Jones D N, Bowen W D, Portoghese P S, Holtzman S G
Department of Pharmacology, Emory University School of Medicine, Atlanta, GA 30322-3090.
Eur J Pharmacol. 1993 Nov 9;249(2):167-77. doi: 10.1016/0014-2999(93)90429-l.
Naloxone and naltrindole attenuate the locomotor response to amphetamine, implicating delta-opioid receptors in the opioid-antagonist/amphetamine interaction. To determine the role of delta-opioid receptor subtypes in this phenomenon, rats were pretreated with the following selective antagonists administered intracisternally: naltrindole, [D-Ala2,Leu5,Cys6]enkephalin (DALCE, delta 1 receptor selective), naltrindole-5'-isothiocyanate (delta 2 receptor selective). Cumulative dose-response curves to amphetamine were constructed (saline, 0.1, 0.4, 1.6 and 6.4 mg/kg s.c.), with injections every 30 min. Naltrindole was also tested against cumulative doses of cocaine (saline, 3.0, 10, 30 and 56 mg/kg i.p.). Gross and fine motor activity were recorded for 20 min, commencing 10 min postinjection. Amphetamine and cocaine dose dependently increased both gross and fine movements. Naltrindole (10 micrograms) attenuated the gross but not fine activity response to amphetamine, but 10 or 30 micrograms failed to influence the response to cocaine. Naltrindole-5'-isothiocyanate (30 micrograms) attenuated slightly but significantly the gross activity response to amphetamine, whereas DALCE (30 micrograms) was without effect. However, a combination of 10 micrograms each of DALCE and naltrindole-5'-isothiocyanate markedly attenuated the amphetamine-induced increases in gross movements without altering fine activity. These data provide further evidence for the involvement of delta-opioid receptors in the modulation of behavioral effects of amphetamine; both delta 1- and delta 2-opioid receptors appear to play a role. The differential effects of opioid antagonists on locomotor activity stimulated by amphetamine and cocaine suggests differences in the mechanism of action of these drugs not previously appreciated.
纳洛酮和纳曲吲哚可减弱对苯丙胺的运动反应,提示δ-阿片受体参与了阿片拮抗剂/苯丙胺的相互作用。为了确定δ-阿片受体亚型在此现象中的作用,给大鼠脑池内注射以下选择性拮抗剂进行预处理:纳曲吲哚、[D-丙氨酸2,亮氨酸5,半胱氨酸6]脑啡肽(DALCE,δ1受体选择性拮抗剂)、纳曲吲哚-5'-异硫氰酸盐(δ2受体选择性拮抗剂)。构建苯丙胺的累积剂量-反应曲线(生理盐水、0.1、0.4、1.6和6.4mg/kg皮下注射),每30分钟注射一次。还用纳曲吲哚测试了对累积剂量可卡因(生理盐水、3.0、10、30和56mg/kg腹腔注射)的反应。在注射后10分钟开始记录20分钟的总体和精细运动活动。苯丙胺和可卡因剂量依赖性地增加了总体和精细运动。纳曲吲哚(10微克)减弱了对苯丙胺的总体活动反应,但未影响精细活动反应,而10或30微克未能影响对可卡因的反应。纳曲吲哚-5'-异硫氰酸盐(30微克)轻微但显著地减弱了对苯丙胺的总体活动反应,而DALCE(30微克)则无作用。然而,10微克的DALCE和纳曲吲哚-5'-异硫氰酸盐联合使用可显著减弱苯丙胺诱导的总体运动增加,而不改变精细活动。这些数据为δ-阿片受体参与调节苯丙胺的行为效应提供了进一步证据;δ1和δ2阿片受体似乎都发挥了作用。阿片拮抗剂对苯丙胺和可卡因刺激的运动活动的不同影响表明,这些药物的作用机制存在差异,这一点以前未被认识到。