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Re: ritanserin, pimavanserin, and lumateperone undopaminergic

Posted by SLS on September 12, 2021, at 21:26:49

In reply to Re: ritanserin, pimavanserin, and lumateperone SLS, posted by undopaminergic on September 12, 2021, at 13:54:19

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

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

"It is perhaps surprising that asenapine shares the high relative affinities at 5-HT2C and H1 receptors of clozapine and olanzapine yet avoids inducing the profound weight gain associated with these drugs; in bipolar patients asenapine showed a mean increase of 1.9kg vs 4.1kg with olanzapine over 12 weeks [McIntyre et al. 2009]. While effects on 5-HT1B and/or 5-HT1A receptors could conceivably contribute, asenapine administration demonstrates a notable lack of effect on 5-HT2C receptor density in rat brain [Tarazi et al. 2010]. This is similar to that of the weaker antagonists risperidone and quetiapine and is in contrast to the down-regulation seen with olanzapine [Tarazi et al. 2002]. The difference could conceivably relate to a 5-HT2C antagonism by asenapine in the absence of the inverse agonism exhibited by olanzapine and clozapine [Herrick-Davis et al. 2000] although this is untested; whatever the mechanism, it does indicate profoundly different pharmacological influences between asenapine and olanzapine on these important receptors involved in the control of body weight."

Good luck.

- Scott

Some see things as they are and ask why.
I dream of things that never were and ask why not.

The only thing necessary for the triumph of evil is that good men do nothing.




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