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Formula | C27H29IN2O4 |
Molar mass | 572.443 g·mol−1 |
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IBNtxA, or3-iodobenzoyl naltrexamine, is an atypicalopioidanalgesic drug derived fromnaltrexone. In animal studies it produces potent analgesic effects that are blocked bylevallorphan[1] and so appear to beμ-opioid mediated, but it fails to produceconstipation orrespiratory depression, and is neither rewarding or aversive[2] inconditioned place preference protocols.[3] These unusual properties are thought to result from agonist action at asplice variant orheterodimer of the μ-opioid receptor,[4] rather than at the classical full length form targeted by conventional opioid drugs.[5]
In the Radioligand binding assay it has shown to have affinities of 0.11nM at the MOR, 0.24nM at the DOR and 0.03nM at the KOR and in the Hot- Plate Assay it is shown to be around 20x more potent thanmorphine. Azido Aryl Analogues of IBNtxA retain significant activity at the MOR.[6]