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Re: ritanserin, pimavanserin, and lumateperone SLS

Posted by undopaminergic on September 13, 2021, at 8:10:20

In reply to Re: ritanserin, pimavanserin, and lumateperone undopaminergic, posted by SLS on September 12, 2021, at 21:26:49

> Hi again.


> > You don't mention asenapine (Sycrest, Saphris). This is currently my main candidate.
> I didn't know that about asenapine. Is it an inverse-agonist?

Antagonist I believe. According to my data, of all the numerous receptors it touches, it has the highest affinity for 5-HT2C.

> I think you're looking at the right one, if for no other reason than I have seen it work long-term in a friend of mine to produce an improvement in both mood and cognition.

Yes, you mentioned that in another post.

> However, she has schizoaffective disorder, bipolar-type.

I might have that too.

> However, asenapine could not prevent the manic psychosis that she experienced as a reaction to Effexor. When I tried asenapine, I received a mild-moderate antidepressant effect that lasted for about a week before it capitulated to my supremely stubborn brain. I like asenapine. I found it to be a very clean drug with respect to side effects, including sedation or brain-fog.

That is surprising, given how many receptor types it antagonises.

> I understand that most of the atypical antipsychotics are actually inverse-agonists of the 5-HT2a/c receptors.

I think they are mostly regular antagonists. Also, pretty much all of them have higher affinity for 5-HT2A than 5-HT2C.

Last time I checked, I only found one inverse agonist at 5-HT2C, and that was sertindole (Serdolect). I tried it and had to quit due to extreme nasal congestion.

> However, I read one paper that said specifically that asenapine was a pure antagonist and not an inverse agonist at 5-HT2a receptors with little affinity for 5-HT2c receptors. Asenapine causes virtually no weight gain compared to the great amount of weight gain with olanzapine and clozapine.

That is great. In any case, I've *lost* weight on clozapine.

> Good luck.






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