Abstract
Novel 2'-heteroaryl-2-(phenoxymethyl)imidazolines have been identified as potent agonists of the cloned human alpha(1)-adrenoceptors in vitro. The nature of the 2'-heteroaryl group can have significant effects on the potency, efficacy, and subtype selectivity in this series. alpha(1A) Subtype selective agonists have been identified.
MeSH terms
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Adrenergic alpha-1 Receptor Agonists*
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Adrenergic alpha-Agonists / pharmacology*
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Humans
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Hydrogen Bonding
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Imidazoles / chemical synthesis*
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Imidazoles / pharmacology*
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Phenyl Ethers / chemical synthesis*
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Phenyl Ethers / pharmacology*
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Receptors, Adrenergic, alpha-1
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Recombinant Proteins
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Structure-Activity Relationship
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Urinary Incontinence, Stress / prevention & control
Substances
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ADRA1A protein, human
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Adrenergic alpha-1 Receptor Agonists
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Adrenergic alpha-Agonists
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Imidazoles
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Phenyl Ethers
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Receptors, Adrenergic, alpha-1
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Recombinant Proteins