Abstract
Novel pyrroloimidazoles 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 subtypes. Pyrimidine 19 possessed attractive CNS drug-like properties with good membrane permeability and no evidence for P-gp mediated efflux.
MeSH terms
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ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
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Adrenergic alpha-1 Receptor Agonists*
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Adrenergic alpha-2 Receptor Agonists
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Animals
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Cell Line
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Dogs
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Humans
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Imidazoles / chemistry*
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Imidazoles / metabolism
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Imidazoles / pharmacology*
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Microsomes, Liver / metabolism
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Pyrimidines / chemistry*
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Pyrimidines / metabolism
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Pyrimidines / pharmacology*
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Receptors, Adrenergic, alpha-1 / metabolism
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Receptors, Adrenergic, alpha-2 / metabolism
Substances
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ADRA1A protein, human
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ADRA1B protein, human
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ADRA1D protein, human
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ADRA2A protein, human
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ATP Binding Cassette Transporter, Subfamily B, Member 1
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Adrenergic alpha-1 Receptor Agonists
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Adrenergic alpha-2 Receptor Agonists
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Imidazoles
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Pyrimidines
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Receptors, Adrenergic, alpha-1
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Receptors, Adrenergic, alpha-2