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[新型脑啡肽类似物的镇痛作用]

[The analgesic action of new enkephalin analogs].

作者信息

Solov'eva E V, Kulikov S V, Khar'kovskiĭ A O, Bogdanov E G

出版信息

Eksp Klin Farmakol. 1994 Nov-Dec;57(6):20-2.

PMID:7756949
Abstract

The enkephalin analogue peptide IKB-901 containing epsilon-ACA and cysteine with the modified S-end shows an analgetic activity in rats (1 micron, intrathecally and 5 mg/kg intravenously) and in cats (0.35 and 0.7 mg/kg intravenously). Naloxone (0.1 mg/kg) prevents the analgetic effect of peptide. The coadministration of the peptide and the enkephalinase inhibitor D-phenylalanine (0.35 and 10 mg/kg, respectively) enhances analgesia and displays an antihypertensive effect in nociceptive stimulation.

摘要

含有ε-ACA和具有修饰S端的半胱氨酸的脑啡肽类似物肽IKB-901在大鼠(鞘内注射1微克和静脉注射5毫克/千克)和猫(静脉注射0.35和0.7毫克/千克)中显示出镇痛活性。纳洛酮(0.1毫克/千克)可预防该肽的镇痛作用。该肽与脑啡肽酶抑制剂D-苯丙氨酸(分别为0.35和10毫克/千克)共同给药可增强镇痛作用,并在伤害性刺激中显示出降压作用。

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