Beta-Adrenergic blocking action of halonitrophenethanolamines
Letts, L.G.; Easson, P.A.; Temple, D.M.; Williams, L.R.; Pasaribu, S.J.; Lap, B.V.; Lim, C.H.
Archives Internationales de Pharmacodynamie et de Therapie 238(1): 105-113
1979
ISSN/ISBN: 0003-9780 PMID: 39529 Document Number: 142813
A series of phenethanolamines with N-isopropyl and N-tertbutyl substituents and ring-substituted with nitro- and halogen groups has been prepared. Using guinea-pig isolated atrial and tracheal preparations, the influence of the nitro-group on the beta 1- and beta 2-antagonist actions of the mono-halogen compounds was determined, and the antagonist and partial agonist effects of the halo-nitro-compounds on beta-adrenoceptors in these tissues measured to help elucidate structure-activity relations in this series. The halonitro compounds did not show enhanced activity compared with the mono-halogen substituted analogues. Several of the new compounds showed slight but significant beta 2-antagonist selectivity of action, and one compound was significantly beta 1-selective.