• N&PD Moderators: Skorpio | thegreenhand

  • Neuroscience & Pharmacology Discussion Welcome Guest
    Posting Rules Bluelight Rules
    Recent Journal Articles Chemistry Mega-Thread
    FREE Chemistry Databases! Self-Education Guide

GHB analogue.

There's nothing magical about partial agonists. IA is hardly the end all be all of adverse effects and tolerance development. In fact, in many cases the distinction between a full agonist and partial agonist is often arbitrary, or at best relative to other drugs in its class. There are a slue of other factors involved.
 
well for GABA B phenibut is a full agonist and its truly a disaster relative to partial agonists in many ways
 
HOCPCA DEFINITELY sounds like one to avoid like the plague. Its a potent GHB receptor agonist, which means it will act as a strong glutamate receptor agonist. Also, isn't it selective for GHB receptors? that would also remove any protection provided against excitotoxicity by the GABAb agonist effect of GHB.

Also, aren't low doses of GHB more neurotoxic than higher doses, because of its having far higher affinity/efficacy at GHB receptors compared to GABAbRs?
 
I don't think there are such things as GABAB partial agonists... GS-39783 is a positive allosteric modulator (a la barbiturates/benzodiazepines @ GABAA), so is CGP-7930, they aren't partial agonists unfortunately.

Presumably some analog of baclofen may be a partial agonist, it's where I would start for sure in a screening effort. Too far into alkyl groups on the B position of GABA and you get calcium channel affinity (gabapentin, pregabalin, etc) and decreased BA at L-type amino acid transporter. Even phenibut has some affinity for Ca2+ channels compared to baclofen.

Just because something is a GHB agonist doesn't make it a glutamate agonist too, BTW. Although excessive GHBR agonism can cause seizures and the like.
 
I did not mean to imply that a GHBr agonist means that a compound of such nature is a direct agonist at either ionotropic or metabotropic GLuRs, but rather, that GHB receptor agonists are glutamate secretagogues.
 
You must log in or register to reply here.
Top