MT-45 mu/NMDA?

[borohydride]

I recently read a Short Communication from 1970 in which the activity of each of the MT-45 isomers was tested. The article is called:

ANALGESIC ACTIVITY AND OPIATE RECEPTOR BINDING OF 1-CYCLOHEXYL-4-(1,2-DIPHENYLETHYL)PIPERAZINE by Fujimura, Tsurumi, Nozaki, Hori & Imai.

What was interesting was that the (S) isomer has over 10 times the mu binding of the (R) (0.14 vs 1.18). When the enantiopure drugs were tested, the (S) isomer was x7 more potent than the (R) as an analgesic (4.4 vs 30mg/Kg).

The odd thing was that in the same analgesic test, the racemate had an ED50 of 1.7, almost 3 times the potency of the (S) isomer.

Looking at their structures, does anyone else think this compound has decent NMDA activity?

I sure hope so because the list of mu/NMDA reads like a list of whose who!

Ketobemidone
Dipipanone (methadone also has a little, but nowhere near Diconal
Levorphanol

I think most people would be happy with any of that bunch"



I just wish someone would get on with the -MeO phenyl analogue which is x2 the potency and regarded as utter bliss...

[borohydride]

Now I've tried it - it sucks!

That's the truth of drug-design; you cannot predict euphoria (even DRI doesn't do that, some DRIs are nasty - mainly slow onset/long duration).

[Benz]

You can't win them all. Good to see you back posting Boro. Benz