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AT-076
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AT-076 : ウィキペディア英語版
AT-076

AT-076 is a so-called opioid "pan" antagonist and is the first reasonably balanced antagonist known of all four opioid receptor types. It acts as a silent antagonist of all four of the opioid receptors, behaving as a competitive antagonist of the μ-opioid receptor (Ki = 1.67 nM) and δ-opioid receptor (Ki = 19.6 nM) and as a noncompetitive antagonist of the κ-opioid receptor (Ki = 1.14 nM) and nociceptin receptor (Ki = 1.75 nM).〔 AT-076 was derived from the selective κ-opioid receptor antagonist JDTic via removal of the 3,4-dimethyl group of the ''trans''-(3''R'',4''R'')-dimethyl-4-(3-hydroxyphenyl)piperidine antagonist scaffold, which increased affinity for the nociceptin receptor by 10-fold and for the μ- and δ-opioid receptors by 3-6-fold.〔
==See also==

* Cebranopadol
* Buprenorphine
* BU09059

抄文引用元・出典: フリー百科事典『 ウィキペディア(Wikipedia)
ウィキペディアで「AT-076」の詳細全文を読む



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