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鞘内注射部分阿片类激动剂盐酸纳布啡的镇痛作用。

The analgetic effects of an intrathecally administered partial opiate agonist, nalbuphine hydrochloride.

作者信息

Schmauss C, Doherty C, Yaksh T L

出版信息

Eur J Pharmacol. 1982 Dec 17;86(1):1-7. doi: 10.1016/0014-2999(82)90389-2.

Abstract

Nalbuphine (0.1-200 micrograms), unlike morphine (0.1-10 micrograms) administered intrathecally had no effect on the tail flick or hot plate response latencies. In contrast, both intrathecal nalbuphine and morphine inhibited, in a monotonic, dose dependent fashion, the writhing evoked by intraperitoneally administered acetic acid (ED50 = 38 nmol and 1.12 nmol, respectively.) The effects of intrathecal nalbuphine and morphine was antagonized by an equal dose of naloxone administered systemically. Co-intrathecal administration of morphine and nalbuphine revealed that a maximum inhibition of writhing could be obtained with low doses of either drug, while the effects of higher doses of either drug were attenuated as compared to the effects produced by the high dose of either drug alone. These data are consistent with the suggestion that nalbuphine exerts its agonistic effect through a mechanism that is pharmacologically distinct from that of morphine, and the likelihood of two populations of opioid receptors associated with the pain response evoked by thermal and visceral afferents, respectively is considered.

摘要

与鞘内注射吗啡(0.1 - 10微克)不同,鞘内注射纳布啡(0.1 - 200微克)对甩尾或热板反应潜伏期没有影响。相反,鞘内注射纳布啡和吗啡均以单调、剂量依赖性方式抑制腹腔注射醋酸诱发的扭体反应(ED50分别为38纳摩尔和1.12纳摩尔)。鞘内注射纳布啡和吗啡的作用可被全身给予等量纳洛酮拮抗。鞘内同时给予吗啡和纳布啡显示,低剂量的任何一种药物均可获得最大扭体抑制效果,而与单独使用高剂量的任何一种药物相比,高剂量的任何一种药物的效果均减弱。这些数据与以下观点一致,即纳布啡通过一种在药理学上与吗啡不同的机制发挥其激动作用,并且考虑了分别与热和内脏传入神经诱发的疼痛反应相关的两类阿片受体的可能性。

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