Department of Physiology and Anatomy, Faculty of Pharmaceutical Sciences, Tohoku Medical and Pharmaceutical University, 4-4-1 Komatsushima, Aoba-ku, Sendai 981-8558, Japan.
Laboratory of Medicinal Chemistry and Medical Research Laboratories, School of Pharmacy, Kitasato University, 5-9-1 Shirokane, Minato-ku, Tokyo 108-8641, Japan.
Curr Top Med Chem. 2020;20(31):2866-2877. doi: 10.2174/1568026620666200922113430.
Since a μ-opioid receptor gene containing multiple exons has been identified, the variety of splice variants for μ-opioid receptors have been reported in various species. Amidino-TAPA and IBNtxA have been discovered as new analgesics with different pharmacological profiles from morphine. These new analgesics show a very potent analgesic effect but do not have dependence liability. Interestingly, these analgesics show the selectivity to the morphine-insensitive μ-opioid receptor splice variants. The splice variants, sensitive to these new analgesics but insensitive to morphine, may be a better molecular target to develop the analgesics without side effects.
由于已经鉴定出含有多个外显子的 μ-阿片受体基因，因此在各种物种中已经报道了 μ-阿片受体的各种剪接变体。氨甲酰基-TAPA 和 IBNtxA 已被发现为具有与吗啡不同药理学特征的新型镇痛药。这些新型镇痛药表现出非常有效的镇痛作用，但没有依赖性。有趣的是，这些镇痛药对吗啡不敏感的 μ-阿片受体剪接变体具有选择性。对这些新型镇痛药敏感但对吗啡不敏感的剪接变体可能是开发无副作用的镇痛药的更好的分子靶标。
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