Showing papers in "Biochemical Pharmacology in 1975"

TL;DR: The relationships between 50 per cent inhibitory concentration and dissociation constants of the complex are shown for various mechanisms of inhibition, and several methods for the estimation of very low Ki, values are presented.

TL;DR: It was possible to conclude that, in the tissue slice system, an experimentally observed release was real, whereas a releasing action evoked an apparent inhibition of uptake equal in magnitude to the releasing action.

TL;DR: Adenosine deaminase (adenosine aminohydrolase, EC 3.5.4) has been purified about 3000-fold from human erythrocytes and Tubercidin (7-deaza- adenosine) and toyocamycin were devoid both of substrate and inhibitor activity.

TL;DR: Thiono-sulfur-containing compounds administered by intraperitoneal injection to untreated, phenobarbital-pretreated and 3-methylcholanthrene-pret treated adult male rats significantly decreased the concentration of cytochrome P-450 in the microsomes from each treatment group, and similar reductions in benzphetamine metabolism were seen.

TL;DR: The biphasic nature of the dissociation of the deaminase-coformycin complex (EI complex) indicates that the EI complex undergoes a slow conformational change, which is consistent with the known mechanisms of inhibitions by these inhibitors.

TL;DR: The pharmacokinetic modeling derived for the present purpose should be of general utility in the quantitation of enterohepatic recycling of drugs or metabolites whose loci of intended or untoward effects include the liver or gut.

TL;DR: Addition of methionine to the oral paracetamol dose protects against death and liver injury, and it is suggested that this may be a useful technique for making par acetamol safe against the danger of overdose.

TL;DR: Removal of solid food for 18 hr not only decreases hepatic aryl hydrocarbon hydroxylase activity in female rats, but also lowers the degree of inhibition by 7,8-benzoflavone.

TL;DR: In Europe, malnutrition leads to an increase in LOS and in hospital costs, both at the individual and the national level, both on the individual level and as percentage of national health expenditures.

TL;DR: A number of widely used antidepressants inhibit dopamine uptake by rat brain nuclei-free homogenates, suggesting the existence of two components responsible for the accumulation of 3H-dopamine into synaptosomal suspensions from whole brain.

TL;DR: Diclofenac sodium, the sodium salt of o-(2,6-dichlorophenylamino)-phenylacetic acid, is a potent inhibitor of sheep seminal vesicle prostaglandin synthetase in vitro.

TL;DR: Results from experiments in vitro and in vivo suggest that, while haloperidol has a direct effect on the dopamine receptor-associated cyclase activity, morphine must act by another mechanism, and that chronic use of either drug produces enhanced dopamine sensitivity.

TL;DR: The structure-activity relationships presented give some guidance for design of non-neurotoxic pesticides and more stable and less toxic alternatives to Mipafox as a selective inhibitor of neurotoxic esterase have been found.

TL;DR: It is concluded that the higher activities in the AA strain are due mainly to those aldehyde dehydrogenases of mitochondrial and microsomal fractions, which have K m -values for aldehydes in the millimolar range.

TL;DR: These results correlate reasonably well with previously determined results in more intact preparations and suggest that adenylate cyclase-coupled β-adrenergic receptors reflect the specificity of physiological β-adsensergic receptors.

TL;DR: The overall effect was to compress the time course in which ODC activity passed through its ontogenetic pattern; both the peak in activity and the drop to the characteristic low adult activity level occurred earlier and were accelerated.

TL;DR: Female rats were more susceptible to TCDD actions on liver microsomal PNP glucuronyltransferase than males, and actinomycin D appeared to block the initial phase of induction.

TL;DR: It is concluded that the carcinogen safrole leads to the biosynthesis of a 3-methylcholanthrene type cytochrome P-450 and formation of a safrole metabolite-cytochromeP-450 complex which in turn can be cleaved in vitro by safrole or other lipophilic compounds.

TL;DR: Ethanol and acetaldehyde inhibited the (Na + + K + )-activated ATPase activity of plasma membranes prepared from the guinea-pig heart by dose-dependent and antagonized by the K + concentration in the reaction mixture.

TL;DR: The results implicate the presence of a carrier-mediated transport mechanism for translocation of the drug into the cells, and suggest that drug resistance in these cells is due at least in part to impaired accumulation and binding of vincristine within the cell.