Phenibut a gabapentinoid

[Solipsis]

Phenibut as a gabapentinoid

"R-phenibut binds to the α2–δ subunit of voltage-dependent calcium channels and exerts gabapentin-like anti-nociceptive effects". Pharmacology Biochemistry and Behavior 137: 23–29. doi:10.1016/j.pbb.2015.07.014. ISSN 0091-3057. PMID 26234470

wtf Is it true that the affinity it has for VDCCs makes gabapentinoid activity of phenibut more salient than any GABA_B agonism ?

 

[belligerent drunk]

It appears to be so. I think racemate has like 4 fold higher affinity for VDCC than for GABAB - both S- and R-phenibut have similar affinities at VDCC whereas only R-phenibut has any GABAB affinity. But I wouldn't say that this makes its GABAB agonism insignificant. Subjectively, it still has typical GABAergic properties.

 

[dopamimetic]

Yeah, seems to be the case. I've always been quite cautious with phenibut because of the withdrawal stories but do now think a bit different - these people who acquire it off the net nearly always go cold turkey at some point when they run out etc. off crazy high dosages without knowing much about the pharmacology and all. If you do that with pregabalin, you'll end up in severe withdrawal too.

Phenibut appears to be somewhat like pregabalin with minor GABA-B and dopamine agonism...

 

[belligerent drunk]

^ doesn't it have PEA antagonism instead?