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Anybody knows is diphenidine/MXP/ephenidine a ligand for non-NMDA receptors?

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Renald

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Jul 8, 2015
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I have not found any information regarding these compounds, to they act on non-NMDA receptors in "therapeutic" (recreational) dosages? Anybody knows binding profiles of these compounds? SERT/NET/DAT/opioid/histamine/Ach etc?
 
I don't think much has appeared in the literature regarding their off-target effects. I believe a comprehensive screening has been performed but it remains unpublished.
 
Pretty much all dissociatives are also monoamine reuptake inhibitors, I'd be very surprised if that's not the case with the diphenylethylamines.
 
At least diphenidine and MXP are heavily stimulating. It was too much of a disturbing cold-ish push for me, so that I gave them up after a few attempts.
I guess either prominent noradrenergic activity and/or strong glutamate rebound. The only time I've tried ephenidine (although this was by far no safe use that time) it had a strong, but brief antidepressant-like afterglow.

Maybe I'll try ephenidine again one day as it seems to be the less harsh one of them, but they scare me somewhat now.. Ketamine and MXE are much more mellow (and I've thought of MXE to be disturbingly manic in higher doses before.. but it's nothing compared to the diphenidines.)

Also all of them contain a phenethylamine part (ephenidine -> ethylamphetamine) - but this is in laymen's terms and probably says next to nothing.
 
Diphenidine overlays DXM & MK-801 (being flexible). Sadly, it's not very soluble in the form of the hydrochloride (sulfate you can snort) but the truth is that easily the best analogue does away with the nitrogen being on a ring. N-isopropyl gives an almost perfect imitation of K... but apparently it was too difficult to make in bulk...
 
DXM/DXO are quite strong NRIs, and for MK-801 which is said to be dysphoric, that would fit too..
 
I don't think you can relate the dysphoric effects of dizocilpine to NRI properties so easily. It hasn't been tested in humans to my knowledge, so I guess it might have only been found not to be self-administered but it's not synonymous with dysphoric for sure. Kappa agonists are described as dysphoric and I guess some of them might actually turn out to be quite interesting if they have enough mu activity. I somehow have some doubts whether dissociation alone is the desired effect of dissociatives like ketamine for instance, dissociatives can differ one from another quite a lot, some are more sought-after and some are less, I guess it's governed by a different action without which plain dissociation is a rather unpleasant experience.

DXM and DXO could have a direct effect on different 5-HT and adrenergic receptors too, secondary to their main actions, but possibly adding to the side effects. As for me the main unpleasant aspect of DXM experience was always nausea and I felt that all the other unpleasant effects like anxiety were strongly related to feeling sick and vomiting but I never found it to be particularly dysphoric for my mind, quite the opposite actually, if it wasn't for the physical side effects, I'd certainly find DXM to be the best dissociative out there. On the other hand on ephenidine I felt a weird inner uneasiness and there weren't enough positive effects to compensate for that (but it's worth noting that I was still on benzodiazepines then which made my experiences with dissociatives quite unpredictable).

Anyway, given their structure diphenidine and its relatives are likely to interact with monoamine transporters to some extent.
 
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