Biologic actions and pharmacokinetic studies of auranofin.

The preclinical profiles of auranofin (Ridaura), an oral chrysotherapeutic agent, parenteral gold sodium thiomalate, gold thioglucose, and their respective ligands were compared. Auranofin was more effective than gold sodium thiomalate in suppressing inflammation and stimulating cell-mediated immunity. In contrast to gold sodium thiomalate and gold thioglucose, auranofin inhibited cellular release of lysosomal enzymes, antibody-dependent cellular cytotoxicity, production of antibodies in adjuvant arthritic rats, and antibodies involved in cytotoxicity reactions.

Pharmacokinetics of auranofin in animals.

Gold from orally administered auranofin (AF) was absorbed 17-23% in rats and 15-38% in dogs. Gold was highly bound to blood cells and plasma proteins. Gold terminal half life was 1.

Metabolism of 7,8-dichloro-1,2,3,4-tetrahydroisoquinoline, a phenylethanolamine N-methyltransferase inhibitor. II. Species difference in metabolism and synthesis of its metabolites.

1. 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline (DCTQ), a potent reversible inhibitor of phenylethanolamine N-methyltransferase, was well absorbed, readily metabolized and excreted mainly in urine. 2.

Correlation of [14C]muscimol concentration in rat brain with anticonvulsant activity.

Muscimol, an in vivo and in vitro GABA agonist, has anticonvulsant activity against bicuculline-induced seizures when given systemically to rats. To determine whether parent compound or a metabolite possessed the anticonvulsant activity, experiments were performed with [14C]muscimol. Anticonvulsant activity was determined by the percent of animals protected against tonic forelimb extension induced by bicuculline.