Abstract
Several WB4101 (1)-related compounds were synthesized. Their alpha-adrenoreceptor blocking properties were evaluated in order to understand the kind of interaction occurring between the amine function of (1)-related compounds and the alpha-adrenoreceptor anionic site. The results suggest that a charge reinforced hydrogen bond rather than an ion pairing might play a most important role in receptor binding.
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 / pharmacology
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Animals
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Clonidine / antagonists & inhibitors
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Clonidine / pharmacology
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Cocaine / pharmacology
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Dioxanes / chemical synthesis*
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Dioxanes / pharmacology
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Electric Stimulation
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In Vitro Techniques
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Male
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Muscle Contraction / drug effects
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Muscle, Smooth / drug effects
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Norepinephrine / antagonists & inhibitors
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Propranolol / pharmacology
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Rats
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Structure-Activity Relationship
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Vas Deferens / drug effects
Substances
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Adrenergic alpha-Antagonists
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Dioxanes
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Propranolol
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(2-(2',6'-dimethoxy)phenoxyethylamino)methylbenzo-1,4-dioxane
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Cocaine
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Clonidine
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Norepinephrine