US-2017217913-A1
I'm not surprised that researchers have gone on to establish the QSAR of MOR agonists thar are based on tianeptine, It was @fastandbulbous who accurately described the chemistry of such compounds as having a certain element of 'black magic'. [1229] onwards lists the EC50 of some of the compounds covered by the patent. Example 83 appears to be the most active.
[1230] onwards lists activity relative to the prototype (tianeptine) and several 'rules' are divined to estimate said activity.
While none of the examples are likely to be of particularly potent, it does provide a class seemingly unrelated to all previously demonstrated MOR agonists. While example 83 (1.81 μM) might be considered quite active, I doubt the synthesis would make any of the series facile targets for custom synthesis. Possibly in a single step.
That said, depending on the synthesis, it may be the case that an intermediate used in the synthesis of tianeptine could be obtained to produce that specific compound.
I think it important to note that toxicology information does not seem to be available and what we do know about tianeptine suggests that it's a rare example of a super-agonist. If that proves to be the case, it introduces even more risks. But overall I consider it to be primarily of academic interest.
I'm not surprised that researchers have gone on to establish the QSAR of MOR agonists thar are based on tianeptine, It was @fastandbulbous who accurately described the chemistry of such compounds as having a certain element of 'black magic'. [1229] onwards lists the EC50 of some of the compounds covered by the patent. Example 83 appears to be the most active.
[1230] onwards lists activity relative to the prototype (tianeptine) and several 'rules' are divined to estimate said activity.
While none of the examples are likely to be of particularly potent, it does provide a class seemingly unrelated to all previously demonstrated MOR agonists. While example 83 (1.81 μM) might be considered quite active, I doubt the synthesis would make any of the series facile targets for custom synthesis. Possibly in a single step.
That said, depending on the synthesis, it may be the case that an intermediate used in the synthesis of tianeptine could be obtained to produce that specific compound.
I think it important to note that toxicology information does not seem to be available and what we do know about tianeptine suggests that it's a rare example of a super-agonist. If that proves to be the case, it introduces even more risks. But overall I consider it to be primarily of academic interest.
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