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Re: Amitriptyline and percentages of SERT blockade linkadge

Posted by Skeletor on April 10, 2020, at 17:21:58

In reply to Re: Amitriptyline and percentages of SERT blockade, posted by linkadge on April 10, 2020, at 16:41:21

> According to Wikipedia, amitriptyline dose have significant affinity for the serotonin transporter (more so than the norepinephrine transporter), but probably 10x weaker than clomipramine.
> There are differences in the way that drugs bind to the serotonin transporter, however (different binding sites which may make one drug not directly comparable to another). For example, escitalopram binds to the allosteric site SERT which can enhance the effective inhibition.
> As far as why it is less likely to cause serotonin syndrome, who knows. Some of the serotonin antagonism may reduce it.
> For amitriptyline the affinity of SERT to 5-ht2a is 6. For clomipramine, it is 150. The relatively higher affinity for 5-ht2a may offset some of the SERT effect (preventing serotonin syndrome).
> Linkadge

Thanks for your response. It indeed would make sense. 5HT2 and 5HT3 antagonists seem to attenuate Serotonin toxicity.

Found this, but not sure how legit it is:




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