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Re: Thoughts on the 5h2a receptor » SLS

Posted by Sad Panda on January 9, 2004, at 11:45:25

In reply to Re: Thoughts on the 5h2a receptor, posted by SLS on January 8, 2004, at 8:15:20

> > > 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
>

Hi Scott,

That web site is a pretty good read, Download the "Psychpharamcology Update Notes" program & read it as well as the updates on the website it's self. Dr Gillman gives the impression that he knows what he is talking about.

Here is all the receptor data I could find from his website.


__________________5-HT__NE____H1___5-HT2A__A1___M1
CLOMIPRAMINE___0.28___38____15_____23_____50____25
IMIPRAMINE______1.4____37_____37____150_____32___60
AMITRIPTYLINE___4.3____35_____1_____18_____24____13
DOTHIEPIN________8.6____46_____3.6__________450___38
NORTRIPTYLINE___18_____4.3____6.3___41______55___50
DESIPRAMINE____________0.83___60____350____100___210
DOXEPIN__________68____29.5____0.2___27______23___52
MIANSERIN________4000_________0.4___________34_____
MIRTAZAPINE__________________0.12___30_____________
NEFAZODONE_____200__________24000__26_____48_____
VENLAFAXINE_____8.9____1060__35000________35000___
PAROXETINE______0.13____40________________________80
SERTRALINE______0.29__________24000_________380__1300
FLUOXETINE______0.81____240_________280__________1000
CITALOPRAM_____1.16________________________________
FLUVOXAMINE____2.2________________________________

Cheers,
Panda.


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poster:Sad Panda thread:297739
URL: http://www.dr-bob.org/babble/20040109/msgs/298574.html