CAJ | 학술논문

阿片类镇痛药镇痛活性好,广泛用于临床.阿片受体主要分为3种亚型,即μ、δ、κ阿片受体.目前临床上使用的阿片类镇痛药大多为μ受体激动剂,但易引起成瘾性、呼吸抑制等副作用.δ受体激动剂镇痛活性较弱,但δ受体激动剂和拮抗剂均能调节μ受体激动剂的镇痛作用,同时参与成瘾性等副作用形成.因此,设计具有μ/δ双重功效的药物是新一代低毒副作用镇痛药的发展方向.该文综述了具有μ/δ双重功效药物的研究现状,为设计低毒副作用镇痛药物提供新思路.
아편류진통약진통활성호,엄범용우림상.아편수체주요분위3충아형,즉μ、δ、κ아편수체.목전림상상사용적아편류진통약대다위μ수체격동제,단역인기성은성、호흡억제등부작용.δ수체격동제진통활성교약,단δ수체격동제화길항제균능조절μ수체격동제적진통작용,동시삼여성은성등부작용형성.인차,설계구유μ/δ쌍중공효적약물시신일대저독부작용진통약적발전방향.해문종술료구유μ/δ쌍중공효약물적연구현상,위설계저독부작용진통약물제공신사로.
Opioid analgesics are potent pain-killer and are widely used in clinical practice.Opioid receptors are classified into μ,δ,κ subtypes.Most of the currently available opioid analgesics are μ opioid receptor agonists, but they cause undesired side effects such as physical dependence, respiratory depression and constipation and so on.The antalgic activity of δ receptor agonist is weaker than that of μ agonist, but it can modulate the activity of μ receptor and prevent its addiction. Therefore, discovering and designing compounds with μ/δ dual action is a new way for finding analgesics with low toxicity and less side effects.This review summarizes the development of compound with dual μ/δ activities and provides a new strategy for designing analgesics with low toxicity and less side effects.