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Binding and functional affinity of some newly synthesized phenethylamine and phenoxypropanolamine derivatives for their agonistic activity at recombinant human β3‐adrenoceptor
Thirteen new compounds have been evaluated for their potencies and efficacies asβ3‐adrenoceptor agonists on human β3‐ adrenoceptor expressed in COS‐7 and Chinese hamster ovary (CHO) cells using radio ligand binding assay and cyclic AMP (cAMP) accumulation assay. Expand
Molecular characterization of pharmacological properties and selectivity of SWR-0315NA for beta3-adrenoceptors.
Results indicate that although SWR-0315NA has lower binding selectivity towards beta-AR subtypes, it is a selective agonist with high intrinsic activity for beta(3)-AR as compared with (-)-isoproterenol. Expand
Structure-activity relationship studies of phenoxypropanolamine derivatives for beta 3-adrenergic activity.
This study evaluated the structural modification of the parent SWR-0342SA and their effects on the binding affinities as well as functional activities of these derivatives using COS-7 cells and CHO cells expressing human beta 1, beta 2, beta 3-AR and only beta3-AR respectively. Expand
Comparison of the binding affinity of some newly synthesized phenylethanolamine and phenoxypropanolamine compounds at recombinant human β‐ and α1‐adrenoceptor subtypes
Six new compounds were evaluated and the binding affinities for human α1‐adrenoceptors expressed in Chinese hamster ovary (CHO) cells were compared using a radioligand‐binding assay to confirm the finding of this manuscript that this phenoxypropanolamine group of β2‐phenyl‐2‐hydroxyethyl ligands could also be used as α1-adrenOceptor ligands. Expand