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[各种阿片类药物的μ、δ和κ特性]

[The mu, delta and kappa properties of various opioids].

作者信息

Ohta S, Niwa M, Nozaki M, Hattori M, Shimonaka H, Dohi S

机构信息

Department of Anesthesiology & Critical Care Medicine, Gifu University School of Medicine.

出版信息

Masui. 1995 Sep;44(9):1228-32.

PMID:8523655
Abstract

Recently, the highly selective mu, delta and kappa radiolabeled opioid ligands, such as 3H-DAGO (mu ligand), 3H-DPDPE (delta ligand) and 3H-U69593 (kappa ligand) are available. Using the kappa-homogeneous preparations from human placenta and mu-enriched gerbil cerebellum membrane preparations with these highly selective radiolabeled opioid ligands, clinically used opioids were tested for their mu, delta and kappa properties. The mu agonists such as morphine and fentanyl display a very low affinity for delta and kappa receptor. Among the agonist-antagonist, buprenorphine and butorphanol appeared to be the most highly selective agonists for mu and kappa opioid receptors, respectively. Most ligands identified as specific agonists are in fact only selective and appear to interact at more than one receptor type.

摘要

最近,有了高选择性的μ、δ和κ放射性标记阿片样物质配体,如3H-DAGO(μ配体)、3H-DPDPE(δ配体)和3H-U69593(κ配体)。使用来自人胎盘的κ同质性制剂以及富含μ的沙鼠小脑膜制剂和这些高选择性放射性标记阿片样物质配体,对临床使用的阿片类药物的μ、δ和κ特性进行了测试。μ激动剂如吗啡和芬太尼对δ和κ受体的亲和力非常低。在激动剂-拮抗剂中,丁丙诺啡和布托啡诺似乎分别是μ和κ阿片受体的最高选择性激动剂。大多数被鉴定为特异性激动剂的配体实际上只是选择性的,并且似乎能与不止一种受体类型相互作用。

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