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所选阿片类药物及颅内强化反应。

Selected opioids and responding for intracranial reinforcement.

作者信息

Reid L D, Hubbell C L, Dunn L L, Hunter G A, Costa T

出版信息

Neuropeptides. 1985 Feb;5(4-6):331-4. doi: 10.1016/0143-4179(85)90020-4.

Abstract

Rats fixed with chronically indwelling electrodes for intracranial stimulation (ICS) of the lateral hypothalamus pressed a lever during daily sessions for a fixed intensity of ICS. Before some sessions, they were given placebo, or ethylketocyclazocine (EKC) in racemic or isomeric forms [either (+)EKC or (-)EKC]. Naloxone (NX) was also given with the agents. The racemate facilitated pressing across a narrow range of small doses (centered about 0.02 mg/kg). At no dose did (-)EKC, a potent analgesic, facilitate pressing and typically depressed it. (+)EKC, at doses of 0.04 and 0.08 mg/kg, facilited pressing. These data provide further confirmation that opioid analgesia and ability to enhance pressing are separable. When NX was given with a large dose of the racemate, paradoxically pressing for ICS was facilitated. Apparently, NX selectively blocked the effects of (-)EKC. SKF 10047 was also administered in racemic and isomeric forms. All three forms produced some facilitation of pressing at small doses (e.g., 0.75 mg/kg) and depressed pressing at large doses (e.g., 5.0 mg/kg).

摘要

通过长期植入电极进行下丘脑外侧颅内刺激(ICS)的大鼠,在每日实验期间,会为了固定强度的ICS而按压杠杆。在某些实验前,给它们注射安慰剂,或以消旋体或异构体形式(即(+)EKC或(-)EKC)注射乙基酮环唑辛(EKC)。同时也给它们注射纳洛酮(NX)。消旋体在小剂量的窄范围内(以约0.02mg/kg为中心)促进按压。强效镇痛药(-)EKC在任何剂量下都没有促进按压,反而通常会抑制按压。(+)EKC在0.04和0.08mg/kg的剂量下促进按压。这些数据进一步证实了阿片类镇痛作用和增强按压能力是可分离的。当给大鼠注射大剂量消旋体并同时注射NX时,矛盾的是,为了ICS而进行的按压得到了促进。显然,NX选择性地阻断了(-)EKC的作用。SKF 10047也以消旋体和异构体形式给药。所有三种形式在小剂量(如0.75mg/kg)时都产生了一定程度的按压促进作用,而在大剂量(如5.0mg/kg)时则抑制按压。

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