156833-28-2Relevant academic research and scientific papers
PYRIDINE COMPOUNDS AS SUBTYPE SELECTIVE MODULATORS OF ALPHA2B AND/OR ALPHA 2C ADRENERGIC RECEPTORS
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Page/Page column 14, (2010/08/18)
The invention relates specifically to the use of certain 4-[1-(1H-Imidazol-4-yl)-ethyl]-2,3-substituted pyridine compounds and pharmaceutical compositions thereof to treat disorders associated with selective subtype alpha 2 adrenergic receptor modulation.
Medetomidine analogs as α2-adrenergic ligands. 2. Design, synthesis, and biological activity of conformationally restricted naphthalene derivatives of medetomidine
Zhang, Xiaoyan,Yao, Xiao-Tao,Dalton, James T.,Shams, Gamal,Lei, Longping,Patil, Popat N.,Feller, Dennis R.,Hsu, Fu-Lian,George, Cliff,Miller, Duane D.
, p. 3001 - 3013 (2007/10/03)
A new series of naphthalene analogs of medetomidine have been prepared and evaluated for their α-adrenergic activities. The methylnaphthyl analog 5a showed significant selectivity for α2-adrenoceptors and behaved as a partial α1-agonist in rat aorta preparations. In contrast, the Z-ethylene analog 8c was α1-selective and behaved as a potent α1-antagonist. Two rigid analogs (6 and 7) exhibited large differences in binding affinities at α1- vs α2-receptors, indicating that the conformational flexibility of 5a is important for the fulfillment of the α-adrenergic activities. Molecular modeling studies began with conformational analysis of classical phenethylamines and medetomidine analogs. Superimposition of medetomidine conformations with those of phenethylamines provided a tentative explanation for the α2-adrenergic activity of the new imidazoles. A common binding mode for phenethylamines and imidazoles with α2-adrenoceptors is proposed. Knowledge of the biological properties of the 4-substituted imidazoles, integrated with the information derived from computer-assisted molecular modeling, has provided new insights for the structural and conformational requirements of this class as new adrenergic drugs.
A Structure-Activity Relationship Study of Benzylic Modifications of 4--1H-imidazoles on α1- and α2-Adrenergic Receptors
Hong, Seoung-Soo,Romstedt, Karl J.,Feller, Dennis R.,Hsu, Fu-Lian,Cupps, Thomas L.,et al.
, p. 2328 - 2333 (2007/10/02)
The naphthalene analog of medetomidine (1), 4--1H-imidazole (2), is a highly potent, selective α2-adrenoceptor agonist.We have initiated a structure-activity relationship study of the replacement of the methyl group on the
