NMDA receptors

10708 Views 9 Replies 5 Participants Last post by riya_rai84, Dec 7, 2012

DrSeddik

Discussion Starter · Dec 28, 2009

I don't like NMDA receptors, I get seriously irritated when I see them in a question, so if anybody knows any high yield information other than these about them, please share.

- Ketotifen and PCP are NMDA antagonists, both were essentially anaesthetic agents, PCP is now only abused with Marijwana.
- Neurotransmitter is Glutamate, with the help of glycin
- They are CNS stimulants
- Blockade prevents tolerance to opioids.

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ahassan

· #2 · Dec 29, 2009

here's what I think is HY:
1. the NMDA receptor if found throughout the CNS (eg.hippocampus, cerebral cortex, spinal cord)

2. when glutamate n the cofactor glycine bind to the NMDA receptor the gate is opened and influx of Na n Ca and efflux of K occurs.

3. in addition, a voltage dependent membrane depolarization is required to open the gate bcz the NMDA receptor is "plugged" by extracellular Mg at resting membrane potential.

4. drugs, Amantidine (noncompetitive blocker)

Memantine (noncompetitive, use-Dependant blocker)

Ketamine (Ketalar, special K, k) is an antagoinist that acts as a CNS depressent & dissociative anesthetic, date rape drug.

PCP n Dizocilpne are NMDA receptor open channel blockers.

Will add your points as well.

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DrSeddik

Discussion Starter · #3 · Dec 29, 2009

This is realy helpful. But what do you mean by (NMDA receptor open channel blockers), does it mean they only act on stimulated NMDA receptors ? Also in memantine (use dependant blocker)?

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ahassan

· #4 · Dec 29, 2009

open channel blockers- requires the NMDA receptor to be open to be able to gain access to their binding sites.

use dependent- it becomes an effective antagoinist only after repeated receptor activation and channel opening.

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fauzan

· #5 · Dec 29, 2009

emmm...

the anti-epileptic drug FELBAMATE acts on NMDA receptors and causes its inhibition...

whereas the drug TOPIRAMATE, acts on non- NMDA (AMPA receptors ).... topiramate is also a Na channel blocker and a Gaba channel agonist....

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tomymajor

· #6 · Dec 29, 2009

Plz I want to know relation beteen NMDA receptors and Glycine

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tomymajor

· #7 · Dec 29, 2009

tomymajor said:
Plz I want to know relation beteen NMDA receptors and Glycine

I think it is NMDA antagonist???

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DrSeddik

Discussion Starter · #8 · Dec 29, 2009

tomymajor said:
Plz I want to know relation beteen NMDA receptors and Glycine

It's been mentioned, it's a cofactor for the stimulator glutamate

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ahassan

· #9 · Jan 2, 2010

some other important points I came across:

1. The NMDA receptor is important clinically bcz its hyperactivity causes excessive influx of Ca ions, this is known as glutamate toxicity, especially in the caudate nucleus leading to cell death and is implicated in Huntington disease.

2. this receptor is involved in the learning process through longterm potentiation in the hippocampus.

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riya_rai84

· #10 · Dec 7, 2012

ahassan said:
some other important points I came across:

1. The NMDA receptor is important clinically bcz its hyperactivity causes excessive influx of Ca ions, this is known as glutamate toxicity, especially in the caudate nucleus leading to cell death and is implicated in Huntington disease.

2. this receptor is involved in the learning process through longterm potentiation in the hippocampus.

some where is also mention that valproic acid blocks the NMDA receptors and thereby affecting the potassium current

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