Biomedical subjects

B V Lap

Publications and source records attributed to B V Lap.

3 recordsLinked to original sources

PubMed1979

beta-Adrenergic blocking action of halonitrophenethanolamines.

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.

2-Hydroxyphenethylamine↗

PubMed1978

2-Methoxyphenylethanolamines, potential beta-adrenergic blocking agents.

The effect of the introduction of a 2-methoxy substituent on the beta-adrenergic antagonistic properties of a series of 3- and 4-substituted phenylethanolamines (1) was studied. Both the series of bromo- and methyl-substituted compounds behaved similarly, indicating that electronic forces are not significant in determining beta-adrenergic antagonist activity. When compared with the corresponding phenylethanolamines without a 2-methoxy substitutent, the 2-methoxy-4-substituted derivatives (3a and 3d) had enhanced potency and selectivity but the 2,3- (3b and 3e) and the 2,5-disubstitution patterns (3c and 3f) showed a loss of activity. The inconsistent changes in activity prevented any firm conclusions being made about the effect of the ether oxygen and the beta-adrenoceptor antagonistic activity of phenoxypropanolamines.

Adrenergic beta-Antagonists↗

PubMed1977

The beta-adrenergic activity of some monosubstituted phenethanolamines.

A series of monosubstituted phenethanolamines with N-isopropyl and N-tert-butyl substituents has been prepared. A detailed pharmacological study has been made of the beta-adrenergic activity of these materials as the nitrogen substituent and the nature and position of the phenyl substituent were changed, and their selectivity has been determined for beta1- and beta2-adrenoceptors in guinea-pig and cat tissues.

Animals↗