Showing papers in "Biochemical Pharmacology in 1973"

TL;DR: The analysis described shows K I does not equal I 50 when competitive inhibition kinetics apply; however, K I is equal to I 50 under conditions of either noncompetitive or uncompetitive kinetics.

TL;DR: With the use of the method described in this publication, the metabolism of (—)− 3 H-NE released spontaneously from the rat vas deferens was studied and it accounted for 70 per cent of the total radioactivity.

TL;DR: A brain γ-aminobutyric acid (GABA) level increase has been observed after n-dipropylacetate (nDPA) treatment.

TL;DR: A greater difference was found between the sexes, the female rats of both strains having a more rapid ethanol oxidation and oxygen consumption, compared with the respective males, and the AA strain displayed a significantly lower level of acetaldehyde during ethanol oxidation than did the ANA strain.

TL;DR: The data suggest that inhibition of bacterial growth results from interference of DNA function by binding of silver ions along the helical chain.

TL;DR: The results suggest that the [ 3 H]amines are accumulated within specific neurons of brain tissue and that they are selectively released by amphetamine.

TL;DR: It is demonstrated that chloroquine in concentrations around 1–2 × 10−5 M strongly interferes with mucopolysaccharide degradation in the living cell and electron microscopy shows that a morphological picture resembling a lysosomal storage disease develops in these cells after less than 2 days exposure to the drug.

TL;DR: Evidence is presented that, although M-6-G was a highly polar conjugate, it can penetrate the blood brain barrier and react with the receptor of analgesic action without prior hydrolysis of the glucuronide linkage.

TL;DR: The ability of 4-chloroamphetamine to inhibit the high affinity uptake of serotonin by synaptosomes and to release serotonin from synaptoomes is probably related to the prolonged lowering of brain serotonin levels in rats treated with 4- chloroamphetamine.

TL;DR: In this paper, Salsolinol and tetrahydropapaveroline (THP) were found to be competitive inhibitors of dopamine O-methylation in vitro, their calculated inhibitor constants (ki values) being 0.13 and 0.02 mM respectively.

TL;DR: The kidney clearance of Ara-C exhibits essentially the same variation with body weight as inulin, and the model is physiologic and permits the incorporation of chemical reactions in appropriate anatomic sites with kinetic characteristics of their local environment.

TL;DR: A relationship was found between the formation of lipid peroxides and the activities of drug-metabolizing enzymes in liver microsomes of rats and addition of EDTA to the incubation mixture produced marked changes in the Michaelis constants ofdrug-metabolic enzymes and in inhibition constants of SKF 525-A.

TL;DR: It is proposed that the diabetogenic action of streptozotocin is related to decrease in pancreatic beta cell pyridine nucleotide concentrations resulting from the combination of reduced tissue uptake of precursors and a decrease in synthesis of NAD.

TL;DR: A good correlation was found between the ability of a given analog to displace 3H-colchicine from rat brain microtubule protein and its antimitotic or antigout properties.

TL;DR: It is suggested that N -acetylation is not required for carcinogenesis of the urinary bladder and that the expression of urinary bladder or hepatocarcinogenicity by arylamines and arylacetamides in a given experimental system may depend on the quantitative ability of the species being studied to utilize pathways for the interconversion of aRYlacetamide derivatives and aRYlamine derivatives.

TL;DR: It was confirmed that at least one N -methyl group was necessary for anti-cancer activity but there was no correlation between dealkylation by liver microsomes and activity since a diethyl triazene was readily dealksed but not active.

TL;DR: The decrease during pregnancy of hepatic glucuronyl transferase is attributed to competitive inhibition by high levels of endogenous estrogenic and progestational steroids, but the decrease in the activities of the microsomal hydroxylating enzymes is attributed in part to the decreases in P-450, which may result from highlevels of growth factors.

TL;DR: Olivetol, which represents a partial structure for all of the compounds tested, showed high activity, indicating that the inhibitory power of the cannabinoids resides in the aromatic portion of the molecule.

TL;DR: It is concluded that under the conditions used, measurement of release of newly absorbed 5-HT is a reasonably good measure of the release of endogenous 4-HT, indicating that newly absorbed5-HT behaves like endogenous 5- HT, except for a slight tendency to be more easily released.

TL;DR: Findings suggest that control mechanisms can maintain uridine nucleotide levels in a normal range, even in the presence of strong inhibitors of de novo UMP biosynthesis.

TL;DR: It is suggested that the behavioural effects of haloperidol might in part be due to actions on the metabolism of GABA and glutamate, and interaction of TSC with glutamate metabolism might be a factor in seizure-provoking activity of the drug.

TL;DR: In guinea-pigs treated with phenobarbitone 50 mg/kg for up to 5 days a highly significant correlation (r = 0.61, P) is found between the levels of these drugs and survival in animals treated with these drugs.

TL;DR: The results indicate that changes in brain serotonin metabolism are associated with both the acute effects of morphine and with morphine tolerance, as indicated by the rate of accumulation of 5-HIAA after administration of probenecid and an increase in turnover of serotonin after treatment with pargyline.

TL;DR: Bovine adrenal glands responded to single injections or continuous infusions of aminophylline by increased release of catechoiamines, but this effect was not mediated by the release of acetylcholine in the gland, since it was not blocked by cholinergic blocking agents.

TL;DR: There was, however, an increase in GAD activity, but no change in GABA-T activity or the rate of disappearance of 3 H-GABA, suggesting that these effects may be due to an action of ethanol on the metabolic pool of GABA as distinct from the transmitter pool.

TL;DR: It must be concluded that CBD, which is by far more potent in inhibiting drug metabolism than other cannabinoids, contributes significantly to the effects of crude cannabis preparations at least in rodents.