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大鼠皮下注射后,强啡肽及其类似物的抗伤害感受、催乳素释放和肠道运动抑制活性。

Antinociceptive, prolactin releasing and intestinal motility inhibiting activities of dermorphin and analogues after subcutaneous administration in the rat.

作者信息

Rossi A, di Salle E, Briatico G, Arcari G, de Castiglione R, Perseo G

出版信息

Peptides. 1983 Jul-Aug;4(4):577-80. doi: 10.1016/0196-9781(83)90064-5.

DOI:10.1016/0196-9781(83)90064-5
PMID:6647121
Abstract

A series of analogues and shorter homologues of dermorphin (DM), a frog skin heptapeptide with potent morphine-like activity, have been assayed in the rat after subcutaneous (SC) administration at the screening dose of 4 mg/kg. The effects taken into account are: analgesia (tail-pinch test), stimulation of prolactin (PRL) secretion, and inhibition of gastro-intestinal (GI) motility (charcoal meal transit). Effective doses were calculated for the most active compounds. The potency of DM (H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2) in the different tests was: tail-pinch: ED50 = 0.83 mg/kg; PRL release: ED100 = 0.3 mg/kg; inhibition of GI motility: ED30 = 1.8 mg/kg.

摘要

肤吗啡(DM)是一种具有强吗啡样活性的蛙皮七肽,已对其一系列类似物和较短的同系物以4mg/kg的筛选剂量进行皮下注射后在大鼠体内进行了测定。所考虑的效应包括:镇痛(夹尾试验)、催乳素(PRL)分泌刺激以及胃肠(GI)蠕动抑制(炭末推进试验)。计算了最具活性化合物的有效剂量。DM(H-Tyr-D-Ala-Phe-Gly-Tyr-Pro-Ser-NH2)在不同试验中的效力为:夹尾试验:ED50 = 0.83mg/kg;PRL释放:ED100 = 0.3mg/kg;胃肠蠕动抑制:ED30 = 1.8mg/kg。

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Antinociceptive, prolactin releasing and intestinal motility inhibiting activities of dermorphin and analogues after subcutaneous administration in the rat.大鼠皮下注射后,强啡肽及其类似物的抗伤害感受、催乳素释放和肠道运动抑制活性。
Peptides. 1983 Jul-Aug;4(4):577-80. doi: 10.1016/0196-9781(83)90064-5.
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