Abstract
A unique combination of alpha 2-adrenoreceptor antagonist and serotonin-selective reuptake inhibitory activities has been identified in a series of 2-substituted 4,5-dihydro-1H-imidazole derivatives. This combination of blocking activities has provided one of these derivatives, napamezole hydrochloride (2), with potential as an antidepressant. A discussion of the syntheses of these compounds includes a convenient method for the conversion of nitriles to imidazolines with ethylenediamine and trimethylaluminum.
MeSH terms
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Animals
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Antidepressive Agents*
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Blepharoptosis / chemically induced
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Brain / drug effects
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Brain / metabolism
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Chemical Phenomena
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Chemistry
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Dioxanes / metabolism
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Dioxanes / pharmacology
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Dopamine / metabolism
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Idazoxan
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Imidazoles / chemical synthesis
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Imidazoles / metabolism
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Imidazoles / pharmacology*
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Male
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Mice
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Muscle Contraction / drug effects
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Muscle, Smooth / physiology
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Norepinephrine / metabolism
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Rats
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Rats, Inbred Strains
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Receptors, Adrenergic, alpha / drug effects*
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Receptors, Adrenergic, alpha / physiology
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Serotonin / metabolism*
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Structure-Activity Relationship
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Tetrabenazine / antagonists & inhibitors
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p-Chloroamphetamine / antagonists & inhibitors
Substances
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Antidepressive Agents
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Dioxanes
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Imidazoles
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Receptors, Adrenergic, alpha
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Serotonin
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p-Chloroamphetamine
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Dopamine
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Norepinephrine
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Idazoxan
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Tetrabenazine