Abstract
A series of 2-[(heteroaryl)methyl]imidazolines was synthesized and tested for their activities at α(1)- and α(2)-adrenoceptors and imidazoline I(1) and I(2) receptors. The most active 2-[(indazol-1-yl)methyl]imidazolines showed high or moderate affinities for α(1)- and α(2)-adrenoceptors. However, their intrinsic activities at α(2A)-adrenoceptors proved to be negligible. A selected 7-chloro derivative behaved as a potent α(1)-adrenoceptor antagonist and exhibited peripherally mediated hypotensive effects in rats.
Copyright © 2011 Elsevier Ltd. All rights reserved.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic alpha-Antagonists / chemical synthesis*
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Adrenergic alpha-Antagonists / chemistry
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Adrenergic alpha-Antagonists / pharmacology
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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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Humans
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Imidazolines / chemical synthesis
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Imidazolines / chemistry*
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Imidazolines / pharmacology
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Motor Activity / drug effects
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Rats
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Receptors, Adrenergic, alpha-1 / chemistry
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Receptors, Adrenergic, alpha-1 / metabolism
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Receptors, Adrenergic, alpha-2 / chemistry
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Receptors, Adrenergic, alpha-2 / metabolism
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Structure-Activity Relationship
Substances
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Adrenergic alpha-Antagonists
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Imidazolines
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Receptors, Adrenergic, alpha-1
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Receptors, Adrenergic, alpha-2