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Re: any drugs with strong NRI action ?

Posted by Hordak on June 30, 2018, at 16:59:02

In reply to any drugs with strong NRI action ?, posted by TriedEveryMedication on June 25, 2018, at 14:59:48

Clomipramine with its metabolite! ;=)

"Although clomipramine shows around 100- to 200-fold preference in affinity for the SERT over the NET, its major active metabolite, desmethylclomipramine (norclomipramine), binds to the NET with very high affinity (Ki = 0.32 nM) and with dramatically reduced affinity for the SERT (Ki = 31.6 nM).[49][50] Moreover, desmethylclomipramine circulates at concentrations that are approximately twice those of clomipramine.[51] In accordance, occupancy of both the SERT and the NET has been shown with clomipramine administration in positron emission tomography studies with humans and non-human primates.[52][53] As such, clomipramine is in fact a fairly balanced SNRI rather than only a serotonin reuptake inhibitor (SRI).[54]"

https://en.wikipedia.org/wiki/Clomipramine

https://psychotropical.info/clomipramine-potent-snri-anti-depressant/


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poster:Hordak thread:1099300
URL: http://www.dr-bob.org/babble/20180521/msgs/1099370.html