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ID: ALA1149219

Journal: Bioorg Med Chem Lett

Title: Binding of beta-carbolines at imidazoline I2 receptors: a structure-affinity investigation.

Authors: Glennon RA, Grella B, Tyacke RJ, Lau A, Westaway J, Hudson AL.

Abstract: A series of ring-substituted (i.e., methoxy and bromo) 3,4-dihydro- and 1,2,3,4-tetrahydro-beta-carbolines was examined at I(2) imidazoline receptors, as was the effect of ring-opening, ring-expansion, and translocation of the piperidinyl nitrogen atom. Several analogues were identified that bind with K(i) <20 nM at I(2) sites and with reduced affinity at alpha(2)-adrenergic receptors, and 1,2,3,4-tetrahydro-gamma-carbolines were identified as a novel class of I(2) imidazoline receptor ligand.

CiteXplore: 15013009

DOI: 10.1016/j.bmcl.2003.11.078