Английская Википедия:IBNtxA
Шаблон:Short description Шаблон:Drugbox
IBNtxA, or 3-iodobenzoyl naltrexamine, is an atypical opioid analgesic drug derived from naltrexone. In animal studies it produces potent analgesic effects that are blocked by levallorphan[1] and so appear to be μ-opioid mediated, but it fails to produce constipation or respiratory depression, and is neither rewarding or aversive[2] in conditioned place preference protocols.[3] These unusual properties are thought to result from agonist action at a splice variant or heterodimer 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 than morphine. Azido Aryl Analogues of IBNtxA retain significant activity at the MOR.[6]
References
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Шаблон:Cite journal
- ↑ Keck TM, Uddin MM, Babenko E, Wu C, Moura-Letts G. Abuse Liability and Anti-Addiction Potential of the Atypical Mu Opioid Receptor Agonist IBNtxA. The FASEB Journal 31 (1 Supplement), 985.4-985.4, 2017
- ↑ Шаблон:Cite journal
