I1 imidazoline receptor agonists

Ian Musgrave Ian.Musgrave at med.monash.edu.au
Thu Aug 1 19:01:31 EST 1996


G'Day All

<4tpkik$nqh at selene.rz.uni-duesseldorf.de> bernd rupp 
<rupp at pharm.uni-duesseldorf.de> writes:>From: bernd rupp 
<rupp at pharm.uni-duesseldorf.de>>Subject: I1 imidazoline receptor agonists
>Date: 1 Aug 1996 06:58:28 GMT

>I need biologycal and physical datas about selective I1 imidazoline receptor
>agonists.
>Greatly appreciate any help.

There are currently two candidates for relatively selective I1 receptor 
"agonists", moxonidine and rilmenidine. There are a few problems though. 
Firstly, the notion of what is an imidazoline agonist is problematical. A 
compound is said to be an "agonist" if it produces hypotension when injected 
into the RVLM. It is still not clear if this is actually an agonist action. 
Secondly the actual affinities of these compounds for I2-sites and 
alpha2-adrenoceptors vary between groups (moxonidine has been variously 
described as 70 times more selective for I1 sites than for alpha2 to having 
no affinity for I1 sites at all). You would be well advised to check the 
affinity in your test system first. There is a new compoune AGN 192403 (Munk 
et al 1996), with high affinity for I1 binding sites, which is neither an 
antagonist nor an agonist for blood pressure responses.

The following references will get you started.

Bricca, G, Dontenwill, M, Molines, A, Feldman, J, Tibirica, E, Belcourt, A, 
and Bousquet, P (1989) Eur J Pharmacol 163  373-7Bricca, G, Zhang, J, Greney, 
H, Dontenwill, M, Stutzmann, J, Belcourt, A, and Bousquet, P (1993) Br J 
Pharmacol 110  1537-43Campbell, WR, and Potter, DE (1995) Ann N Y Acad Sci 763 
463-85Coupry, I, Lachaud, V, Podevin, RA, Koenig, E, and Parini, A (1989) Am J 
Hypertens 2  468-70Ernsberger, P, Haxhiu, MA, Graff, LM, Collins, LA, Dreshaj, 
I, Grove, DL, and Graves, ME (1994) Cardiovasc Drugs Ther 8 Su pl 1 p27-41
King, PR, Suzuki, S, Louis, WJ, and Gundlach, AL (1995) Ann N Y Acad Sci 763 
194-207
Regunathan, S, Bramwell, S, and Reis, DJ (1995) Ann N Y Acad Sci 763 290-4
Munk et al., (1996) J Medicinal Chem 39 1193-5
---------------------------------------------
Ian Musgrave Ph.D, Prince Henry's Institute of Medical Research
PO Box 5152, Clayton 3168, Australia.
Phone +61 3 550 4286 FAX +61 3 550 6125
Lab: Ian.Musgrave at med.monash.edu.au <http://www.mmcc.monash.edu.au/~ian-mu/>
Private: Reynella at werple.mira.net.au <http://werple.mira.net.au/~reynella/>



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