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-(3R,4R)-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.
primaryTopic
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-(3R,4R)-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.
has abstract
AT-076 is a so-called opioid " ...... -opioid receptors by 3-6-fold.
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IUPAC name
(3R)-7-hydroxy-N-[(2S)-1-[4-(3 ...... ydroisoquinoline-3-carboxamide
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PubChem
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Wikipage page ID
46,401,622
Wikipage revision ID
734,296,383
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CC[C@@H]NC[C@H]3CC4=CC=CO
StdInChIKey
LGYDWJJZDCXEOV-JWQCQUIFSA-N
subject
comment
AT-076 is a so-called opioid " ...... -opioid receptors by 3-6-fold.
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label
AT-076
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