Abstract
A number of imidazoline, imidazole and guanidinium compounds and other drugs were compared for their ability to bind to non-adrenergic idazoxan (imidazoline) I-receptors in particulate guinea pig cerebral cortex and ileum smooth muscle fractions. Radioligand binding with [3H]idazoxan was used for the experiments. Computer modelling of the binding data gave dissociation constants for drug binding to both I-receptors and alpha 2-adrenoceptors. Most drugs showed similar affinities for I-receptors in cortex and ileum. However, medetomidine stereoisomers as well as a few other drugs clearly delineated the I-receptors in cortex and ileum as different.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic alpha-Agonists / pharmacology*
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Adrenergic alpha-Antagonists / metabolism
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Animals
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Binding, Competitive
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Cerebral Cortex / drug effects
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Cerebral Cortex / metabolism*
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Dioxanes / pharmacology
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Guinea Pigs
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Idazoxan
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Ileum / metabolism
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Ileum / ultrastructure
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Imidazoles / metabolism
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Imidazoles / pharmacology*
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Kinetics
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Medetomidine
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Muscle, Smooth / metabolism
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Muscle, Smooth / ultrastructure
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Receptors, Adrenergic, alpha / metabolism
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Receptors, Drug / drug effects
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Receptors, Drug / metabolism*
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Stereoisomerism
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Tritium
Substances
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Adrenergic alpha-Agonists
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Adrenergic alpha-Antagonists
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Dioxanes
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Imidazoles
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Receptors, Adrenergic, alpha
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Receptors, Drug
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idazoxan receptor
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Tritium
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detomidine
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Medetomidine
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Idazoxan