GS 015-14C was synthetized from [1-14C]-chloracetic acid and 3-carbethoxyamino-10,11-dihydro-5H-dibenz[b,f]azepine. The whole radioactivity yield passing all synthesis stages was 32% at a radiochemical purity of more than 98%.
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The antiarrhythmic action of GS 015 was studied in proportion to its plasma concentrations ascertained in parallel, making use of the model of the two-step coronary ligature in the conscious dog. Blood levels of 1.0 microgram/ml (2 mg/kg i.
View Article and Find Full Text PDFThe antiarrhythmic action of GS 015 was studied proportionally to its plasma concentrations ascertained in parallel, using the model of the electrofibrillation of the cat's heart. Blood levels of about 1.3 micrograms/ml after i.
View Article and Find Full Text PDFExcretion, blood level, distribution, and metabolite samples were studied on the rat after application of GS 015 marked by 14C. The compound is quickly and completely absorbed and metabolized from an aqueous solution. The marked substances form a broad blood level maximum, at the occasion of which a main metabolite distinguishes itself apart from the initial compound at first provable yet.
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