Fendosal (200 mg) was given orally to each of two separate groups of twelve healthy male volunteers on separate occasions to assess the influence of food or antacid on the bioavailability of fendosal. Blood samples (20 ml) were drawn during 12 hours post-dosing and fendosal plasma concentrations were quantitated by a validated fluorescence technique. Food was shown to have no significant effect (p greater than 0.05) on fendosal bioavailability. However, the bioavailability of fendosal in the presence of an antacid was reduced by 80 per cent. In vitro studies suggested that a complexation between unionized fendosal and the metal ions contained in the antacid may be responsible for the decrease in the rate and extent of absorption observed in vivo.

Adult↗

PubMedDate not supplied

Quinoline esters as potential antimalarial drugs: effect on relapses of Plasmodium cynomolgi infections in monkeys.

Two compounds of the quinoline ester series, WR 197236 (6-butyl-4-hydroxy-3-methoxycarbonyl-7-beta-phenoxyethoxyquinoline ) and WR 194905 (4-acetoxy-6-decyloxy-7-isopropoxy-3-methoxycarbonylquinoline++ +), exhibit anti-relapse activity against sporozoite-induced Plasmodium cynomolgi B infections in rhesus monkeys. Both the compounds have been found to be curative when given intramuscularly in 7 daily doses of 15 mg/kg, and no relapses were observed during the observation period of 120 d.

Animals↗

PubMedDate not supplied

Effect of aging on cyclic AMP levels and adenylate cyclase and phosphodiesterase activities in the rat corpus striatum.

Cyclic AMP levels and activities of adenylate cyclase and phosphodiesterase in the striatum were measured in 4, 12, 24 and 30 month-old rats. No age-related changes were observed either in cyclic AMP levels or basal adenylate cyclase activity. However, there was an age-related decline in dopamine sensitivity of adenylate cyclase without affecting NaF-induced stimulation. There was also an age-dependent decrease in phosphodiesterase activity at low substrate concentrations (3 X 10(-7) and 3 X 10(-6) M) but not at high substrate concentrations (3 X 10(-5) and 3 X 10(-4) M). These results suggest that the functions of dopaminergic neurons may have been altered by aging.

Adenylyl Cyclases↗

PubMedDate not supplied

Relationship between levels of cyclic nucleotides and gamma-aminobutyric acid during ethanol withdrawal in rats.

Cyclic nucleotide and gamma-aminobutyric acid (GABA) levels were measured in four brain areas of control rats and rats undergoing ethanol withdrawal. Cyclic adenosine 3',5' monophosphate (cyclic AMP) was increased in the cerebral cortex and pons-medulla oblongata; cyclic guanosine 3',5'-monophosphate (cyclic GMP) was increased in the cerebellum and cerebral cortex; and GABA was decreased in the cerebellum, subcortex and pons-medulla oblongata. Individual values in withdrawn animals were correlated and subjected to a factor analysis. One of the common factors identified by this analysis was important for all but one of the levels which changed during ethanol withdrawal. Significant correlations of levels correlated with this factor included a negative correlation between cyclic GMP and GABA levels in the cerebellum, a positive correlation between cyclic GMP levels in the cerebellum and cyclic AMP levels in the pons-medulla oblongata and a positive correlation between cyclic AMP levels in the pons-medulla oblongata and cerebral cortex. These results indicate that multiple brain areas and neurotransmitters are involved in ethanol withdrawal.

Alcoholism↗