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| Formula | C26H35N3O3 |
| Molar mass | 437.584 g·mol−1 |
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AT-076 is a so-calledopioid "pan" antagonist and is the first reasonably balancedantagonist known of all fouropioid receptor types.[1] It acts as asilent antagonist of all four of the opioid receptors, behaving as acompetitive antagonist of theμ-opioid receptor (Ki = 1.67 nM) andδ-opioid receptor (Ki = 19.6 nM) and as anoncompetitive antagonist of theκ-opioid receptor (Ki = 1.14 nM) andnociceptin receptor (Ki = 1.75 nM).[1] AT-076 was derived from the selective κ-opioid receptor antagonistJDTic via removal of the 3,4-dimethyl group of thetrans-(3R,4R)-dimethyl-4-(3-hydroxyphenyl)piperidine antagonist scaffold which increasedaffinity for the nociceptin receptor by 10-fold and for the μ- and δ-opioid receptors by 3-6-fold.[1]
