Questions about receptor abboundance

[/navarone/]

Good day

Lately I got kind of stuck while thiking about a matter that interests me to a personal level since i, like many, have suffered from a few psychological and neurological problems in the past. So i would like to ask you something.

So I do know that the amount of neurotransmitter stimulation is dependent on the amount of receptors ready to accept them and a lack in the number of receptors, if severe, can lead to many kinds of neurological or psychological problems since even if the brain is streamed with a very high concentration of receptor ligands, there are not enough bindign sites to detect them and as a consequence many of the excess ligands are broken down before they can bind to the specific receptor.
Please let me know if there's anything wrong in what I wrote.

Now my question is, speaking in terms of sobriety and brain health, can there be a true excess in receptors/binding sites and if yes, could that abboundance in bindind sites cause any negative reactions on a brain that is not experiencing any kind of heavy stress?

Basically what I was asking myself is: if a brain has a number of receptors/binding sites which is above the standards is it a more efficent and vigilant brain i.e. a healthier brain?

Also what factors, apart from genetics, modulate the number of active binding sites on a neuron?

 

[helium-4]

I can't answer your questions, but I do know that not all of the receptors necessarily need to be occupied for maximum pharmacological response. Some drugs only use of to 2% of the receptors to produce the maximum pharmacological response.

 

[Black]

Basically what I was asking myself is: if a brain has a number of receptors/binding sites which is above the standards is it a more efficent and vigilant brain i.e. a healthier brain?

not necessarily. a overabundance of receptors could be pathological as well. i don't know an example for the receptors you are thinking about, but a overabundance of growth factor receptors is a factor in tumorigenesis.

Also what factors, apart from genetics, modulate the number of active binding sites on a neuron?

for example epigenetics (modulating the expression of the genes by attaching or deattaching methyl groups to the dna) or simply recent activity. if there's a lot of neurotransmitters hitting a neuron, receptors will be desensitised, internalised and some of them degraded.

 

[Hammilton]

epigenetics has always fascinated me. I forget the name of the drug right now, but there's one being used quite successfully to remove methyl markets from DNA in the treatment of some previously untreatable forms of cancer, with very positive effect.

I remember it was trialed in the 70's, dismissed as far too toxic, but interest sparked again with doses much lower than before, and still good efficacy.

 

[Black]

that's quite interesting. i'll have to look that up some time.

 

[Hammilton]

It's Decitabine or Azacitidine, the former, i think.