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5ht2b agonists

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dip12

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Joined
Feb 4, 2012
Messages
82
Ok so 5ht2b agonists are BAD (as in seriously dangerous) for the heart but purely hyperthetically would a selecive 5ht2b agonist (i.e no other action) be a fun drug / anxiolytic etc?

It seems a lot of medications effect it (up or down regulation of 5ht2b after long term ssri, MDMA, mephedrone etc etc)

Is there such a thing as a CNS selective drug? anyone know of any examples?
 
dip12 said:
Is there such a thing as a CNS selective drug? anyone know of any examples?
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If by this you mean a drug that is active only in receptors behind the blood-brain-barrier, no. Not to my knowledge is this possible.

However I think your premise is mistaken in that 5ht2b displays its cardiac properties through its CNS mechanism. i.e. there are no 5ht2b receptors in the heart, it is mediated by CNS 5ht2b receptor activation as a function upon the heart.
 
Nagelfar said:
However I think your premise is mistaken in that 5ht2b displays its cardiac properties through its CNS mechanism. i.e. there are no 5ht2b receptors in the heart, it is mediated by CNS 5ht2b receptor activation as a function upon the heart.
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5-HT2B receptors are expressed in heart valves, I think.

OP, wikipedia says 5-HT2B stimulation induces "neuronal sensitization to tactile stimuli" i.e. tactile enhancement, which makes me think that 5-HT2B may underlie the pleasant physical sensations induced by serotonergics.
 
If by this you mean a drug that is active only in receptors behind the blood-brain-barrier, no. Not to my knowledge is this possible.
Click to expand...

Well, you could administer a drug that doesn't pass the BBB intracranially... :P

ebola
 
atrollappears said:
5-HT2B receptors are expressed in heart valves, I think.
Click to expand...

Then perhaps I am mistaken.

ebola? said:
Well, you could administer a drug that doesn't pass the BBB intracranially... :P
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A drug that metabolizes from one that does (cross the BBB) to one that doesn't, at some brain exclusive site, would be an interesting prospect, wouldn't it? Though being simpler yet not doing so seems an impossibility, might it have to bond covalently to some loose enzyme or such? How complicating.

Is it so that not crossing the BBB can mean travel outside? That never diffusing out into the blood stream is even possible for a molecule within? There would almost I think need to be a system of active transport of molecules fitting particular criteria from the rest of the body *to* the brain, almost.
 
Yeah I think fenfluramine toxicity was generally thought to be via 5ht2b receptors in the heart.

In terms of CNS selective, (having remembered) there is L-DOPA combined with peripheral dopa-decarboxylaze inhibitors - not an easy mechanism to incorporate a 5ht2b agonist though. :\

If it wasn't for the serious cardiac (fatal) problems this looks an interesting molecule:

http://en.wikipedia.org/wiki/BW-723C86
 
dip12 said:
In terms of CNS selective, (having remembered) there is L-DOPA combined with peripheral dopa-decarboxylaze inhibitors - not an easy mechanism to incorporate a 5ht2b agonist though. :\
Click to expand...

The idea of selectively canceling out its peripheral activity is not too hard to implenent: general 5-HT2B agonist + 5HT2B antagonist incapable of crossing the BBB. That would entail finding the latter agent, but I'm sure someone could manage it through receptor modeling.
 
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