Pasternak Gavril W
Laboratory of Molecular Neuropharmacology and Department of Neurology, Memorial Sloan-Kettering Cancer Center, New York, New York, USA.
J Pain Symptom Manage. 2005 May;29(5 Suppl):S2-9. doi: 10.1016/j.jpainsymman.2005.01.011.
Opioids provide excellent pain relief in most patients. Yet the responses of patients to individual opioids can vary markedly, even among the mu opioids. Understanding this variability would greatly enhance our ability to treat patients appropriately. Classical pharmacological studies have long implied the existence of multiple subtypes of mu opioid receptors. More recently, a number of variants of the cloned mu opioid receptor have been described. These variants all show the same selectivity for mu opioids, confirming their classification as mu opioid receptors. Yet, they differ in their functional activation by opioids as well as in their localization within cells and regions in the brain. These multiple mu opioid receptors may help explain the range of responses seen clinically among patients for the various opioid drugs.
阿片类药物在大多数患者中能提供出色的疼痛缓解效果。然而,即使在μ阿片类药物中,患者对个体阿片类药物的反应也可能有显著差异。了解这种变异性将极大地提高我们合理治疗患者的能力。长期以来,经典药理学研究一直暗示存在多种μ阿片受体亚型。最近,已描述了克隆的μ阿片受体的多种变体。这些变体对μ阿片类药物均表现出相同的选择性,证实它们可归类为μ阿片受体。然而,它们在阿片类药物的功能激活以及在细胞和脑区中的定位方面存在差异。这些多种μ阿片受体可能有助于解释临床上患者对各种阿片类药物所表现出的反应范围。