Drugs which interact with the glycine receptor

[FrogWarrior]

Glycine receptors are ligand gated chloride channels, thus they cause sedating effects when activated. Strychnine is a potent glycine receptor antagonist which causes death by seizures and convulsions. Similarly, chloride channel blockers like picrotoxin and bicuculine block glycine Cl channels in the same way they do GABA_a chloride channels. I'm guessing potent agonists would have strong sedating effects similar to anasthetics like halothane. The wiki page:
https://en.wikipedia.org/wiki/Glycine_receptor#Agonists
lists a few agonists. Heres a glycine prodrug:
https://en.wikipedia.org/wiki/Milacemide
I don't know whether they abandoned research because it was ineffective at binding to glycine receptors, or just ineffective at treating Alzheimers. Either way I doubt the drug is available. Taurine in my experience has no sedative effects at all, so I'm guessing it has very low affinity for glycine reeptors, and/or bad bioavailability. Surely they have developed some selective, potent glycine receptor agonists. They would be a good research tool as well as a possible lead for a new class of anasthetics/sedatives. Anyone here know anything about this?

 

[mad_scientist]

You might be better off looking for inhibitors of the glycine reuptake transporter (i.e. increasing glycine signaling indirectly). Compounds like LY-2365109 and Org 25543 seem to have some quite significant effects in animals, while all the directly acting glycine agonists are quite weak. Don't look that safe though...

 

[lenses]

Noopept!