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Influence of lipophilicity and chirality on the selectivity of ligands for beta 1- and beta 2-adrenoceptors

el Tayar, Nabil
Testa, Bernard
Van de Waterbeemd, Hans
Kaumann, A. J.
Published in Journal of pharmacy and pharmacology. 1988, vol. 40, no. 9, p. 609-612
Abstract Eudismic and QSAR analyses are reported for the beta 1- and beta 2-adrenoceptor affinities and beta 1-selectivity of 10 enantiomeric pairs of ligands with only N-isopropyl or N-t-butyl groups. For both receptors, the eudismic index (ratio of affinity) increases with the affinity of the eutomers. However, the affinity of the distomers for the beta 2-adrenoceptor is relatively high, suggesting additional hydrophobic interactions. This is confirmed by various correlations between affinities and lipophilicities, showing that the affinity for beta 2-adrenoceptors is slightly more dependent on lipophilicity than that for beta 1-adrenoceptors. As a result, the beta 1-selectivity of the investigated beta 1-adrenoceptor ligands is strongly and negatively correlated with their lipophilicity (r = -0.942).
Keywords Adrenergic beta-Agonists/metabolismAdrenergic beta-Antagonists/metabolismChemistry, PhysicalLigandsLipidsPhysicochemical PhenomenaReceptors, Adrenergic, beta/*metabolismSolubilityStereoisomerism
PMID: 2907026
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EL TAYAR, Nabil et al. Influence of lipophilicity and chirality on the selectivity of ligands for beta 1- and beta 2-adrenoceptors. In: Journal of pharmacy and pharmacology, 1988, vol. 40, n° 9, p. 609-612.

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Deposited on : 2010-08-06

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