[每周一问]NO.3 阿片受体

2005-09-17 00:00 来源:麻醉疼痛专业讨论版 作者:西门吹血
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[每周一问]NO.3 阿片受体

We continue our discussion of the most commonly used analgesics in the management of pain, opioids. This week we consider opioid receptors.
1. How are opioid receptors similar and different?
我们继续讨论疼痛治疗中最常用的镇痛药—阿片药物。本周主要讨论阿片受体。

1.阿片受体的异同点?

有三种类型的阿片受体,分别为μ,κ,δ受体。
σ受体和伊普西隆(ε)受体不在被认为是阿片受体。除了在兔子体内发现外,没有在人类体内发现有ε受体。σ受体与ketamine相关,其作用不能为纳洛酮所逆转。μ,κ,δ受体均为G-蛋白偶联并有7个跨膜通道蛋白。亚型之间的不同主要是由于对不同阿片受体亲和力的不同,其次是阿片受体基本氨基酸序列的不同。
相对于κ,δ受体来说,大多数临床应用的阿片药物更多的作用于μ受体。克隆了阿片受体后,有前景的新的特效阿片剂将可能被发现,这些药物可以最大的降低疼痛不适,同时使其副作用降至最低。


There are 3 types of opioid receptors:
1.  Mu
2.  Kappa
3.  Delta
Sigma and Epsilon receptors are no longer thought to be opioid receptors. Epsilon receptors have not been found in man (only rats). Sigma receptors bind to ketamine and its effects are not reversible with nalaxone. Mu, Kappa and Delta receptors are all G-protein coupled and have 7 transmembrane spanning proteins. The differences between subtypes are due to different affinities for various opioids secondary to differences in their primary amino acid sequences.
Most clinically used opioids bind and stimulate mu receptors to a much greater extent than kappa and delta receptors. As opioid receptors have been cloned, hopefully new specific agents will be introduced which optimize pain relief while minimizing undesirable side effects.

References:
1.  Atheheson R, Lambert DA. Update on opioid receptors. Br J Anaesth 73:132-34, 1994.
2.  Satoh M, Minami M. Molecular Pharmacology of the opioid receptor. Pharmacol Ther 68:343-65, 1995.
Site Editor: Sunil Eappen, M.D.
Department of Anesthesiology, Perioperative and Pain Medicine, Harvard Medical School


编辑: Zhu

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