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For ages I was fascinated by ketobemidone analogues. Could it really be that N-methyl was the only full agonist? As it turns out, no. The example here is 15x the parent. I feel comfortable showing this one as it really WOULD be too much like hard work for the dodgy RC companies to make it. I haven't mentioned the patent number, I'm sure the interested can find it soon enough.
My other surprise was that substituting the piperidine ring results in inactive compounds. I noted that picenadol was made from the trans isomers of a compound and that while one was a pure agonist, the other was an antagonist. As far as I am aware, nobody ever bothered to separate the isomers of, say, 3-methyl ketobemidone. Careful overlaying shows that the appropriate isomer of ketobemidone WILL overlay but it would have to possess some very special properties to be worth the effort. In this, it's like allylprodine. The interesting thing about that is that compound is that the alkene spatially overlays the alkene in 14-Cinnamoyloxycodeinone - so it's possible for people modeling the specific binding sites of the mu receptor can place the alkene. Interestingly, it only works if the aromatic bears a phenolic group.
For ages I was fascinated by ketobemidone analogues. Could it really be that N-methyl was the only full agonist? As it turns out, no. The example here is 15x the parent. I feel comfortable showing this one as it really WOULD be too much like hard work for the dodgy RC companies to make it. I haven't mentioned the patent number, I'm sure the interested can find it soon enough.
My other surprise was that substituting the piperidine ring results in inactive compounds. I noted that picenadol was made from the trans isomers of a compound and that while one was a pure agonist, the other was an antagonist. As far as I am aware, nobody ever bothered to separate the isomers of, say, 3-methyl ketobemidone. Careful overlaying shows that the appropriate isomer of ketobemidone WILL overlay but it would have to possess some very special properties to be worth the effort. In this, it's like allylprodine. The interesting thing about that is that compound is that the alkene spatially overlays the alkene in 14-Cinnamoyloxycodeinone - so it's possible for people modeling the specific binding sites of the mu receptor can place the alkene. Interestingly, it only works if the aromatic bears a phenolic group.
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