Scott Clemans

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After arildone administration, four compounds were identified in the excreta of laboratory animals: unchanged drug, arildone; the O-desmethyl metabolite, 4-[6-(2-chloro-4-hydroxy)phenoxy]hexyl-3,5-heptanedione; the sulfate ester of 2-chloro-4-methoxyphenol; and a labile conjugate of chlorohydroquinone, tentatively characterized as the sulfate ester. The(More)
A gas chromatograph-mass fragmentography method for simultaneous assay of 17-monochloroacetyl-ajmaline (MCAA) and its hydrolysis product, ajmaline, is described. Recovery of both compounds from whole blood averaged 71%. About 5% of MCAA was hydrolyzed during the assay procedure. The method was accurate and precise to within a few percent. It was suitable(More)
The disposition of quinfamide 1-(dichloroacetyl)-6-(2-furoyloxy)-1, 2, 3, 4-tetrahydroquinoline, an enteric anti-amoebic agent, was studied in the rat. A peak blood level equivalent to 2.3 micrograms/ml of quinfamide was observed at 7 hr following a 20 mg/kg oral dose. Urinary recovery of radioactivity was much higher (84%) following intravenous than oral(More)
The synthesis and gastric antisecretory activity of a series of indole-1-alkanamides and pyrrole-1-alkanamides are presented. A marked elevation of the pH of the gastric secretions of the rat was observed after oral administration of 100 mg/kg of 2,3-dimethylindole-1-acetamide (2), -1-propionamide (8), and -1-butyramide (13). Replacement of either methyl(More)
A sensitive and specific radioimmunoassay of dog and human plasma pentazocine is described. Rabbit antiserum and the second antibody method separated bound from free pentazocine. The radioimmunoassay employed an 125I-labeled radioligand and required extraction from the sample prior to quantitation. The method had a detection limit of approximately 200(More)
N-(1, 1-Dimethylethyl)-N'-[2-(4-pyridinyl)-4-pyrimidinyl]urea, Win 40, 882, was eliminated from the blood stream of dogs by two apparent first-order processes with alpha- and beta-phase half-lives of 0.2 hr and 1.4 hr, respectively. Radioactivity of the administered dose was excreted by rats in the feces and via the kidneys; about 40-45% of the dose was(More)
The metabolism of trilostane, a novel inhibitor of adrenal steroidogenesis, was studied in the rat and monkey. In the rat, a peak blood level, equivalent to 2 microgram/ml of trilostane, was observed following a 25 mg/kg oral dose; excretion was mainly via the feces. In the monkey, the peak plasma level, equivalent to 15 microgram/ml, was observed 2 hr(More)
The biotransformation of 14C-amrinone was studied in rats, dogs, and monkeys by automated gradient high-performance liquid chromatography. The major pathways of metabolism elucidated are: A) glucuronidation at the primary amino nitrogen atom and/or the enolized oxygen atom of the pyridone ring; B) addition of glutathione at the pyridone 2-position and(More)