How do GABAnergics differ in their mechanism of action.

[Hammilton]

You're kind of stupid huh, a poor mimic of the original mad scientist.

I mean that post is beyond retarded.

The GABA-A receptor consists of two alpha subunits, two beta subunits, and one gamma subunit.

benzodiazepines don't target the alpha subunit any more than they target the gamma subunit. The binding site consists of amino acids from both subunits.

Barbituates (ketamines) bind the beta subunit increasing the duration of channel opnenings

This part is the absolutely hilarious. Ketamine and barbs have nothing in common. LOL. Barbs are not "ketamines." christ, any retard who read wikipedia's entry on the GABA-A receptor would know more than you apparently.

You've basically just said everything that has already been said, but in a much shittier manner.

I hope this is just an attempt to reach your post count to get rid of the greenlighter tag, because this garbage would be weak for OD, or even the defunct TOTSE.

 

[acetylcholine]

To get back to original question. Different types of GABAergics act on different GABA receptors throughout the body. GABAa and GABAb are obvious examples.

But pertaining specifically to GABA A, different cells and tissues contain GABA A receptors composed of varied kinds of subunits. One composition often seen is 2(a1), 2(b2), 1(gamma2).

benzodiazepines don't target the alpha subunit any more than they target the gamma subunit. The binding site consists of amino acids from both subunits.

However, some benzos bind better than others depending on the amino acids that make up the binding sites between the subunits. The Alpha subunit is one that is often mentioned. Their affinity to different subunit areas is largely what gives benzo-site binding ligands their variable effects and "feel". For example Zolpidem has greater affinity for receptors with a1 subunits.

Here's a quote from the abstract of Compartmentation of alpha 1 and alpha 2 GABA(A) receptor subunits within rat extended amygdala: implications for benzodiazepine action. that should be helpful to understanding the variable distribution and effect of GABA receptors.

The binding properties and action of benzodiazepines depend on the alpha-subunit profile of the hetero-pentameric receptors: whereas the alpha1 subunit is associated with benzodiazepine type I pharmacology and reportedly mediates sedative as well as amnesic actions of benzodiazepines, the alpha2 subunit confers benzodiazepine type II pharmacology and mediates the anxiolytic actions of benzodiazepines...

...A moderate expression of the alpha1 subunit could be detected in compartments of the medial subdivision and a strong expression of the alpha2 subunit throughout the central subdivision. It is concluded that the alpha1 and alpha2 subunits are differentially expressed within the extended amygdala, indicating that this structure is compartmentalized with respect to function and benzodiazepine action.

One more thing...

I've been away from this site for a while, but stumbled on this post while attempting to find out more about quaalude binding.

Hammilton, I see you are in your usual unapologetic form, but your condescension and ego really bothers me here. What's the point of insulting people and nitpicking words? I notice that in this thread you seem to spend more time mocking others' posts than you do answering questions or actually explaining the details.

Why is this allowed to go on?

BTW, I believe subunit and subtype are sometimes used interchangeably.

 

[Hammilton]

Hammilton, I see you are in your usual unapologetic form, but your condescension and ego really bothers me here. What's the point of insulting people and nitpicking words? I notice that in this thread you seem to spend more time mocking others' posts than you do answering questions or actually explaining the details.

somethings are just so hilariously retarded that I just can't help myself. As it happens in this thread. Had you paid any attention, you'd have seen this poster posting tons of this same sort of bullshit over a few days, without any apparent attempt at making intelligent posts. You could try to make me feel bad for being an ass to someone who is trying (I'm not going to care then) but someone just posting nonsense for the sake of posting nonsense won't get even a twinge of guilt

Why is this allowed to go on?

obviously I'm so clearly awesome that there's no point in trying to smudge the awesome off. Seriously though, the real question should be why such stupidity is allowed here. This isn't TOTSE

BTW, I believe subunit and subtype are sometimes used interchangeably.

By who? There's a big and important difference between the terms, this isn't nitpicking. Subunits are bits of protein. GABA-A and GABA-B are both subtypes of the GABA receptor, but there's fuck all similarity between them. That GABA binds is about where it ends. You could say that GABA-A a1y2b1 and GABA-A a2y2b1 are both subtypes of GABA-A, too, but here it gets ridiculously complicated with perhaps hundreds of possibilities (though what's actually expressed is much more limited, and what's expressed often even more so). Subunits make up Subtypes (at least within Cys-loop LGIC's)

silly

 

[ShaolinBomber]

Did anyone inform the OP that it is GABAergic and not GABAnergic yet?

just wondering.

 

[negrogesic]

GABA (gamma hydroxybutyric acid)
Has
an alpha, a beta and a gamma subunit they are all in the same protein complex.
Alcohol and benzodiazapines target teh alpha subunit causing an increase in frequency of channel openings
Barbituates (ketamines) bind the beta subunit increasing the duration of channel opnenings

Don't post here if you don't know what you are talking about...

 

[acetylcholine]

you'd have seen this poster posting tons of this same sort of bullshit over a few days

You're right about that. Anyone who throws around the term "4-HT receptor" should expect a backlash.

obviously I'm so clearly awesome that there's no point in trying to smudge the awesome off. Seriously though, the real question should be why such stupidity is allowed here.

I too am frustrated by users who consider themselves internet biochem phd's and post wrong and potentially harmful information. Most boards I visit are kind of "soft" when it comes to allowing members to chastise others for misinformation. These boards prefer the "you are wrong. period. this is right." approach. BUT, your style has given me some laughs so I guess all's the better.:D

By who? There's a big and important difference between the terms, this isn't nitpicking. Subunits are bits of protein. GABA-A and GABA-B are both subtypes of the GABA receptor, but there's fuck all similarity between them. That GABA binds is about where it ends. You could say that GABA-A a1y2b1 and GABA-A a2y2b1 are both subtypes of GABA-A, too, but here it gets ridiculously complicated with perhaps hundreds of possibilities (though what's actually expressed is much more limited, and what's expressed often even more so). Subunits make up Subtypes (at least within Cys-loop LGIC's)

When writing that, I could have sworn I read the two used interchangeably in some reputable source, but searching now, I can't find this usage at all. I have found usage of "subtype" in the "specific collection of kinds of subunits" sense, but this is not the way that poster was using it. So you are right!