Abstract
A series of 2-[(arylmethoxy)imino]imidazolidines was synthesized by reacting 2-chloro-4,5-dihydroimidazole with corresponding O-arylmethylhydroxylamines and evaluated for their alpha-, alpha2-adrenergic and imidazoline I1, I2 receptor binding affinities. The most potent 2-[(naphthalen-1-ylmethoxy)imino]imidazolidine showed a high selectivity and good affinity for the [3H]prazosin-labeled alpha1-adrenoceptors (K(i) = 107 nM). Representative compounds of this series were also tested in vivo for possible circulatory effects in rats after intravenous administration.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Animals
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Blood Pressure / drug effects
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Heart Rate / drug effects
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Imidazolidines / chemical synthesis
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Imidazolidines / metabolism
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Imidazolidines / pharmacology*
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Imidazoline Receptors / metabolism
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Male
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Radioligand Assay
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Rats
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Rats, Sprague-Dawley
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Rats, Wistar
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Receptors, Adrenergic, alpha-1 / metabolism
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Receptors, Adrenergic, alpha-2 / metabolism
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Structure-Activity Relationship
Substances
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Imidazolidines
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Imidazoline Receptors
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Receptors, Adrenergic, alpha-1
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Receptors, Adrenergic, alpha-2
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imidazoline I1 receptors
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imidazoline receptor 2