Investigation of the affinities of two new beta-carbolines for rat brain imidazoline(2) receptors.
The beta-carbolines are possible endogenous ligands and modulators of the imidazoline binding sites (I-BSs). Relatively little is known about this class of compound and its interaction with the I-BS. Presented here are the binding data for two aryl ring substituted dihydro-beta-carbolines at the imidazoline(2) binding site (I(2)-BS) and alpha(2)-adrenoceptor: BG-326 (5-bromo-4,9-dihydro-3H-b-carboline) and BG-350 (5-methoxy-4,9-dihydro-3H-b-carboline). Both compounds show good affinity and selectivity for the I(2)-BS.
Tyacke
R J
RJ
Psychopharmacology Unit, School of Medical Sciences, University of Bristol, Bristol BS8 1TD, UK.
Lau
A
A
Grella
B
B
Glennon
R A
RA
Nutt
D J
DJ
Hudson
A L
AL
D000818:Animals; D001921:Brain / Q000378:metabolism*; D002243:Carbolines / Q000737:chemistry* / Q000378:metabolism*; D002462:Cell Membrane / Q000378:metabolism; D054755:Imidazoline Receptors; D008297:Male; D015394:Molecular Structure; D020033:Protein Isoforms / Q000378:metabolism; D051381:Rats; D017208:Rats, Wistar; D018341:Receptors, Adrenergic, alpha-2 / Q000378:metabolism; D011955:Receptors, Drug / Q000378:metabolism*
D002243:Carbolines; D054755:Imidazoline Receptors; D020033:Protein Isoforms; D018341:Receptors, Adrenergic, alpha-2; D011955:Receptors, Drug