[Biotransformation of B 24/76 in the rat, minipig, dog and man].

After oral administration of B 24/76 (1) on experimental animals (rat, minipig, dog) and human beings 11 metabolites could be isolated from urine, faeces and bile. The structure of 7 compounds was elucidated by means of TLC and MS. The investigated species are showing an analogues metabolic pattern with differences in the intensity and main metabolites.

Subacute effects of propranolol and B 24/76 on isoproterenol-induced rat heart hypertrophy in correlation with blood pressure.

We compared the potential beta-receptor blocker, B 24/76 i.e. 1-(2,4-dichlorophenoxy)-3[2-3,4-dimethoxyphenyl)ethanolamino]-prop an-2-ol, which is characterized by beta 1-adrenoceptor blocking and beta 2-adrenoceptor stimulating properties with propranolol.

[The demonstration of proteolytic activity of bovine coronary arteries and the effect of drugs and other substances on it].

Intracellular neutral proteinases activity of bovine coronary arteries was demonstrated, isolated and partially characterized. The enriched crude enzyme preparation can be inhibited by diisopropylphosphofluoridate (DFP) and phenylmethylsulfonylfluoride (PMSF). The inhibitor concentration (pI50 values) by DFP and PMSF in the enzyme preparation and for trypsin are very similar.

Myosin isoenzymes in normal and hypertrophied human hearts.

Distinct myosin isoforms were identified from the ventricles and atria of foetal, normal and hypertrophied human hearts. Ventricle and atrium myosins cannot be differentiated by their sedimentation behaviour in the analytical ultracentrifuge, they vary, however, with regard to the Ca2+-dependent ATPase and also the activation parameters in measurements of the enzyme activity in dependence on temperature. In agreement with other authors we observed a foetal light chain in the ventricular tissue of the latter half of gestation, when myosin was characterized by SDS-polyacrylamide gel electrophoresis and isoelectric focusing.

[Renal excretion of dimethylphosphate and its thio-derivatives following application of dimethoate, bromophos, naled or trichlorfon to rats].

Dimethoate, bromophos, naled or trichlorophon were applied i.p. or p.

[Characterization of cyclic AMP-dependent protein kinase from smooth muscle of cattle and its modification by drugs].

Cyclic AMP-dependent protein kinase activity (ATP: protein phosphohydrolase, EC 2.7.1.

Acute and cutaneous toxicity of beta-chlorovinyl ketones and aldehydes in rodents.

The acute toxicity (LD50, intraperitoneal in the mouse) of beta-chlorovinyl ketones and aldehydes used as intermediates for organic syntheses was determined and their action on the skin of rodents investigated. Ketones of the type Cl-CH-CH-COR prove to be relatively toxic and display a markedly necrotic action after percutaneous absorption. In comparison with this the isomeric aldehydes Cl-CR-CH-CHO have a lower acute and less markedly cutaneous toxicity.

[Acute and subchronic experiments on the effects of microcrystalline cellulose on various pharmacological and biochemical parameters in mongrel rabbits].

The subchronic intravenous application of microcrystalline cellulose (MCC), in a dose of 5 mg/kg twice weekly for 10 weeks, resulted in servere crystal embolism in the lungs of the animals. The clinical parameters were either unchanged (erythrocyte and leucocyte counts, differential blood picture, osmotic resistance of the erythrocytes, total serum bilirubin, serum protein and serum protein fractions) or slightly pathological (hemoglobin content, hematocrit, GOT and GPT). The results from tests of the liver function (by means of bromosulphthaleine clearance) and of the renal function as well as the ophthalmologic examination were not indicative of damaged parenchyma or disturbed microcirculation.

[Correlations between chemical structure and cardiac effectivity of a group of beta-receptor blockaders].

13 compounds from the families of halogenated phenylethanolamines and phenoxypropanol-amines were tested for their antagonistic effect against an isoproterenol-induced increase in heart rate and lowering of blood pressure, and the AD50 values were determined. All the substances had beta-adrenolytical effects. 2.

Some properties of adenosine deaminase from vascular smooth muscle and its inhibition by various vasodilators.

Because of some uncertainties still existing about the role of adenosine deaminase in the drug-influenced adenosine breakdown, the authors isolated this enzyme from vascular smooth muscle and studied the inhibition of its activity by some vasodilating drugs. The adenosine deaminase was purified 360-fold from bovine carotid artery by means of (NH4)2SO4-precipitation, heat treatment, and gel filtration. This enzyme behaves in a similar way as preparations of the same enzyme from other tissues in respect to pH-dependence and Michaelis constant.

[The effect of diisopropylfluorphosphate on the adenylate cyclase activity and the 3',5'-AMP content of myocardium and brain].

Adenylate cyclase [ATP-pyrophosphatelyase (cyclizing) EC 4.6.1.

[Structure-activity relationships of halogenated phenylethanolamine and phenoxypropanolamine].

12 compounds from the series of halogenated phenylethanolamines and phenoxypropanolamines were tested at the isolated rabbit jejunum, and the pD2-and pA2-values were determined. All the substances act beta-adrenolytically. Except for 3,4-dichloronoradrenaline, which stimulates the alpha-receptors, all the compounds still have pronounced beta-mimetic effects.

[The effect of fluoridated phenylethanolamines on hyperglycemia induced by catecholamines in the rat].

10 compounds from the 2.4- and 3.4-difluorinated phenylethanol-amines series were tested for their antagonistic action against a hyperglycemia induced by catecholamines in rats, and the ED50 and AD50 values were determined.