Metabolic fate of carteolol hydrochloride (OPC-1085), a new β-adrenergic blocking agent. III. Autoradiographic distribution studies in mice.

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Abstract
Distribution of a new .beta.-adrenergic blocking agent, 3H-carteolol, was studied in mice by whole body autoradiography. The distribution of radioactivity was observed in all organs except the eyes and brain, with particularly high specific activities in the kidneys, liver, gall bladder and content in the intestines within a short time after either oral or i.v. administration. The radioactivity was then promptly eliminated from all tissues and organs, and excreted almost entirely in the urine and bile. Propranolol is known to be distributed at a high concentration in the brain; the concentration of (3H-) carteolol detectable in the brain was slight. In the adrenal gland, the radioactivity was localized in the medulla. Radioactivity was also detected in the stomach contents after the i.v. administration. The distribution of radioactivity in the fetus through the placenta was less than that in the major organs of the mother mouse, and the elimination of the activity was more rapid in the fetus than in mother. Carteolol and its metabolites do to some extent pass through the blood-brain barrier and placenta.