bindingaffinity
Bluelighter
- Joined
- Apr 19, 2012
- Messages
- 150
Ok folks, so lately I've been trying to learn more about GABA-A receptors and their pharmacology. From what I've read, it seems like there are at least 4 main binding sites:
There are a number of other questions I have about other GABA-A ligands, such as:
- binding site of GABA itself, also targeted by muscimol and gaboxadol
- barbiturate/picrotoxin binding site
- benzodiazepine/flumazenil/DBI binding site
- etomidate (& analogues)/methaqualone (& analogues)/loreclezole binding site
There are a number of other questions I have about other GABA-A ligands, such as:
- which binding site is targeted by ethanol and other alcohols? (e.g., trichloroethanol, ethchlorvynol, chloroform, 2M2B...)
- do subtype-specific GABA-A ligands such as zolpidem bind to a different site than benzodiazepines? or does the affinity of ligands for that site vary widely based on the subtypes of the given receptor?
- how (if at all) do GABA analogues such as pregabalin, gabapentin, and valproic acid interact with GABA receptors?
- have the atypical psychedelic/deliriant actions of muscimol been pharmacologically explained? how about zolpidem?
- in the doses used in ayahuasca and changa, do beta-carboline alkaloids manifest any effects caused by GABA-A interaction, or are they acting solely as MAO inhibitors?