新型α-2肾上腺素能放射性配体[3H]-MK912在人α-2A、α-2B和α-2C肾上腺素能受体中对α-2C具有选择性。
The novel alpha-2 adrenergic radioligand [3H]-MK912 is alpha-2C selective among human alpha-2A, alpha-2B and alpha-2C adrenoceptors.
作者信息
Uhlén S, Porter A C, Neubig R R
机构信息
Department of Pharmacology, University of Michigan, Ann Arbor.
出版信息
J Pharmacol Exp Ther. 1994 Dec;271(3):1558-65.
We have determined the binding affinities of the novel alpha-2 adrenoceptor antagonist radioligand [3H]-MK912 for the cloned human alpha-2A, alpha-2B and alpha-2C adrenoceptors. The KD-values were 1.25 nM, 1.36 nM and 0.086 nM for the alpha-2A, alpha-2B and alpha-2C subtypes, respectively. Thus, the selectivity of [3H]-MK912 for the human alpha-2C adrenoceptor vs. the human alpha-2A and alpha-2B adrenoceptors is 14-fold and 16-fold, respectively. The alpha-2C selectivity, and the very high affinity of [3H]-MK912 for the alpha-2C adrenoceptor subtype (KD = 86 pM) makes this radioligand a promising tool for studying the role of alpha-2C adrenoceptors in the human. A selection of antagonists useful for differentiating between the human alpha-2A, alpha-2B and alpha-2C adrenoceptor subtypes is discussed.
我们已经测定了新型α-2肾上腺素能受体拮抗剂放射性配体[3H]-MK912对克隆的人α-2A、α-2B和α-2C肾上腺素能受体的结合亲和力。对于α-2A、α-2B和α-2C亚型，KD值分别为1.25 nM、1.36 nM和0.086 nM。因此，[3H]-MK912对人α-2C肾上腺素能受体相对于人α-2A和α-2B肾上腺素能受体的选择性分别为14倍和16倍。α-2C选择性以及[3H]-MK912对α-2C肾上腺素能受体亚型的极高亲和力（KD = 86 pM）使得这种放射性配体成为研究人α-2C肾上腺素能受体作用的有前景的工具。本文讨论了一系列有助于区分人α-2A、α-2B和α-2C肾上腺素能受体亚型的拮抗剂。
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