AP-3 (propionate homolog of AP-4)

[Limpet_Chicken]

What is the SAR requirement for NMDA antagonist activity of the 2-amino-terminal phosphoncarboxylic acid series, and would it be potentially worth a shot as a dissociative?

Others in the series are AP-4 (2-amino-4-phosphonobutanoic acid), AP-5, the pentanoic acid homolog, and AP-7 the heptanoic acid derivative.

Is the 3-carbon chain homolog active? worth tasting?

 

[Limpet_Chicken]

http://www.chinaphar.com/1671-4083/22/556.pdf

Second thoughts, those figures on brain Ca2+ content and reports of the L-isomer causing cerebral oedema (mind you via localised microinjection) I don't think it sounds too pleasant.

 

[nuke]

Yeah, cerebral edema and vasospasm are the big problems with a lot of NMDA antagonists (especially the phenylcyclohexane derivatives).

As F&B's bioassays of substituted phenylcyclohexane derivatives has revealed as well, some of these NMDA antagonists appear to cause extreme hypertension/tachycardia in large doses too (but maybe that's acting more as an NDRI than anything else). But in combination, those things are basically really bad, so one has to watch out for them if they're trying to come up with exciting new dissociative antidepressants.

 

[atara]

It'd be nice if we could just make xenon somehow. Alas.

 

[Limpet_Chicken]

MAKE it? not without a cyclotron.

But its available as a speciality gas, just horrendously expensive.

AFAIK xenon acts on other targets too, ion channels and as an AMPA antagonist.

Nuke, is the hideous neurotoxicity with some of these drugs dose dependent? the oedema sure seemed to be, but that still leaves me a bazillion miles away from wanting to actually bioassay the stuff.