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Re: SLS and all....5ht1a autoreceptor antagonists.... » bleauberry

Posted by SLS on September 4, 2008, at 22:04:45

In reply to Re: SLS and all....5ht1a autoreceptor antagonists...., posted by bleauberry on September 4, 2008, at 20:26:07

> I do not understand what an agonist would do. Would that further worsen an already over-sensitive receptor?

I think being exposed to a stimulating ligand (whether it be the endogenous neurotransmitter or one synthesized as a drug) causes a downregulation of the receptor membranes - both pre- and post- synaptic. Sometimes, I get the idea that perhaps it doesn't matter which way you push the system, as long as the system is encouraged to reregulate itself. This would explain the apparant paradox of SSRIs and tianeptine.


> Also could you please explain to me what a "reverse agonist" is and how it works? When I see that term it confuses me.

Inverse agonist.

An inverse agonist binds to a receptor, but does not stimulate it. In fact, it does just the opposite. It exerts a negative force upon neuronal activity. If a neural pathway is supposed to make you feel hot:

agonist - feel hot
antagonist - feel "not hot"
inverse agonist - feel cold

That's not the best example of the phenomenon, but I hope it helps a little.


- Scott

 

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