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Bioorg Med Chem Lett. 2009 Jun 1;19(11):3118-21. doi: 10.1016/j.bmcl.2009.03.162. Epub 2009 Apr 7.

Potent and selective alpha1A adrenoceptor partial agonists--novel imidazole frameworks.

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  • 1Pfizer Global Research and Development, Sandwich Labs, Sandwich, Kent, UK.


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.

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