-Arg[Hyp3-Thi5-D-Tic7-Tic8]-bradykinin (NPC 16731) inhibited bradykinin (BK) binding and BK-induced contraction in guinea-pig ileum, being markedly more potent than D-Phe7-BK analogues as a BK2 receptor antagonist. In isolated trachea NPC 16731, unlike other BK2 antagonists, inhibited BK binding and BK-induced contraction, and 45Ca2+ efflux in tracheal smooth muscle cells. That NPC 16731 potently inhibits BK effects in trachea provides further evidence for the existence of the airway BK3 receptor.
摘要
D-精氨酸[Hyp3-硫代5-D-噻唑烷7-噻唑烷8]-缓激肽（NPC 16731）抑制豚鼠回肠中缓激肽（BK）的结合及BK诱导的收缩，作为BK2受体拮抗剂，其效力明显强于D-苯丙氨酸7-BK类似物。在离体气管中，与其他BK2拮抗剂不同，NPC 16731抑制BK的结合、BK诱导的收缩以及气管平滑肌细胞中的45Ca2+外流。NPC 16731有效抑制气管中BK的作用，为气道BK3受体的存在提供了进一步证据。
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