06-22-2018, 03:38 PM
(This post was last modified: 06-22-2018, 03:39 PM by thepianist.)
Very interesting stuff for sure. It doesn't seem the US is as interested in this research as perhaps Asian countries are based on my knowledge of gov funding (though I don't work in psychiatric disorders).
Based on the limited information that I've gathered, I remember seeing some experimental results that showed a down-regulation of certain GABA receptors, despite having activity at others. A molecule that binds MORE selectively to certain GABA sites and not others? Sounds very plausible? Of course (considering the number of benzos already known and studied).
The main problem that researchers working on benzodiazepines faced (I know some old timers that worked in that area back when it was 'hot') and had to sort of accept was: even though certain benzos (like bromaz, clonaz, triaz, loraz, etc) have shown higher specificity at certain gaba receptors, ALL of the gaba receptors WILL 'get a taste' so to speak of any benzo taken. Scientists have found which GABA receptors are responsible for anxiolysis, those for muscle relaxation, those responsible for the amnesic side effects. Problem is, medicines with that kind of specificity for the gaba receptors aren't known, yet. Maybe the answer is in this thioneodiazepine class.
Being an optimist, I'd say even preliminary results that show what appears to be complete specificity for certain GABA receptors is reason enough to fund more research. I'm sure it's already being conducted somewhere.
I know my old scientist friends would get a kick if thienodiazepines replaced benzos to become a solution to the drowsy/amnesic side effects.
Based on the limited information that I've gathered, I remember seeing some experimental results that showed a down-regulation of certain GABA receptors, despite having activity at others. A molecule that binds MORE selectively to certain GABA sites and not others? Sounds very plausible? Of course (considering the number of benzos already known and studied).
The main problem that researchers working on benzodiazepines faced (I know some old timers that worked in that area back when it was 'hot') and had to sort of accept was: even though certain benzos (like bromaz, clonaz, triaz, loraz, etc) have shown higher specificity at certain gaba receptors, ALL of the gaba receptors WILL 'get a taste' so to speak of any benzo taken. Scientists have found which GABA receptors are responsible for anxiolysis, those for muscle relaxation, those responsible for the amnesic side effects. Problem is, medicines with that kind of specificity for the gaba receptors aren't known, yet. Maybe the answer is in this thioneodiazepine class.
Being an optimist, I'd say even preliminary results that show what appears to be complete specificity for certain GABA receptors is reason enough to fund more research. I'm sure it's already being conducted somewhere.
I know my old scientist friends would get a kick if thienodiazepines replaced benzos to become a solution to the drowsy/amnesic side effects.

