Dr. Scott Sherr
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So GABA-A receptors have chloride channels that chloride goes in. It hyperpolarizes the membrane there that the receptor is in. And as a result of that, the neuron that's on what's called the postsynaptic side stops firing. So that's why it's called an inhibitory neurotransmitter because when GABA binds to its site, it opens up the receptor.
So GABA-A receptors have chloride channels that chloride goes in. It hyperpolarizes the membrane there that the receptor is in. And as a result of that, the neuron that's on what's called the postsynaptic side stops firing. So that's why it's called an inhibitory neurotransmitter because when GABA binds to its site, it opens up the receptor.
So GABA-A receptors have chloride channels that chloride goes in. It hyperpolarizes the membrane there that the receptor is in. And as a result of that, the neuron that's on what's called the postsynaptic side stops firing. So that's why it's called an inhibitory neurotransmitter because when GABA binds to its site, it opens up the receptor.
It prevents the firing of the neuron on that postsynaptic side. So most of the drugs that we know of affect the GABA receptor, the GABA-A receptor, and most of the drugs don't bind to where GABA binds, but they bind on what are these called, these allosteric sites, these sites around on those subunits that either enhance the affinity for GABA to bind or decrease the affinity for GABA to bind.
It prevents the firing of the neuron on that postsynaptic side. So most of the drugs that we know of affect the GABA receptor, the GABA-A receptor, and most of the drugs don't bind to where GABA binds, but they bind on what are these called, these allosteric sites, these sites around on those subunits that either enhance the affinity for GABA to bind or decrease the affinity for GABA to bind.
It prevents the firing of the neuron on that postsynaptic side. So most of the drugs that we know of affect the GABA receptor, the GABA-A receptor, and most of the drugs don't bind to where GABA binds, but they bind on what are these called, these allosteric sites, these sites around on those subunits that either enhance the affinity for GABA to bind or decrease the affinity for GABA to bind.
The most common one that all of us know about that we have on a regular basis across the United States and the world is alcohol. Alcohol binds to an allosteric site on the GABA-A receptor, increasing the affinity for GABA to bind, increasing the chloride going in, and inhibiting that neurotransmitter, inhibiting that neuron from firing. There's lots of other ones that we can talk about.
The most common one that all of us know about that we have on a regular basis across the United States and the world is alcohol. Alcohol binds to an allosteric site on the GABA-A receptor, increasing the affinity for GABA to bind, increasing the chloride going in, and inhibiting that neurotransmitter, inhibiting that neuron from firing. There's lots of other ones that we can talk about.
The most common one that all of us know about that we have on a regular basis across the United States and the world is alcohol. Alcohol binds to an allosteric site on the GABA-A receptor, increasing the affinity for GABA to bind, increasing the chloride going in, and inhibiting that neurotransmitter, inhibiting that neuron from firing. There's lots of other ones that we can talk about.
There's lots of drugs. There's lots of natural plants that do it as well. But we can talk about, I think, that in a little bit. When it comes down to the GABA-B receptor, GABA-B is a little bit different. GABA-B is called a G protein couple receptor. And it just basically means it has something on the presynaptic side and the postsynaptic side that are working together.
There's lots of drugs. There's lots of natural plants that do it as well. But we can talk about, I think, that in a little bit. When it comes down to the GABA-B receptor, GABA-B is a little bit different. GABA-B is called a G protein couple receptor. And it just basically means it has something on the presynaptic side and the postsynaptic side that are working together.
There's lots of drugs. There's lots of natural plants that do it as well. But we can talk about, I think, that in a little bit. When it comes down to the GABA-B receptor, GABA-B is a little bit different. GABA-B is called a G protein couple receptor. And it just basically means it has something on the presynaptic side and the postsynaptic side that are working together.
Calcium, potassium, those are the electrolytes that are going on there. And that basically has the capacity to decrease the firing of that postsynaptic neuron as well. So the major drug that works on the GABA-B receptor that most people know of is baclofen. which is an antispasmodic drug. So it works mainly in the spinal cord actually to decrease spasm of muscles.
Calcium, potassium, those are the electrolytes that are going on there. And that basically has the capacity to decrease the firing of that postsynaptic neuron as well. So the major drug that works on the GABA-B receptor that most people know of is baclofen. which is an antispasmodic drug. So it works mainly in the spinal cord actually to decrease spasm of muscles.
Calcium, potassium, those are the electrolytes that are going on there. And that basically has the capacity to decrease the firing of that postsynaptic neuron as well. So the major drug that works on the GABA-B receptor that most people know of is baclofen. which is an antispasmodic drug. So it works mainly in the spinal cord actually to decrease spasm of muscles.
And the other drug that's very commonly used or not very commonly used, but very commonly known as the date rate drug is GHB or gamma hydroxybutyric acid, which is GHB. And this is a, it's known as a date right drug, but it's actually a really great drug used for spasm, used for narcolepsy, used for sleep as well. And so it's got some medical benefit.
And the other drug that's very commonly used or not very commonly used, but very commonly known as the date rate drug is GHB or gamma hydroxybutyric acid, which is GHB. And this is a, it's known as a date right drug, but it's actually a really great drug used for spasm, used for narcolepsy, used for sleep as well. And so it's got some medical benefit.
And the other drug that's very commonly used or not very commonly used, but very commonly known as the date rate drug is GHB or gamma hydroxybutyric acid, which is GHB. And this is a, it's known as a date right drug, but it's actually a really great drug used for spasm, used for narcolepsy, used for sleep as well. And so it's got some medical benefit.
So you have your GABA-A receptor and you have your GABA-B receptor. And the GABA-A has all these subunits that other kinds of compounds can bind to that help the GABA itself bind to its site on the receptor. And then you have the GABA-B receptor as well, which is this G protein coupler receptor a little bit different.
So you have your GABA-A receptor and you have your GABA-B receptor. And the GABA-A has all these subunits that other kinds of compounds can bind to that help the GABA itself bind to its site on the receptor. And then you have the GABA-B receptor as well, which is this G protein coupler receptor a little bit different.