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5-HT 1b agonists

Anders Fugelli anders.fugelli at basalmed.uio.no
Wed Jun 7 06:13:49 EST 1995


In article <stephan-0706950007450001 at modem0-9.lifesci.ucla.edu>
(bionet.neuroscience), 
stephan at psych.ucla.edu (Stephan Anagnostaras) wrote:

> In article
> <Pine.ULT.3.91j.950606180722.3970A-100000 at stein2.u.washington.edu>, Joshua
> Singer <jhsinger at u.washington.edu> wrote:
> 
> > Does anyone know of specific 5-HT 1b receptor agonists or antagonists? 
> > Any information is appreciated.
> 
> Why don't you just look in the RBI catalog under 5-HT antagonists and
> find selectivity for 1b?
> 
> -- 
> STEPHAN ANAGNOSTARAS                   UCLA BEHAVIORAL NEUROSCIENCE
> STEPHAN at PSYCH.UCLA.EDU

Dear Stephan and Joshoua.

I think that if you look in the RBI catalog, you will notice that selective
5-HT1B agonists or antagonist are NOT comercially available.
There are some agents that might be used:

Agonists:
- TFMPP is not selective for 1B but has a  slightly higher
preference for this recepor than others

- RU 24969 similar

-CGS 12066 has  reasonable selectivity for 1B

-The newly introduced agonist from Pfizer CP 93129
has reportedly good selectivety and potency at 1B receptors.
This is NOT comercially available.

Antagonists:
-No selcetive antagonists available to date,
use cyanopindolol for example, although this is also equipotent at 1A
receptors,
in addition to being a beta-adrenergic receptor antagonist.

For more information see the review by Daniel Hoyer et al.
in Pharmacological Reviews 1994 (don't remember the  vol. off-hand)

Anders Fugelli
anders.fugelli at basalmed.uio.no
Institute of Neurophysiology
University of Oslo
Norway



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