Tagashira E, Kachur J F, Carter W H, Dewey W L
J Pharmacol Exp Ther. 1984 Apr;229(1):214-7.
The ability of tripelennamine and chlorpheniramine to potentiate morphine- and pentazocine-induced antinociception in drug-naive and morphine-tolerant mice was tested utilizing the hot-plate method. Both tripelennamine and chlorpheniramine alone produced dose-dependent increases in hot plate latency which were naloxone reversible. Cross-tolerance developed between tripelennamine and morphine, whereas no cross-tolerance developed between chlorpheniramine and morphine. Neither tripelennamine nor chlorpheniramine significantly potentiated morphine-induced antinociception in drug-naive mice. The effects of tripelennamine and morphine were additive. Tripelennamine but not chlorpheniramine, however, significantly potentiated antinociception produced by low but not high doses of pentazocine in drug-naive mice. Furthermore, in morphine-tolerant mice, tripelennamine, but not chlorpheniramine, potentiated both morphine- and pentazocine-induced antinociception. It is concluded that the abuse of various narcotic-tripelennamine combinations can be attributed, at least in part, to a specific property of tripelennamine to potentiate narcotic effects in the drug-naive and morphine-tolerant state.
利用热板法测试了曲吡那敏和氯苯那敏增强吗啡和喷他佐辛对未用药小鼠和吗啡耐受小鼠诱导的镇痛作用的能力。单独使用曲吡那敏和氯苯那敏均可使热板潜伏期呈剂量依赖性增加,且这种增加可被纳洛酮逆转。曲吡那敏和吗啡之间产生了交叉耐受性,而氯苯那敏和吗啡之间未产生交叉耐受性。在未用药小鼠中,曲吡那敏和氯苯那敏均未显著增强吗啡诱导的镇痛作用。曲吡那敏和吗啡的作用具有相加性。然而,在未用药小鼠中,曲吡那敏而非氯苯那敏可显著增强低剂量而非高剂量喷他佐辛产生的镇痛作用。此外,在吗啡耐受小鼠中,曲吡那敏而非氯苯那敏增强了吗啡和喷他佐辛诱导的镇痛作用。得出的结论是,滥用各种麻醉剂-曲吡那敏组合至少部分可归因于曲吡那敏在未用药和吗啡耐受状态下增强麻醉作用的特定特性。