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Re: Thoughts on the 5h2a receptor

Posted by SLS on January 8, 2004, at 8:15:20

In reply to Re: Thoughts on the 5h2a receptor » linkadge, posted by Sad Panda on January 8, 2004, at 7:41:03

> > Acording to
> >
> > http://sl.schofield3.home.att.net/medicine/psychiatric_drugs_chart.html
> >
> > The only tryciclic that has appreciable affinity for blocking the 5-th2a receptor is amitryptaline.

> According to
> http://www.psychotropical.com/notes/628.html

> ------------------------------------------------

> 5-HT2A receptors
>
> Studies using sleep EEGs on new drugs like nefazodone and mirtazapine suggest that 5-HT2A blockade produces an improvement in sleep patterns that is clinically useful. Many antidepressant drugs have such properties, data as below. Low numbers means high potency, ie bigger effect.


> SSRIs nil sig except
> fluoxetine 280
>
> Trimipramine 15
> Amitriptyline 18
> Clomipramine 23
> Doxepin 27
> Trazodone 25
> Nefazodone 26
> mirtazapine ~30
> Nortriptyline 41
>
> Imipramine 150
> desipramine 350
> lofepramine 200


I could not find any information regarding the potency of trimipramine and clomipramine as ligands for 5-HT2 receptors. However, it appears that the list is accurate. Potency is moderate. I think I'll give it a ++ and add this to my chart. The Ki of of these drugs lie between 10-50(nM), an order of magnitude less potent than risperidone 0.2-0.5(nM), and somewhat less than amitriptyline 1.0-5.0(nM).

Thanks for the heads-up!

Can you recommend any more sources of this type of information?

Thanks.


- Scott

 

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