Psycho-Babble Neurotransmitters Thread 816089

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Agomelatin

Posted by Markwell on March 4, 2008, at 7:46:54

I asked this question previously but does anyone have any information on when Agomelatin might be available in the US. Anyone hear any good reports on efficacy?

 

Agomelatin and 5-HT2C

Posted by rgb on March 10, 2008, at 10:54:39

In reply to Agomelatin, posted by Markwell on March 4, 2008, at 7:46:54

Sorry, can't answer your question directly, but just a thought on agomelatine:

Wikipedia specifically says that it's a 5-HT2C antagonist. If it's really selective for 5-HT2C as opposed to 5-HT2A, this would be a quite interesting add-on to an SSRI. In my dilettantish understanding, 5-HT2C is the main culprit in dopamine inhibition; correct me if I'm wrong. Unfortunately, all other 5-HT2C antagonists I know also block histamine and/or dopamine. I also wouldn't like to antagonize 5-HT2A.

Are there any legal ways of obtaining "no-mans-land" compounds like this? I hope this isn't against the rules, feel free to delete this last paragraph otherwise :)

 

Re: Agomelatin and 5-HT2C » rgb

Posted by Questionmark on April 27, 2008, at 22:29:27

In reply to Agomelatin and 5-HT2C, posted by rgb on March 10, 2008, at 10:54:39

(This would be better on PBabble, no?)
I'm 97% certain that agomelatine is a 5-HT2C antagonist and primarily if not solely selective for that receptor (vs. other 5-HT subtypes).
Yes it would be incredibly interested in trying this and it is a d*** shameful tragedy that the FDA did not approve it. I was looking forward to trying it so much. AHH!
Oh, but i always forget whether 5-HT2C or 5-HT2A receptors are more responsible-- or both relatively equally-- for dopamine inhibition with 5HT-ergic drugs. I believe it's kind of confusing based on a lot of the literature, though, if i remember correctly. Some talk about 5-ht2a being primarily responsible; others 5-ht2c. And then many simply speak of 5-HT2 receptors in general. Ah sorry, yeah that was real helpful.


> Sorry, can't answer your question directly, but just a thought on agomelatine:
>
> Wikipedia specifically says that it's a 5-HT2C antagonist. If it's really selective for 5-HT2C as opposed to 5-HT2A, this would be a quite interesting add-on to an SSRI. In my dilettantish understanding, 5-HT2C is the main culprit in dopamine inhibition; correct me if I'm wrong. Unfortunately, all other 5-HT2C antagonists I know also block histamine and/or dopamine. I also wouldn't like to antagonize 5-HT2A.
>
> Are there any legal ways of obtaining "no-mans-land" compounds like this? I hope this isn't against the rules, feel free to delete this last paragraph otherwise :)

 

Re: Agomelatin and 5-HT2C

Posted by Markwell on May 22, 2008, at 13:36:56

In reply to Re: Agomelatin and 5-HT2C » rgb, posted by Questionmark on April 27, 2008, at 22:29:27

What do you mean that the FDA hasn't approved it? Have they rejected it or is it still in the approval process? I think this is one I want to try. What phase is it in?

 

Re: Agomelatin and 5-HT2C

Posted by Negcreep on July 21, 2008, at 6:55:04

In reply to Re: Agomelatin and 5-HT2C, posted by Markwell on May 22, 2008, at 13:36:56

http://en.wikipedia.org/wiki/Agomelatine

Its VERY close to being approved by the EMEA in europe, and is in phase III trials is the US.


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