Louis L. Radulovic

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Gabapentin, an analog of gamma-aminobutyric acid, exhibits anticonvulsant properties in both animal models and humans. Gabapentin pharmacokinetics was studied in laboratory animals using HPLC and radiometry. Oral bioavailability was 40% in monkeys administered 25 mg/kg, 79% in mice and rats receiving 50 mg/kg, and 80% in dogs administered 50 mg/kg. Binding(More)
Pregabalin has shown clinical efficacy for treatment of neuropathic pain syndromes, partial seizures, and anxiety disorders. Five studies in healthy volunteers are performed to investigate single- and multiple-dose pharmacokinetics of pregabalin. Pregabalin is rapidly absorbed following oral administration, with peak plasma concentrations occurring between(More)
UNLABELLED Gabapentin (GBP) is a non-metabolized, non-plasma protein bound, renally excreted antiepileptic drug that is actively absorbed via the system L amino acid transporter. Previous studies have demonstrated that gabapentin displays dose-dependent absorption. OBJECTIVES These studies were conducted to determine inter- and intra-subject variability(More)
Pregabalin (Lyrica) is a novel amino acid compound that binds with high affinity to the alpha2-delta (alpha2-delta) auxiliary protein of voltage-gated calcium channels. In vivo, it potently prevents seizures, pain-related behaviors and has anxiolytic-like activity in rodent models. The present studies were performed to determine the profile of pregabalin(More)
Single-dose administration of 50 mg of 1-[2-[bis[4- (trifluoromethyl)phenyl]methoxy]ethyl]-1,2,5,6-tetrahydro-3- pyridinecarboxylic acid monohydrochloride resulted in temporary neurological and psychological symptoms in two subjects. Because of the nature of adverse effects, urine from a subject who received CI-966 orally was extracted to investigate the(More)
Objectives: CI-994 (N-acetyl dinaline, PD123654) is a novel oral agent active in a broad variety ofmurine and human tumor xenografts. While cytotoxic in theBrown Norway (BN) rat leukemia model, growth inhibition inother murine and human tumor xenografts is predominantlycytostatic. Its specific mechanism of action remains unknown.Following CI-994(More)
Biotransformation of theobromine (TBR) was compared in rats, mice, hamsters, rabbits, and dogs by assaying urinary metabolites using HPLC after oral administration of a 5 mg/kg dose containing 8-14C-TBR. Recovery of radioactivity ranged from 60-89% of the dose in urine, and from 2-38% of the dose in feces, with most material being excreted during the first(More)
1. Previous studies have demonstrated the presence of glutathione S-transferases in the skin of rodents and humans. This study represents the first attempt to purify cytosolic glutathione S-transferases from skin of 3-day-old rats. 2. A partial purification of the enzyme was achieved by a two-step procedure: affinity chromatography followed by HPLC. Two(More)
A specific and highly sensitive method for the measurement of CI-979 in human plasma is described. The compound and internal standard were extracted from alkalinized plasma with methyl tert.-butyl ether and analyzed by capillary gas chromatography with nitrogen-selective detection. The method was demonstrated to be accurate and precise. Since the limit of(More)