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Dr. Bob is Robert Hsiung, MD,
bob@dr-bob.orgShown: posts 1 to 16 of 16. This is the beginning of the thread.
Posted by linkadge on January 7, 2004, at 15:43:06
I have kind of figured out what the 5hta receptor does for me. I am still debating weather to block it or not.
With 5t2a activity, I am very much not obsessed with things. This makes certain learning much more easy to do, but other learning much more difficult. It makes me want to stay away from people and to enjoy my own indepandance. However on SSRI's I alway get into a panic when my independace is compromised. On Celexa alone I would die if I had to get married. I am never irritable, just suicidal.
If I block the receptor, then I become much more social. I feel sad if I am lacking human contact. I want to get married. I become more obsessed. I enjoy reading. I cannot remember things well, and am not very smart, I cen get irritable, but am never suicidal.
Quite frankly I like Celexa alone but I don't fit into society very well.
Linkadge
Posted by SLS on January 7, 2004, at 16:25:25
In reply to Thoughts on the 5h2a receptor, posted by linkadge on January 7, 2004, at 15:43:06
> I... am not very smart
No, you're not. You are very, VERY smart.
:-)
I envy you your brain power.
- Scott
Posted by SLS on January 7, 2004, at 16:32:35
In reply to Thoughts on the 5h2a receptor, posted by linkadge on January 7, 2004, at 15:43:06
> I have kind of figured out what the 5hta receptor does for me. I am still debating weather to block it or not.
> Quite frankly I like Celexa alone but I don't fit into society very well.
Why don't you give Abilify a quick trial added to Celexa.
By the way, how did you arrive at your conclusions regarding the effects of 5-HT2a blockade? What drugs did you use?
- Scott
Posted by tensor on January 7, 2004, at 17:03:15
In reply to Re: Thoughts on the 5h2a receptor, posted by SLS on January 7, 2004, at 16:32:35
Posted by linkadge on January 7, 2004, at 17:16:01
In reply to Re: Thoughts on the 5h2a receptor, posted by SLS on January 7, 2004, at 16:32:35
I have used quite a few that block the 5ht2a receptor.
Seroquel, Risperdal, Remeron, Periactin.
Noramlly (on celexa alone) I am not antisocial, but I just don't like to hang around and talk.
I am very independant.But when I take a 5h2a receptor antagonist. All of a sudden things change. For starters I sleep like a baby. I start obsessing about things - like drawing pictures in my head. I am able to cry. I feel homesick. I like listening to music and watching long movies. And dumb things like "being proud to be a canadian", things that would never even cross my mind normally. I feel more plugged into the world. (on celexa alone I always feel like I am trying to wake up from something, trying to get an objective view of what is happening.
Even though the former feelings are so unnatural, I enjoy them, I feel like a somebody, and not like an everybody. Weird.
Linkadge
Posted by linkadge on January 7, 2004, at 17:44:42
In reply to Re: Thoughts on the 5h2a receptor, posted by linkadge on January 7, 2004, at 17:16:01
My findings also seem to fit with current ideas on the 5ht2a receptor. Antidepressants which block the 5h2a receptor don't seem to be very good at treating OCD.
Posted by Sad Panda on January 7, 2004, at 23:48:49
In reply to Re: Thoughts on the 5h2a receptor, posted by linkadge on January 7, 2004, at 17:44:42
> My findings also seem to fit with current ideas on the 5ht2a receptor. Antidepressants which block the 5h2a receptor don't seem to be very good at treating OCD.
Clomipramine blocks 5-HT2a & is supposed to be great for OCD.
Cheers,
Panda.
Posted by linkadge on January 8, 2004, at 6:44:54
In reply to Re: Thoughts on the 5h2a receptor » linkadge, posted by Sad Panda on January 7, 2004, at 23:48:49
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.
I thought that anafranil was essentially a very sertogenic tryciclic.
Linkadge
Posted by Sad Panda on January 8, 2004, at 7:41:03
In reply to Re: Thoughts on the 5h2a receptor, posted by linkadge on January 8, 2004, at 6:44:54
> 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.
>
> I thought that anafranil was essentially a very sertogenic tryciclic.
>
> Linkadge
>
>According to
http://www.psychotropical.com/notes/628.html-------------------------------------------------
5-HT2A receptorsStudies 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.
Many neuroleptic drugs, both old and new, are also potent 5-HT2A blockers.SSRIs nil sig except
fluoxetine 280Trimipramine 15
Amitriptyline 18
Clomipramine 23
Doxepin 27
Trazodone 25
Nefazodone 26
mirtazapine ~30
Nortriptyline 41Imipramine 150
desipramine 350
lofepramine 200
Dr Ken Gillman MRC PsychPsychoTropical Research
Email me any relevant comments - kgillman@psychotropical.com
-------------------------------------------------
My understanding is that anafranil has the most effect on 5-HT when compared to other tricyclics too, but it also affects a lot of other receptors, ie: clomipramine, imipramine, amitriptyline & doxepin all have very similar NE reuptake inhibiting abilites.
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
Posted by linkadge on January 8, 2004, at 9:03:21
In reply to Re: Thoughts on the 5h2a receptor, posted by SLS on January 8, 2004, at 8:15:20
Not exactly sure why that is then.
From my understanding (a few studies I will look for), SSRI's were effective for OCD but that effect was diminished/reduced when a 5ht2a receptor blocker was added, Ie trazodone, periactin etc. Perhaps, of the tryciclics, anafranil exerted the most 5ht2a agonism - regardless of its blocking capabilities.
I could be wrong :), but my understanding was that many drugs such as mirtazapine, and trazodone were innefective for OCD (expecially where sexual cotnent was involved in symptoms).
I suppose this effect would need to be studied specifically.
Linkadge
Posted by jparsell82 on January 8, 2004, at 12:28:11
In reply to Re: Thoughts on the 5h2a receptor, posted by linkadge on January 8, 2004, at 9:03:21
How was mirtazapine for you? I am soon going to be giving it a try because of it's 5ht2 & 5ht3 antagonizing abilities. I recently tried Ondansetron for it's 5ht3 antagonizing effect and was pleased. I was less anxious and socially withdrawn... plus I got my appetite back and my stomach tightness went away. Unfortunately, ondansetron is too expensive. Also, I've read mirtazepine is an agonist at 5ht1a receptors. So, that I would think would add to the anxiolytic effect because Buspar's a 5ht1a agonist. Did mirtazepine give you any/much relief from anxiety or ocd?
Posted by linkadge on January 8, 2004, at 17:11:21
In reply to Re: Thoughts on the 5h2a receptor » linkadge, posted by jparsell82 on January 8, 2004, at 12:28:11
It was really a strange drug. It did not work for me, but I can imagine the type of person for which it would work.
The apatite increase is substantial - at least it was for me. The first few weeks are a mixed bag. You will emmediately sleep like a baby, but you will be irritable for a little while.
If your symptoms of anxiety are mainly mental then it may work well for you, however if your syptoms of anxity are more phyiscal like heart palpatitions and sweating, then it may not be the best.
You can always give it a try.
Linkadge
Posted by Iansf on January 8, 2004, at 19:41:35
In reply to Re: Thoughts on the 5h2a receptor » linkadge, posted by Sad Panda on January 8, 2004, at 7:41:03
> 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.
> Many neuroleptic drugs, both old and new, are also potent 5-HT2A blockers.
>
> Trazodone 25
>
>Does anyone know if the typical trazodone dose used for sleep (25mg-100mg)would effectively block 5-HT2A? Or would you have to take a therapeutic dose to get the blocking effect?
Someone also mentioned periactin for blocking 5-HT2A. How much of that is needed?
Thanks.
Ian
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.
Posted by Francesco on January 10, 2004, at 16:59:30
In reply to Re: Thoughts on the 5h2a receptor, posted by linkadge on January 7, 2004, at 17:16:01
> But when I take a 5h2a receptor antagonist. All of a sudden things change. For starters I sleep like a baby. I start obsessing about things - like drawing pictures in my head. I am able to cry. I feel homesick. I like listening to music and watching long movies. And dumb things like "being proud to be a canadian", things that would never even cross my mind normally.
lol
I have a Remeron script and a Remeron box but your post really scares me ! I don't want my mind to think things like: "I am proud to be Italian". I would prefer constipation and dry mouth rather than this ! ;-)
This is the end of the thread.
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