Verma A, Kulkarni S K
Department of Pharmaceutical Sciences, Panjab University, Chandigarh, India.
J Pharm Pharmacol. 1991 Feb;43(2):131-3. doi: 10.1111/j.2042-7158.1991.tb06649.x.
The involvement of D2-dopamine receptors in the antinociceptive action of B-HT 920 (2-amino-6-allyl-5,6,7,8-tetrahydro-(4H) thiazolo-(4,5d)-azepine) has been investigated in mice. B-HT 920 (0.1-2.0 mg kg-1) and apomorphine (0.1-2.0 mg kg-1) produced a dose-dependent increase in tail flick latency. Analgesia induced by apomorphine was blocked by the D2-antagonist, haloperidol (1 mg kg-1) but not by the opioid antagonist, naloxone (1 mg kg-1). The antinociceptive action of B-HT 920 was potentiated by the D1-agonist SKF 38393 (5 mg kg-1), an action antagonized by haloperidol. The selective alpha 2-adrenoceptor blocking drug yohimbine (1 mg kg-1) and naloxone (1 mg kg-1) blocked the antinociceptive action of B-HT 920 (1 mg kg-1). Haloperidol, however, failed to modify the B-HT 920-induced increase in tail flick latency. B-HT 920 and apomorphine reversed reserpine (2 mg kg-1) 4 h-induced hyperalgesia. The reversing action of apomorphine was blocked by haloperidol but not by yohimbine. Thus, a role of alpha 2-adrenoceptors and D2-dopamine receptors is postulated in the antinociceptive action of B-HT 920.
已在小鼠中研究了D2 - 多巴胺受体在B - HT 920(2 - 氨基 - 6 - 烯丙基 - 5,6,7,8 - 四氢 -(4H)噻唑并 -(4,5 - d)氮杂卓)抗伤害感受作用中的参与情况。B - HT 920(0.1 - 2.0毫克/千克)和阿扑吗啡(0.1 - 2.0毫克/千克)使甩尾潜伏期呈剂量依赖性增加。阿扑吗啡诱导的镇痛作用被D2拮抗剂氟哌啶醇(1毫克/千克)阻断,但未被阿片类拮抗剂纳洛酮(1毫克/千克)阻断。D1激动剂SKF 38393(5毫克/千克)增强了B - HT 920的抗伤害感受作用,该作用被氟哌啶醇拮抗。选择性α2 - 肾上腺素能受体阻断药物育亨宾(1毫克/千克)和纳洛酮(1毫克/千克)阻断了B - HT 920(1毫克/千克)的抗伤害感受作用。然而,氟哌啶醇未能改变B - HT 920诱导的甩尾潜伏期增加。B - HT 920和阿扑吗啡逆转了利血平(2毫克/千克)4小时诱导的痛觉过敏。阿扑吗啡的逆转作用被氟哌啶醇阻断,但未被育亨宾阻断。因此,推测α2 - 肾上腺素能受体和D2 - 多巴胺受体在B - HT 920的抗伤害感受作用中起作用。