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Substance P antagonists active in vitro and in vivo.

作者信息

Mizrahi J, Escher E, Caranikas S, D'orléans-Juste P, Regoli D

出版信息

Eur J Pharmacol. 1982 Aug 13;82(1-2):101-5. doi: 10.1016/0014-2999(82)90561-1.

DOI:10.1016/0014-2999(82)90561-1
PMID:6182006
Abstract

[Pro4, Trp7,9]SP-(4-11) and a newly developed compound, [Pro4, Trp7,9,10]SP-(4-11) were shown to be potent antagonists of substance P (SP). They inhibited the hypotensive effect of SP in the anesthetised rats, the vasodilator effect in the rabbit perfused heart and the relaxation induced by SP in dog carotid arteries contracted with noradrenaline. Stimulatory actions of SP in the guinea pig ileum and the guinea pig trachea were also inhibited by the two antagonists, which were shown to be specific for substance P and related peptides in all the pharmacological preparations utilised in the present study.

摘要

相似文献

1
Substance P antagonists active in vitro and in vivo.
Eur J Pharmacol. 1982 Aug 13;82(1-2):101-5. doi: 10.1016/0014-2999(82)90561-1.
2
Receptors for substance P. III. Classification by competitive antagonists.
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3
Tachykinin receptors in smooth muscles: a study with agonists (substance P, neurokinin A) and antagonists.平滑肌中的速激肽受体:一项使用激动剂(P物质、神经激肽A)和拮抗剂的研究。
Eur J Pharmacol. 1985 Nov 26;118(1-2):25-36. doi: 10.1016/0014-2999(85)90659-4.
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Tachykinin antagonists: substitutions in positions 5 and 6 with amino acids from the primary sequence of substance P homologues.
Eur J Pharmacol. 1985 Aug 15;114(2):147-55. doi: 10.1016/0014-2999(85)90622-3.
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Substance P--structure-activity studies and the development of antagonists.P物质——构效关系研究与拮抗剂的开发
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Undeca- and octa-peptide antagonists for substance P, a study on the guinea pig trachea.用于P物质的十一肽和八肽拮抗剂:豚鼠气管研究
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A comparison of the effects of three substance P antagonists on tachykinin-stimulated [3H]-acetylcholine release in the guinea-pig ileum.三种P物质拮抗剂对豚鼠回肠中速激肽刺激的[3H] - 乙酰胆碱释放的影响比较。
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Receptors for substance P. I. The pharmacological preparations.
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引用本文的文献

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Amino Acids. 1993 Jun;5(2):233-8. doi: 10.1007/BF00805985.
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The substance P receptor on rat mast cells and in human skin.大鼠肥大细胞和人类皮肤中的P物质受体。
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Studies on the trigeminal antidromic vasodilatation and plasma extravasation in the rat.大鼠三叉神经逆向性血管舒张和血浆外渗的研究。
J Physiol. 1984 Jan;346:273-85. doi: 10.1113/jphysiol.1984.sp015021.
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Development of a new tachykinin antagonist.一种新型速激肽拮抗剂的研发。
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Proceedings of the British Pharmacological Society. Cardiff, 10th-12th April, 1985. Abstracts.英国药理学会会议记录。加的夫,1985年4月10日至12日。摘要。
Br J Pharmacol. 1985 Jun;85 Suppl(Suppl):204P-393P.
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Study of the contractile effect of 5-hydroxytryptamine (5-HT) in the isolated longitudinal muscle strip from guinea-pig ileum. Evidence for two distinct release mechanisms.豚鼠回肠离体纵行肌条中5-羟色胺(5-HT)收缩效应的研究。两种不同释放机制的证据。
Naunyn Schmiedebergs Arch Pharmacol. 1985 Mar;329(1):36-41. doi: 10.1007/BF00695189.
7
Presence of a substance P-like peptide in an acid extract of the intestinal bulb of the carp (Cyprinus carpio).鲤鱼(鲤属鲤科)肠球部酸提取物中存在P物质样肽。
Br J Pharmacol. 1988 Sep;95(1):39-48. doi: 10.1111/j.1476-5381.1988.tb16546.x.
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Involvement of substance P in the excitatory action of GABAA agonists on cholinergic neurons in the guinea-pig ileum.P物质参与γ-氨基丁酸A受体激动剂对豚鼠回肠胆碱能神经元的兴奋作用。
Naunyn Schmiedebergs Arch Pharmacol. 1987 Jun;335(6):629-35. doi: 10.1007/BF00166979.
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Effect of the tachykinin antagonist, [D-Pro4, D-Trp7,9,10] substance P-(4-11), on tachykinin- and histamine-induced inositol phosphate generation in intestinal smooth muscle.速激肽拮抗剂[D-脯氨酸4,D-色氨酸7,9,10]P物质-(4-11)对速激肽和组胺诱导的肠平滑肌肌醇磷酸生成的影响。
Naunyn Schmiedebergs Arch Pharmacol. 1987 Mar;335(3):296-300. doi: 10.1007/BF00172800.
10
An examination of the pharmacology of two substance P antagonists and the evidence for tachykinin receptor subtypes.两种P物质拮抗剂的药理学研究及速激肽受体亚型的证据
Br J Pharmacol. 1986 Jan;87(1):79-85. doi: 10.1111/j.1476-5381.1986.tb10159.x.