GABA Receptor( BZD) – Structure and Mechanism of Action
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GABA Receptor( BZD) – Structure and Mechanism of Action


alright now in this video we will study the
gaba receptor now gaba receptor is of two types
first is the gaba a and gaba b receptor gaba a is a type of ionotropic receptor and
gaba b is a type of metabotropic receptor or g protien coupled receptor
but in this video we will only focus on the gaba a receptor akright
now first of lets see the structure of the gaba a receptor
i will try to make two views the first is the front view and second is
the top view of the receptor coming to the front view
now the gaba a receptor is a type of pentameric it consiss of five subunits which are arranged
partly extracellularly and partly intracellularly and the five subunits are
two alpha subunits two beta subunits and one gama unit arranged
around a central pore now lets look at the receptor from the top
view consists of the central chloride pore
and two drug binding sites mainly it consists of three drug binding sites
but for the purpose of illustration i have just drawn two
the first is the benzodiazipne binding site and second is the gaba binding site ok now two alpha subunits two beta subunits
and one gama subunit now between the aplha and the beta subunit
is the gaba binding site same as here on the front view and same on
the top view and between the the alpha and the gama subunit is the benzodiazipine binding
site or the bzd allostearic site now the next important thing i would discuss
is the mechanism of action of this gaba receptor now the basic step involved in the activation
of the gaba receptor is binding of a ligand or drug to the gaba site or the benzodiazipine
binding site. now due to this binding the central chloride
pore opens up and causes influx of chloride ions which further causes inhibition of neuron
by creating a state of hyperpolarisation in the neuron
now lets look at the some of the drugs which act on the gaba receptor
first of all i would like to discuss the gama amino buyric acid or the gaba.now this drug
or it is a basically an endogenous agonist of the gaba receptor
it is released at various sites in the cns and it acts on the gaba site and causes the
same sequence of events we have just discussed now the second class of drugs that we will
discuss are grouped under as positive allostearic modulators
now these drugs bind to the benzodiazipine bindind site and cause the same chain of events
now in this category first of all we have the benzodiazipnes
the diazepam clonezepam these just act on the benzodiazipine binding site they are the
positive allostearic modulators now second class of drugs are the barbiturates
the thiopental and the third class of important drugs are
the muscle relaxants like thiocolchicaside also alcohol acts on this site
and then we have some anaesthtic drugs like propofol and etomidate
there are some other drugs but they are not that important as these classes
third important category of drugs are negative allostearic modulators
now there are a whole bunch of drugs which act as negative allostearic modulators but
the one i would like you to remember is flumezanil now this very important drug
it blocks the benzodiazipine binding site or you can say that it is a negative allostearic
modulator of the benzodiazipine binding site now this drug is given in benzo benzodiazipine
overdose and also it is given in the reversal of anaesthesia
now lets look at the affects of activation of the gaba recptor
now the various drugs which act on this receptor produce numerous affects some of which are
anxiolysis anticonvulsant affect
the sedative affect partial amnesia
and muscle relaxation so this was a short review of the gaba receptors
functions and structure i hope you like the video
if you find the video informative please make sure to hit the like button and
subscribe to my channel also i will make a 3d model of the gaba receptor
soon so make sure to subscribe to my channel
to get an update on that video thank u so much guys for watching

79 Comments

  • Justin Chu

    After reading this in Tripathi 4 times over I decided I had enough. Then I stumbled across this video and my, I learned so much! Thank you so much for your work! keep it up!

  • Pen1980IM

    I was on 3mg of Ativan daily for 5 years and switched over to 2mg of klonopin without tapering off the Ativan. I just stopped the Ativan and went to klonopin. A few weeks after I started having very bizarre symptoms like fully body muscle twitching, cramps, pins and needles feeling and a bunch of other scary symptoms. Could the difference in the benzos cause such things? I've been cleared by my doctors and neuromuscular specialists as its not some type of disease. I still twitch 24/7 and still experience strange symptoms to this day which is a year later. Thanks

  • Hassaan Huda Abbasi

    Hey man thanks. I just wanted to see how to draw the structure from side view for prof. But I like how you worked hard for this. Nice. Btw can you understand this sentence: MBBS kar rahay ho ya BDS?

  • 111 a

    Hi, I'm 29 year old, and I've got through extreme&sudden cold turkey since the accident 3 years ago.

    I wasn't ill at all and had a sleep problem and anxiety just like anyone else.
    I was prescribed more than 10 different kinds of psychiatric drugs for 3 weeks including 3 different kinds of benzodiazephines including Ativan, Ativan shot, alprazolam, seroquel, zolpidem, lexapro(ssri), indenol, naltrexone hcl. I figured out later that all of those drugs were unnecessary to me(heard from other hospitals and facilities) The intern was experimenting or intentionally or ignorably gave it to me.

    When I was leaving the hospital, they left me extreme cold turkey.
    They didn't explained me how dangerous those drugs are and how dangerous cold turkey is. At all. They did not give me enough pills when I was leaving the hospital. (They had to explain to me about huge amount of those drug mixing even before they give it to me.)
    They had to let me know in advance that "All of those were addictive, Addiction is extremely dangerous, If you don't slowly tapper off benzodiazepine which is some of pills we gave you, You are going to able to die with cardiac arrest, cardiac neurosis, arrhythmia, heart failure, central nerve system damages, entire body nerve damages, brain damages, every organ failures and more.
    You should gradually tapper off the benzodiazepine.

    Anyway, I wouldn't have been ok even if they informed me about cold turkey and even if they let me tapper off those drugs because it was too much kinds of addictive drugs.

    After came out there, I felt really weird and dizzy for several days. After few days, I felt extreme pain which is unimaginable and fainted with cardiac arrest and respiratory disorder.
    Of course I didn't even know what that was back then. I was ended up in emergency room and then other hospital. I suffered so much after that. I had cardiac arrest every half an hour in a hospital for the first 5-6 months. I took some benzo for 2 months aftet fainting but It was meaningless because it was already after cold turkey& fainting. And any kinds of pills gave me heart bit issue &made me sicker after that.

    I didn't&couldn't take drug from the moment. It's almost 3 yrs off from the accident and I'm still having a lot of problems especially the heart problems. It was really scary, it was crazy. The symptoms I've got through were, muscle spasms, derealization, blurred vision problems, heart failure, arrhythmia, tight chest hard to breath with law lung capacity, significantly decreased body function including digesting problem(slow and not good), dull sensation everywhere including face and the teethridge. These kinds of things.

    I couldn't do any activities as it gave me cardiac arrest&faint. I spent most of my time on bed while fighting a lot of symptoms. I lost most of things of my life.

    I struggled so hard. acupuncture helped me a bit. things got better. But I'm still having heart arrhythmia daily. especially when I'm about to sleep I feel serious arrhythmia again while I can literally feel the imbalance of my damaged nerves and heart.I can feel that the sleep arrhythmia is kind of dangerous one as I instinctively feel the danger of faint if I don't wake up instantly every moment. This is hard. I don't want to get defibrillator yet because it happens every day yet. I'm really curious of my symptoms because people on youtube doesn't talk about irregular heart bit a lot. A doctor told me that there are nerves in heart and it could have been damaged with CNS. I don't know what are things I should do although I know and heard I should struggle yrs more. I'm thinking to visit alternative med center later when I can travel long. Hope their supplements support damaged nerves and more. I can't move a lot ,focus, exercise, take medicines, drink coffee or tea as it gives me scary arrhythmia. I guess people don't focus on heart as it is one issue of many but I'm really curious if you had a heart issue too. or heard of it. It's really important to me. Please share your opinion. And any advice. It would help me a lot. Thank you very much

  • Ju Hao

    I am prescribed Xyrem (GHB) for narcolepsy and Oxazepam (Benzo) for anxiety/panic attacks. Obviously, I don't combine the two. But I'm wondering, since Xyrem is a drug I use almost every night to combat daytime sleepyness, except for on days my anxiety is through the roof and I need to take Oxazepam, what could be the potential side effects of this on my GABA receptors? Let's say I take Xyrem 5 nights a week, and Oxazepam 2 days a week (one dose 10mg). Is this going to fry my head? Will it fuck me up and give me brain damage?

  • Because Kittens & Paint

    Benzodiazepines down regulate GABA receptors in the CNS, GI tract, and brain. Dr's do not advise patients of the real side effects. World Benzodiazepine Awareness Day is July 11. This is a world wide education of the real side effects of benzos.

  • jeffmack57

    You forgot the best part dude. Shortly after you start taking benzos, your gaba receptors get down regulated. So you have to take more to get the same effect. Let's say you were prescribed benzos for anxiety. Initially they work great, then your receptors get down-regulated and you need to take more or your anxiety will come back. This can go on and on. And then when you want to actually stop taking benzos………..well you are fucked then. Those down-regulated gaba receptors take at best months and more than likely, years to get up-regulated back to some semblance of normal.

    Meanwhile, the withdrawal from these can be horrendous. Most people who have withdrawn from benzos and opiates will tell you that opiate withdrawal is a walk in the park compared to benzo withdrawal.

    Don't take benzos longer than a week.
    .

  • Thimble

    I continually worry about my health especiallly about dementia or brain issues. My mum had dementia. I think this is the root cause of it. I am also dealing with chronic hip pain which apparently seems to be some kind of ligament problem as per my orthopeadic doctor.

    It’s non stop going around and around in my mind.
    I take 5mg to 20mg of Valium and it relieves it. Effective.

    I didn’t know life could be so difficult/complicated. Sometimes it’s all too much.

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