Lötsch J, Freynhagen R, Geisslinger G
Pharmazentrum Frankfurt/ZAFES, Institut für Klinische Pharmakologie, Johann-Wolfgang-Goethe-Universität, Frankfurt am Main.
Schmerz. 2005 Oct;19(5):378-82, 384-5. doi: 10.1007/s00482-005-0423-x.
Polymorphisms in the mu-opioid receptor gene may potentially alter the clinical effects of opioid analgesics. A common mu-opioid receptor polymorphism occurring at an allelic frequency of 12% decreases the potency of opioid analgesics in humans. Interestingly, in carriers of this mutation, it appears to be possible to reach analgesia by increasing the opioid dose but side effects appear to occur less often despite the higher opioid dose. This suggests a broadened therapeutic range of the opioids. Other mutations of the mu-opioid receptor, for example three mutations within the third intracellular loop of the receptor, impair receptor signaling, but they are too rare to greatly affect pain therapy or have not yet been investigated in the context of pain therapy.
μ-阿片受体基因的多态性可能会改变阿片类镇痛药的临床效果。一种常见的μ-阿片受体多态性，其等位基因频率为12%，会降低阿片类镇痛药对人类的效力。有趣的是，在这种突变的携带者中，似乎可以通过增加阿片类药物剂量来达到镇痛效果，而且尽管阿片类药物剂量较高，但副作用似乎更少出现。这表明阿片类药物的治疗范围有所扩大。μ-阿片受体的其他突变，例如受体第三个细胞内环内的三个突变，会损害受体信号传导，但它们非常罕见，不会对疼痛治疗产生重大影响，或者尚未在疼痛治疗的背景下进行研究。
