The object of this study was to Investigate the beta-adrenergic receptor binding affinity of 4-acylaminophenoxypropanolamine (10-15) and 5-acylaminonaphthyloxypropanolamine (21-24) derivatives, which were prepared from 4-aminophenol (5) and 5-amino-1-naphthol (16), respectively. The in vitro beta(1)- and beta(2)-adrenergic receptor binding affinities of the newly synthesized compounds were assessed in turkey erythrocyte membrane (beta(1)) and lung homogenates of rats (beta(2)). 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 beta-adrenergic receptor affinity comparable with that of propranolol and shows selectivity to beta(1)-adrenergic receptors
Jindal, D.P., Coumar, M.S., Bruni, G., Massarelli, P. (2002). Synthesis and beta1-, beta2-adrenergic receptor binding studies of 4-acylamino substituted phenoxypropanolamine and 5-acylamino substituted naphthyloxypropanolamine derivatives. ARZNEIMITTEL-FORSCHUNG, 52(9), 654-663.
Synthesis and beta1-, beta2-adrenergic receptor binding studies of 4-acylamino substituted phenoxypropanolamine and 5-acylamino substituted naphthyloxypropanolamine derivatives
BRUNI, GIANCARLO;MASSARELLI, PAOLA
2002-01-01
Abstract
The object of this study was to Investigate the beta-adrenergic receptor binding affinity of 4-acylaminophenoxypropanolamine (10-15) and 5-acylaminonaphthyloxypropanolamine (21-24) derivatives, which were prepared from 4-aminophenol (5) and 5-amino-1-naphthol (16), respectively. The in vitro beta(1)- and beta(2)-adrenergic receptor binding affinities of the newly synthesized compounds were assessed in turkey erythrocyte membrane (beta(1)) and lung homogenates of rats (beta(2)). 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 beta-adrenergic receptor affinity comparable with that of propranolol and shows selectivity to beta(1)-adrenergic receptorsFile | Dimensione | Formato | |
---|---|---|---|
Arzneim.Forsch 2002, 654-663.pdf
non disponibili
Tipologia:
Post-print
Licenza:
NON PUBBLICO - Accesso privato/ristretto
Dimensione
3.11 MB
Formato
Adobe PDF
|
3.11 MB | Adobe PDF | Visualizza/Apri Richiedi una copia |
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
https://hdl.handle.net/11365/8221
Attenzione
Attenzione! I dati visualizzati non sono stati sottoposti a validazione da parte dell'ateneo