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Novel imidazole frameworks have been identified as potent partial agonists of the alpha(1A) adrenergic receptor, with good selectivity over the alpha(1B), alpha(1D) and alpha(2A) receptor sub-types. Nitrile 28 possessed attractive CNS drug-like properties with good membrane permeability and no P-pg mediated efflux. 28 also possessed excellent solubility, metabolic stability and wide ligand selectivity.

Original publication

DOI

10.1016/j.bmcl.2009.03.162

Type

Journal article

Journal

Bioorg Med Chem Lett

Publication Date

01/06/2009

Volume

19

Pages

3118 - 3121

Keywords

ATP Binding Cassette Transporter, Subfamily B, Member 1, Adrenergic alpha-1 Receptor Agonists, Adrenergic alpha-2 Receptor Agonists, Animals, Cell Line, Dogs, Humans, Imidazoles, Receptors, Adrenergic, alpha-1, Receptors, Adrenergic, alpha-2