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Review
. 1991:34:187-94.
doi: 10.1007/978-3-7091-9175-0_24.

Molecular aspects of the receptor activation by imidazolines: an overview

P N Patil  1 , D R Feller, D D Miller
Affiliations
Review

Molecular aspects of the receptor activation by imidazolines: an overview

P N Patil et al. J Neural Transm Suppl. 1991.

Abstract

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.

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