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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 7 of 7. This is the beginning of the thread.
Posted by jaybee9 on September 5, 2007, at 15:04:08
HiI suffer from dysthymia and social anxiety, i've been taking tianeptine but with little success. From reading previous posts and after feeling much better on tyrosine and gaba powder i'm convinced that my gaba and Dopamine levels need to be targeted. But i'm having trouble finding meds that can boost these neurotransmitters without major side effects. Does anybody have any suggestions?
Thanks in advance
Posted by twinch42085 on September 5, 2007, at 17:43:00
In reply to Need some advise on boosting GABA and Dopamine, posted by jaybee9 on September 5, 2007, at 15:04:08
I need a dopamine/serotonin booster. I am taking 4 mg of risperdal and risperdal is a very strong dopamine blocker. I feel like I don't have any dopamine left. I don't know of any boosters.
Posted by Phillipa on September 5, 2007, at 23:55:49
In reply to Re: Need some advise on boosting GABA and Dopamine » jaybee9, posted by twinch42085 on September 5, 2007, at 17:43:00
I may be off base but it seems that the antiparkinson'e meds increase dopamine. See Dopamines thread below for full descriptions of two of the meds Phillipa
Posted by Phillipa on September 6, 2007, at 0:01:10
In reply to Re: Need some advise on boosting GABA and Dopamine, posted by Phillipa on September 5, 2007, at 23:55:49
Gaba from wikipedia Phillipa
GABAA receptor
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The correct title of this article is GABAA receptor. It features superscript or subscript characters that are substituted or omitted because of technical limitations.
The GABAA receptor is one of two ligand-gated ion channels responsible for mediating the effects of Gamma-Amino Butyric Acid (GABA), the major inhibitory neurotransmitter in the brain. The GABAA receptor is also the molecular target of the benzodiazepine class of tranquilizer drugs, and hence it is also often referred to as the benzodiazepine receptor. In addition to the GABA and benzodiazepine binding sites, the GABAA receptor complex appears to have distinct binding sites for furosemide, neuroactive steroids, picrotoxin, barbiturates, ethanol, kavalactones, GHB, and inhalation anesthetics[1]Contents [hide]
1 Structure and function
1.1 Subunits
2 Agonists, antagonists, and inverse agonists
2.1 Agonists
2.2 Antagonists
2.3 Inverse agonists
2.4 Subtype selective ligands
3 See also
4 References
5 External links
[edit] Structure and function
The receptor is a multimeric transmembrane receptor that consists of five subunits arranged around a central pore. The receptor sits in the membrane of its neuron at a synapse. The ligand GABA is the endogenous compound that causes this receptor to open; once bound to GABA, the protein receptor changes conformation within the membrane, opening the pore in order to allow chloride ions (Cl-) to pass down an electrochemical gradient. Because the reversal potential for chloride in most neurons is close to or more negative than the resting membrane potential, activation of GABAA receptors tends to stabilize the resting potential, and can make it more difficult for excitatory neurotransmitters to depolarize the neuron and generate an action potential. The net effect is typically inhibitory, reducing the activity of the neuron. The GABAA channel opens quickly and thus contributes to the early part of the inhibitory post-synaptic potential (IPSP).[2][3]
[edit] Subunits
GABAA receptors are members of the large "Cys-loop" super-family of evolutionarily related and structurally similar ligand-gated ion channels that also includes nicotinic acetylcholine receptors, glycine receptors, and the 5HT3 receptor. There are numerous subunit isoforms for the GABAA receptor, which determine the receptor’s agonist affinity, chance of opening, conductance, and other properties.[4]In humans, the units are as follows:[5]
six types of α subunits (GABRA1, GABRA2, GABRA3, GABRA4, GABRA5, GABRA6)
three β's (GABRB1, GABRB2, GABRB3)
three γ's (GABRG1, GABRG2, GABRG3)
as well as a δ (GABRD), an ε (GABRE), a π (GABRP), and a θ (GABRQ)
There are three ρ units (GABRR1, GABRR2, GABRR3), however these do not coassemble with the classical GABAA units listed above,[6] but rather homooligomerize to form GABAC receptors.Five subunits can combine in different ways to form GABAA channels, but the most common type in the brain is a pentamer comprising two α's, two β's, and a γ (α2β2γ).[5]
The receptor binds two GABA molecules,[7] at the interface between an α and a β subunit.[5]
[edit] Agonists, antagonists, and inverse agonists
Other ligands (besides GABA) interact with the GABAA receptor to increase chloride conductance (agonists), decrease conductance (inverse agonists) or to bind to the receptor and have no effect other than to prevent the binding of agonists or inverse agonists (antagonists). Hence ligands for the GABAA receptor span a range of effects from full agonism to antagonism to inverse agonism.
[edit] Agonists
Full agonists display a large number of effects including anti-anxiety (anxiolytic), muscle relaxant, sedation, anti-convulsion, and at high enough doses, anesthesia. Partial agonists may display a subset of these properties (for example anxiolytic without sedation).Such other agonist ligands include
benzodiazepines (increase pore opening frequency; often the active ingredient of sleep pills and anxiety medications)
imidazopyridines (newer class of sleep medications)
barbiturates (increase pore opening duration; used as sedatives)
kavalactones (psychoactive compunds found in the roots of the kava plant)[8]
certain steroids, called neuroactive steroids[9] [10] [11] [12] [13] [14] [15] [16] [17] [18]
Muscimol is an agonist used to distinguish GABAA from the GABAB receptor.
[edit] Antagonists
Among antagonists arepicrotoxin (non-competitive; binds the channel pore, effectively blocking any ions from moving through it)
bicuculline (competitive; transiently occupies the GABA binding site, thus preventing GABA from activating the receptor)
The antagonist flumazenil is used medically to reverse the effects of the benzodiazepines.
[edit] Inverse agonists
Full inverse agonists have convulsive properties while partial inverse agonists may be useful as aids in memory and learning. An example of a partial inverse agonist is Ro15-4513.
[edit] Subtype selective ligands
A useful property of the many benzodiazepine receptor ligands is that they may display selective binding to particular subsets of receptors comprising specific subunits. This allows one to determine which GABAA receptor subunit combinations are prevalent in particular brain areas and provides a clue as to which subunit combinations may be responsible for behavioral effects of drugs acting at GABAA receptors. These selective ligands may have pharmacological advantages in that they may allow dissociation of desired therapeutic affects from undesirable side effects.
Posted by Jedi on September 6, 2007, at 1:02:28
In reply to Need some advise on boosting GABA and Dopamine, posted by jaybee9 on September 5, 2007, at 15:04:08
Hi Jaybee9,
I take Nardil and clonazepam. Nardil boosts all of the major neurotransmitters, but not without side effects. Clonazepam will boost GABA and may be enough for some people with social anxiety symptoms. I have treatment resistant double depression-atypical with social anxiety. I've had at least four or five bouts of major depression and have suffered with dysthymia since my teenage years. I am now fifty. If the depression and anxiety is bad enough, you can put up with the Nardil side effects. As far as I'm concerned, there is nothing much worse than treatment resistant depression. If your depression is really mild, maybe a stimulant such as modafinil(Provigil) or methylphenidate would boost your dopamine.
Be Well,
Jedi> Hi
>
> I suffer from dysthymia and social anxiety, i've been taking tianeptine but with little success. From reading previous posts and after feeling much better on tyrosine and gaba powder i'm convinced that my gaba and Dopamine levels need to be targeted. But i'm having trouble finding meds that can boost these neurotransmitters without major side effects. Does anybody have any suggestions?
>
> Thanks in advance
>
>
Posted by FredPotter on September 6, 2007, at 15:25:10
In reply to Need some advise on boosting GABA and Dopamine, posted by jaybee9 on September 5, 2007, at 15:04:08
I'm not sure how you know you have a problem with GABA and dopamine, but bupropion is a dopamine agonist while your GABA can be stimulated with a benzo. I take Nardil which does both and other things too, but as Jedi says, at a price
Posted by jaybee9 on September 7, 2007, at 2:34:02
In reply to Re: Need some advise on boosting GABA and Dopamine » jaybee9, posted by FredPotter on September 6, 2007, at 15:25:10
The reason I think I have a problem with my Gaba is because of the feelings of anxiety which are slightly elieved when I take gaba powder or picamillon. I've also tried high doses of tyrosine which works on dopamine levels but poops out quite quickly. Lots of posts on this board also point to gaba and dopamine when the problem is dystymia and social anxiety.
This is the end of the thread.
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