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苯环利定及其衍生物与烟碱型受体离子通道相互作用的表征

Characterization of the interaction of phencyclidine and its derivatives with the ionic channel of the nicotinic receptor.

作者信息

Haring R, Theomy S, Kalir A, Sokolovsky M

出版信息

Arch Toxicol Suppl. 1983;6:81-90. doi: 10.1007/978-3-642-69083-9_12.

DOI:10.1007/978-3-642-69083-9_12
PMID:6312926
Abstract

(3H)-Phencyclidine (PCP) binds specifically to the cholinergic ionophore in synaptic membranes prepared from Torpedo electric organ. Experiments performed by the centrifugation method establish that the binding is saturable, reversible and selective and can be characterized by a single dissociation constant (3.6 +/- 1.8 microM). The maximal binding capacity is 600 +/- 150 pmol/mg of membrane protein. Bound (3H)-PCP can be displaced by unlabelled PCP and a series of its derivatives. The reactivity of PCP derivatives in binding to (3H)-PCP binding sites, as related to structural changes at the phenyl, piperidyl and cyclohexyl moieties, is discussed.

摘要

(3H)-苯环己哌啶(PCP)特异性结合于从电鳐电器官制备的突触膜中的胆碱能离子载体。通过离心法进行的实验表明,这种结合具有饱和性、可逆性和选择性,并且可以用单一解离常数(3.6±1.8微摩尔)来表征。最大结合容量为600±150皮摩尔/毫克膜蛋白。结合的(3H)-PCP可以被未标记的PCP及其一系列衍生物取代。讨论了PCP衍生物与(3H)-PCP结合位点结合的反应性,这与苯基、哌啶基和环己基部分的结构变化有关。

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1
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Arch Toxicol Suppl. 1983;6:81-90. doi: 10.1007/978-3-642-69083-9_12.
2
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