Pasternak Gavril, Pan Ying-Xian
Department of Neurology, Memorial Sloan-Kettering Cancer Center, 1275 York Avenue, NY 10065, USA.
Acta Anaesthesiol Taiwan. 2011 Mar;49(1):21-5. doi: 10.1016/j.aat.2010.12.008. Epub 2011 Mar 17.
Most of the potent analgesics currently in use act through the mu opioid receptor. Although they are classified as mu opioids, clinical experience suggests differences among them. The relative potencies of the agents can vary from patient to patient, as well as the side-effect profiles. These observations, coupled with pharmacological approaches in preclinical models, led to the suggestion of multiple subtypes of mu receptors. The explosion in molecular biology has led to the identification of a single gene encoding mu opioid receptors. It now appears that this gene undergoes extensive splicing, in which a single gene can generate multiple proteins. Evidence now suggests that these splice variants may help explain the clinical variability in responses among patients.
目前使用的大多数强效镇痛药都是通过μ阿片受体起作用的。尽管它们被归类为μ阿片类药物,但临床经验表明它们之间存在差异。这些药物的相对效价在不同患者之间可能有所不同,副作用情况也是如此。这些观察结果,再加上临床前模型中的药理学方法,引发了关于μ受体存在多种亚型的推测。分子生物学的迅猛发展导致了一个编码μ阿片受体的单一基因的鉴定。现在看来,这个基因会进行广泛的剪接,即一个单一基因可以产生多种蛋白质。现在有证据表明,这些剪接变体可能有助于解释患者之间临床反应的变异性。