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Re: what is most selective 2a blocker we have ?? » linkadge

Posted by King Vultan on January 13, 2005, at 15:02:31

In reply to what is most selective 2a blocker we have ??, posted by linkadge on January 13, 2005, at 14:23:43

> Does anyone know what the most selective 2a blocker that we have available.
>
> Is it remeron, or one of the TCA's ??
>
>
> Linkadge


Risperdal at dosages of less than 1 mg/day is easily the most selective 5-HT2A blocker among psychotropic drugs. Remeron's H1 blockade is about 10 times stronger than its 5-HT2A blockade, and Remeron's 2A blockade is only a little more selective than its 2C blockade (Ki of 1.48 vs. 4.1, respectively).

In contrast, Risperdal's 5-HT2A blockade is probably about 20 times stronger than its next relevant blockade (alpha-1 adrenergic). It is also extremely selective for the 2A vs. 2C receptor (Ki of 0.15 vs. 32, a factor of about 200x). Geodon would be the closest to Risperdal in terms of overall selectivity for the 2A receptor, but it is not particularly selective for the 2A vs. 2C receptor.

Todd


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poster:King Vultan thread:441676
URL: http://www.dr-bob.org/babble/20050113/msgs/441693.html