Molecular aspects of the receptor activation by imidazolines: an overview.
Based on the pharmacological activity of chiral imidazolines the steric requirements for the activation of the alpha-adrenoceptor are provided. Importantly, the sequence of interaction of the critical groups of the asymmetric carbon of imidazolines and catecholamines with the alpha-adrenoceptor is postulated. Thus, initial determinants of molecular efficacy are hypothesized. The effect of aromatic fluoro-substitution and introduction of a double bond in the imidazoline moiety on the pharmacologic activity is discussed. The unique mechanism of non-adrenergic vascular activity of isothiocyanato-tolazoline is presented.
Patil
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PN
Ohio State University, College of Pharmacy, Division of Pharmacology, Columbus.
Feller
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DR
Miller
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DD
D000818:Animals; D002395:Catecholamines / Q000494:pharmacology*; D006801:Humans; D007093:Imidazoles / Q000494:pharmacology*; D011942:Receptors, Adrenergic, alpha / Q000187:drug effects / Q000502:physiology*; D013329:Structure-Activity Relationship; D013566:Sympathomimetics / Q000494:pharmacology*
D002395:Catecholamines; D007093:Imidazoles; D011942:Receptors, Adrenergic, alpha; D013566:Sympathomimetics