Bodnar R J, Kelly D D, Glusman M
Pharmacol Biochem Behav. 1979 Sep;11(3):297-301. doi: 10.1016/0091-3057(79)90138-2.
Acute administration of 2-deoxy-D-glucose (2-DG), an antimetabolic glucose analogue induces a powerful analgesia which adapts following repeated administration. 2-DG analgesia displays significant cross-tolerance with morphine, and like morphine analgesia, is potentiated in hypophysectomized rats. The present study examined further the role of opiates in 2-DG analgesia by examining whether the opiate antagonist, naloxone, would affect 2-DG analgesia, and whether ineffective doses of 2-DG and morphine would interact in a synergistic fashion to induce analgesia. Nociceptive thresholds were measured by the flinch-jump test. Naloxone doses of 1, 5, 10 and 20 mg/kg were all ineffective in reducing significantly 2-DG (600 mg/kg) induced pain threshold elevations. Naloxone failed to attenuate 2-DG (350 mg/kg) analgesia whether administered before or after the 2-DG injection. On the other hand, simultaneous administration of sub-analgesic doses of 2-DG (200 mg/kg) and morphine (2.5 mg/kg) summated to produce significant analgesia. This, 2-DG analgesia is similar to opiates in its tolerant and summative actions, yet dissimilar in that naloxone is ineffective in reversing its effects.
急性给予抗代谢葡萄糖类似物2-脱氧-D-葡萄糖(2-DG)可诱导强烈的镇痛作用,但重复给药后会产生适应性。2-DG镇痛与吗啡表现出显著的交叉耐受性,并且与吗啡镇痛一样,在垂体切除的大鼠中增强。本研究通过检查阿片类拮抗剂纳洛酮是否会影响2-DG镇痛,以及无效剂量的2-DG和吗啡是否会以协同方式相互作用以诱导镇痛,进一步研究了阿片类药物在2-DG镇痛中的作用。通过退缩跳跃试验测量伤害性感受阈值。1、5、10和20mg/kg剂量的纳洛酮均不能显著降低2-DG(600mg/kg)诱导的痛阈升高。无论在2-DG注射前还是注射后给药,纳洛酮均不能减弱2-DG(350mg/kg)的镇痛作用。另一方面,同时给予亚镇痛剂量的2-DG(200mg/kg)和吗啡(2.5mg/kg)可产生显著的镇痛作用。因此,2-DG镇痛在耐受性和累加作用方面与阿片类药物相似,但不同之处在于纳洛酮不能逆转其作用。