2,2'-dialkoxybenzhydrylamides and 2,2'-dialkylbenzhydryl esters of N,N-edisubstituted alpha-amino acids. Synthesis and pharmacological evaluation.
Explore the source record for details and available documents.
Biomedical subjects
Publications and source records attributed to A Novelli.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
Explore the source record for details and available documents.
beta-adrenergic receptors (beta-ARs) were identified in CG-5 breast cancer cells using a radiometric assay. The total beta-AR concentration was measured using the highly potent beta-adrenergic antagonist (-)[3H]CGP 12177, and the densities of beta-AR subtypes were discriminated in the presence of highly selective unlabelled ligands (CGP 20712A and ICI 118551). Scatchard analysis revealed good linearity (r > 0.95) and Kd values (0.05-1 nM) indicated the presence of high affinity binding sites in CG-5 cell membranes. beta 2-AR concentrations (74%) were significantly (P < 0.05) higher than beta 1-AR concentrations (36%). Displacement studies indicated that tested adrenergic agonists displaced (-) [3H]CGP 12177 from its specific binding sites in the order of potency (-)isoproterenol > (+/-)clenbuterol > (-)adrenaline > (+/-)dobutamine > > (-)noradrenaline, whereas beta-adrenergic antagonists inhibited the binding in the following order of potency: (-)propranolol > > ICI 118 551 > > CGP 20712A. The functionality of beta-ARs identified in CG-5 cell membranes was demonstrated by the significant increase in cAMP production induced by different concentrations of isoproterenol vs unstimulated cells (control). The pathophysiological role of beta-ARs in breast cancer cells is still undefined, but their presence suggests the possible adrenergic regulation of some cellular activities such as proliferation and/or differentiation.
Explore the source record for details and available documents.