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选择性δ阿片受体激动剂D-丙氨酸-强啡肽II的低温效应

Hypothermic effect of D-Ala-deltorphin II, a selective delta opioid receptor agonist.

作者信息

Broccardo M, Improta G

机构信息

Institute of Pharmacology III, University La Sapienza, Rome, Italy.

出版信息

Neurosci Lett. 1992 May 25;139(2):209-12. doi: 10.1016/0304-3940(92)90554-k.

Abstract

The natural heptapeptide D-Ala-deltorphin II, the most selective agonist for delta-receptors currently available, was used to study the role of brain delta opioid receptors in the control of body temperature. In rats placed in a cold ambient temperature (4 degrees C), intracerebroventricular injections of D-Ala-deltorphin II produced a significant hypothermia. In animals at an ambient temperature of 22 degrees C, only the highest dose employed induced a slight fall in body temperature. At a warm temperature (34 degrees C), D-Ala-deltorphin II induced no significant changes in body temperature. D-Ala-deltorphin II-induced hypothermia, unaffected by naloxone, was significantly reduced by the selective delta receptor antagonist naltrindole. These findings indicate that D-Ala-deltorphin II produces its hypothermic effects at a supraspinal delta receptor, and support the involvement of delta receptors in central control of body temperature.

摘要

天然七肽D-丙氨酰-内啡肽II是目前可用的对δ受体最具选择性的激动剂,被用于研究脑δ阿片受体在体温调节中的作用。将大鼠置于寒冷的环境温度(4摄氏度)中,脑室内注射D-丙氨酰-内啡肽II会导致显著的体温过低。在环境温度为22摄氏度的动物中,只有使用的最高剂量会引起体温略有下降。在温暖的温度(34摄氏度)下,D-丙氨酰-内啡肽II不会引起体温的显著变化。D-丙氨酰-内啡肽II诱导的体温过低不受纳洛酮的影响,但被选择性δ受体拮抗剂纳曲吲哚显著降低。这些发现表明,D-丙氨酰-内啡肽II在脊髓上的δ受体产生其体温过低效应,并支持δ受体参与体温的中枢调节。

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