Nabeshima T, Matsuno K, Kamei H, Kameyama T
Res Commun Chem Pathol Pharmacol. 1985 May;48(2):173-81.
The profile of action of eptazocine, a novel analgesic, on opioid receptors was investigated. Eptazocine caused a concentration-dependent inhibition against the [3H]-naloxone [( 3H]-NLX) specific binding to rat brain synaptic membrane in the absence of sodium cation and GTP (IC50; 7.83 +/- 1.57 microM). The ratios of IC50 values between the absence to the presence of sodium cation alone or sodium cation and GTP were 3.89 and 4.35, respectively. In addition, eptazocine (10 microM) also produced the significant decrease of [3H]-NLX specific binding in the mouse brain synaptic membrane. Moreover, the same dose eptazocine significantly decreased the [3H]-ethylketocyclazocine [( 3H]EKC) specific binding, but not [3H]-phencyclidine [( 3H]-PCP). These results suggest that eptazocine interacts with opioid receptor, and is classified as one of the opiate agonist-antagonist analgesics.
研究了新型镇痛药依他佐辛对阿片受体的作用特征。在无钠离子和鸟苷三磷酸（GTP）的情况下，依他佐辛对[3H] - 纳洛酮（[3H] - NLX）与大鼠脑突触膜的特异性结合产生浓度依赖性抑制（IC50；7.83±1.57微摩尔）。仅存在钠离子或同时存在钠离子和GTP时与无这些成分时的IC50值之比分别为3.89和4.35。此外，依他佐辛（10微摩尔）也使小鼠脑突触膜中[3H] - NLX的特异性结合显著降低。而且，相同剂量的依他佐辛显著降低了[3H] - 乙基酮环佐辛（[3H] - EKC）的特异性结合，但未降低[3H] - 苯环利定（[3H] - PCP）的特异性结合。这些结果表明依他佐辛与阿片受体相互作用，属于阿片激动 - 拮抗型镇痛药之一。
