15958-86-8Relevant articles and documents
Synthesis and β1-, β2-adrenergic receptor binding studies of 4-acylamino-substituted phenoxypropanolamine and 5-acylamino-substituted naphthyloxypropanolamine derivatives
Jindal, Dharam Paul,Coumar, Mohane S.,Bruni, Giancarlo,Massarelli, Paola
, p. 654 - 663 (2007/10/03)
The object of this study was to investigate the β-adrenergic receptor binding affinity of 4-acylaminophenoxypropanolamine (10-15) and 5-acylaminonaphthyloxypropanolamine (21-24) derivatives, which were prepared from 4-amino-phenol (5) and 5-amino-1-naphthol (16), respectively. The in vitro β1- and β2-adrenergic receptor binding affinities of the newly synthesized compounds were assessed in turkey erythrocyte membrane (β1) and lung homogenates of rats (β2). The binding affinities were compared with that of propranolol (3) (propranolol hydrochloride, CAS 318-98-9). The compound N-[5-(3-tert-butylamino-2-hydroxy-propoxy)-naphthalen-1-yl]-acetamide (22) has β-adrenergic receptor affinity comparable with that of propranolol and shows selectivity to β1-adrenergic receptors.