Arzneimittel Forsch
-
Arzneimittel Forsch · Jan 1977
[Effect of the beta-adrenergic blocking agent bupranolol on the plasma renin activity in normotensive rats].
The effects of the beta-adrenergic blocking agent 3-tert.-butyl-amino-1-(6'-chloro-3'-methylphenoxy)-propan-2-ol hydrochloride (bupranolol; KL 255; Betadrenol) on the plasma renin activity (PRA) of normotensive rats were studied in comparison to propranolol. Bupranolol (10--100 microgram/kg) reduced basal PRA and inhibited the isoproterenol as well as dihydralazine induced increase of PRA in a dose dependent fashion. Bupranolol exhibited an effect 2--4 times stronger than that of propranolol. The PRA inhibiting effects of bupranolol seem to be linked to its beta-receptor blocking properties.
-
Arzneimittel Forsch · Jan 1977
The disposition of radioactivity after administration of the anthelminthic methyl-14C-5-cyclopropylcarbonyl-2-benzimidazole carbamate (ciclobendazole) to rats and dogs.
1. The disposition of radioactivity has been studied in rats and dogs after administration of a new anthelminthic agent, 14C-labelled methyl-5-cyclopropylcarbonyl-2-benzimidazole carbamate (14C-ciclobendazole). 2. An oral dose of 14C-ciclobendazole (4 mg/kg) to rats was rapidly absorbed and about 70% and 20% of the dose was excreted in the faeces and urine, respectively, during 2 days. ⋯ A comparison of the areas under the plasma concentration-time relationships after oral, i.p. and i.v. administration of 14C-ciclobendazole to rates indicated that there was no signigicant uptake by the liver during first pass and that an oral dose was well absorbed by rats. 7. The peak plasma concentration in the dog, after an oral dose of 14C-ciclobendazole (4 mg/kg) was reached at about 30 min and declined with a half-life of about 3 h. 8. Ciclobendazole was probably well-absorbed by rats and dogs and excreted more rapidly by the latter species than by the former Relatively higher plasma concentrations of drug and/or metabolites were thus achieved in rats than in dogs.