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Re: Best serotonin 5-HT2C antagonist?

Posted by undopaminergic on September 10, 2021, at 17:27:42

In reply to Re: Best serotonin 5-HT2C antagonist?, posted by linkadge on September 10, 2021, at 16:54:14

> Clomipramine, to some degree is a 5-ht2c antagonist. Many of the TCAs are 5-ht2a/c antagonists.
> There are no available selective 5-ht2c antagonists. The closest is agomelatine, but I don't think this is available in the US.

It is available here in Europe (EU). However, its half-life is only 1--2 hours, which does not sound useful:

I used it many years ago, but did not notice an effect.

> Others would include TCAs, mirtazapine, cyproheptadine and atypical antipsychotics.

Yes. I'm thinking asenapine (Saphris, Sycrest):

Of all receptors, it has the greatest affinity for 5-HT2C.

> I sometimes combine mirtazapine and cyproheptadine. I believe that mirtazapine is an inverse agonist which confers some additional properties over traditional antagonists.

Asenapine is derived from mianserin like mirtazapine.

Last time I checked, sertindole was also an inverse agonist at 5-HT2C. I tried it, but had to cease it very soon due to extreme nasal congestion.

> A selective 5-ht2c antagonist would be quite useful (in my opinion).

Yes, absolutely.

There are some used in research, and I tried to acquire them years ago, but failed.





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