一种P物质拮抗剂（D-脯氨酸2，D-色氨酸7,9）-P物质的作用机制。
The mechanism of action of a substance P antagonist (D-Pro2, D-Trp7,9)-SP.
作者信息
Håkanson R, Hörig J, Leander S
出版信息
Br J Pharmacol. 1982 Dec;77(4):697-700. doi: 10.1111/j.1476-5381.1982.tb09348.x.
Abstract
1 A newly synthesized substance P (SP) analogue, (D-Pro2, D-Trp7,9)-SP, specifically antagonizes the contractile effects of SP on the guinea-pig isolated taenia coli. In addition, previous studies had indicated that the SP analogue per se is capable of contracting this preparation. The results of the present study on the guinea-pig taenia suggest that the smooth muscle contractions produced by the SP analogue are due to histamine release. No contractions were observed following blockade of histamine H1-receptors by mepyramine or following pretreatment with the histamine liberating agent, compound 48/80. 2 Analysis of the inhibition of SP-induced contraction by the analogue suggests that the inhibition is of the competitive type; pA2 was calculated to be 6.1. 3 We conclude that (D-Pro2, D-Trp7,9)-SP is a competitive SP antagonist with histamine-releasing properties.
摘要
- 一种新合成的P物质（SP）类似物，（D-脯氨酸2，D-色氨酸7,9）-SP，可特异性拮抗SP对豚鼠离体结肠带的收缩作用。此外，先前的研究表明，该SP类似物本身能够使该标本收缩。本研究对豚鼠结肠带的结果表明，SP类似物产生的平滑肌收缩是由于组胺释放所致。在用美吡拉敏阻断组胺H1受体后或用组胺释放剂化合物48/80预处理后，未观察到收缩。2. 对该类似物抑制SP诱导收缩的分析表明，这种抑制属于竞争性类型；计算得出的pA2为6.1。3. 我们得出结论，（D-脯氨酸2，D-色氨酸7,9）-SP是一种具有组胺释放特性的竞争性SP拮抗剂。
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A specific substance P antagonist blocks smooth muscle contractions induced by non-cholinergic, non-adrenergic nerve stimulation.一种特异性P物质拮抗剂可阻断由非胆碱能、非肾上腺素能神经刺激所引起的平滑肌收缩。
Nature. 1981 Dec 3;294(5840):467-9. doi: 10.1038/294467a0.
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Release of histamine by substance P.P物质引起组胺释放。
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