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Latest comment: 7 years ago1 comment1 person in discussion
There is an analogue of etonitazene with a carboxamide in US Patent 2,944,062 'Certain Alpha (1-diethylaminoethyl (2), Alpha Aryl Acetamides). The chiral compound is x4 more potent than the parent and the nitrogen of the carboxamide (acetamide) overlays the nitrogen in the piperidine perfectly. From this, and overlays of other compounds, we may be able to spot mu/orl1 agonists. That ORL1 agonists don't depress breathing means that safer opioids can be developed. It has already been established that SB-612,111 increases the analgesia of morphine. It has also been established that both buprenorphine and thienorphine are partial agonists.
Etonitazine, in particular, is an extremely hazardous compound. Sigma-Aldrich describe it as an opiate x100-x1000 morphine in potency. A WHOLE magnitude of difference. The derivative has never been studied outside a few rodent models but if the modification was applied to clonitazine, a compound that may be a)equally active amongst animal models & b)reduce the tolerance & dependence of such compounds. — Preceding unsigned comment added by 81.99.74.135 (talk) 15:36, 28 March 2017 (UTC)Reply
