The perfect antidepressant? Ketamine cousin

[Gaffy]

I've discovered a new class of drugs, the cyclopentyls. And with this chem that shows more serotonergic Activity than dopaminergic, and that has some dissociative perks aswell along MAO A & B, i think there is a GREAT potential for antidepressiva and use.

The stp link:http://www.swisstargetprediction.ch/result.php?job=485497299&organism=Homo_sapiens

@clubcard what do you think?

Substitutions on the phenyl seem to work differently from the arylcyclos and there's no possibility for a ketone, at least according to stp it isn't any good. The N-Methyl and N-Isopropyl and N-Piperidine have been tested, the N-Pyrrolidine showing best results.

N-Piperidine 3-MeO

 

[clubcard]

I think you will find that the angle and position of the amine relative to the aromatic is vital for NMDA affinity in this class of antagonist. If it overlays or NEARLY overlays dizocipine then OK, but dizocipine was the result of a concerted effort to find the exact relationship. 8A-PDHQ (I forget which isomer is active) is interesting. Not only is it more rigid then the phenylcycloalkylamines it is derived from but it's LogP is also improved. I am not aware of anyone substituting the aromatic ring of either of those 2 but I put a note up on the unusual step that Parke Davis made in patenting a single compound - the 2-Cl 5-MeO homologue of ketamine. Patents are not cheap, so I can only conclude that at the time, their research team considered it worth the money.
A lot of patent mining has made me conclude that patenting a single drug candidate is unusual. Usually their are at least a FEW analogues to cover. I would love to have been a fly on the wall....

 

[Gaffy]

I actually think it's the metabolite that plays an active role in its antidepressive effects

 

[allone]

how does one acquire such