Showing papers in "Biochemical Pharmacology in 1982"

TL;DR: A preliminary hypothesis is: in vivo alpha 1 is rapid in onset, short-lived, utilises internal Ca2+, prefers alkalosis and responds to short-term stimuli such as short bursts of nerve impulses or bolus injections of catecholamines; in vitro these categories of response occur but antagonists fail to define an alpha 1/alpha 2 split, suggesting that some critical factor is missing in vitro.

TL;DR: The fundamental role calmodulin plays in biology suggests that this calcium binding protein may provide a new site for the pharmacological manipulation of biological activity, and the inhibitors described hardly scratch the surface of this fertile area of research.

TL;DR: It is suggested that lysosomal alterations are an early and significant step in aminoglycoside-induced nephrotoxicity.

TL;DR: The results obrained indicate that lipid peroxidation is an important even in carbon tetrachloride hepatotoxicity, but that it appears to be only a subsequent event in bromobenzene toxicity, possibly occurring only as a result of glutathione depletion and cell death.

TL;DR: It is suggested that the stimulation and inhibition of insulin release by tolbutamide and diazoxide are due to their respective ability to decrease and to increase the K permeability of the B cell membrane.

TL;DR: It is shown that the first polypeptide to disappear in liver microsomes of phenobarbital-induced rats treated with CC14 was the 52,000 dalton p-450 cytochrome, which was capable of generating the trichloromethyl radical from CCl4 in a reconstituted system containing the purified cy tochrome, NADPH-cytochrome P-450 reductase, NAD PH, CCl 4, and the spin-

TL;DR: In contrast to 3-methylcholanthrene-type inducers, ethoxyquin and trans-stilbene oxide markedly induced GT1 reactions without affecting benzo[a]pyrene monooxygenase.

TL;DR: The results suggest that amphetamine may release [3H]DA by two mechanisms: (1) by accelerated exchange diffusion due to its use of the DA uptake carrier to enter into neurons (this would predominate at low concentrations of amphetamine), and (2) by passive entrance into neurons and displacement of [3h]DA from binding sites ( this would predomeinate at high concentrations of Amphetamine.

TL;DR: The results indicate the presence of non-mast-cell histamine, especially in the brain and stomach, where it may play important physiological roles.

TL;DR: The drug was producing a state of guanine deprivation was provided by high performance liquid chromatography analysis of acid-soluble extracts: a time-dependent fall in the concentrations of GMP and GTP ensued upon exposure to the drug; on the other hand, IMP concentrations increased by ∼15-fold.

TL;DR: The results suggest that release of [3H]DA by sympathomimetic amines may be a carrier-mediated process, and the rate-limiting step in ouabain-induced release may involve inactivation of an enzyme such as Na+K+-ATPase which is coupled to the transport of sodium.

TL;DR: The results demonstrate that inhibition of cellular DNA synthesis by cytosine arabinoside (ara-C) was significantly related to the extent of ara-C incorporation in DNA over a wide range of drug concentrations and times of exposure.

TL;DR: Evidence is presented for two functional forms of phenolsulphotransferase in human tissues: activity ratios, using dopamine and phenol as substrates, varied 30-fold between different tissues, whereas the dopamine to tyramine activity ratio was relatively constant.

TL;DR: A calcium antagonist, verapamil, enhanced the cellular uptake and cytotoxicity of vincristine (VCR) in adriamycin-resistant P388 leukemia (P388/ADM) cells and also enhanced the cells' cytot toxicity and cellular uptake of ADM in VCR- and ADM-resistant cells.

TL;DR: If injected intravenously 2 hr before the drug, a dose of more than 175 mg/kg body weight glutathione (0.57 mmol/kg) protected male mice from acute liver necrosis induced by intraperitoneal administration of paracetamol.

TL;DR: HI-6 was capable of reactivating soman-inhibited acetylcholinesterase when administered up to 30 min post-soman, indicating that the rate of aging of the somAn-acetyl cholinestersterase complex is slower than previously reported.

TL;DR: A variety of experimental observations are reported which strongly support the assumption that the warfarin binding site, or site I of human serum albumin, is better described as thewarfarin-azapropazone binding area, consisting of the overlapping binding sites for warfar in and azapropzone.

TL;DR: From results a reaction pathway could be derived which includes radical and carbanion intermediates as reactive precursors of CTE and CDE, respectively.

TL;DR: In general, acyclo-GDP had a lower V'max and a higher K'm than either GDP or dGDP, while none of these enzymes showed significantly higher rates of phosphorylation with GDP or acy Clovir diphosphate in herpes simplex virus-infected Vero cells as compared to uninfected Veros.

TL;DR: The generation of hydroxyl free radicals in the system consisting of purified NADPH-cytochrome P-450 reductase and anticancer quinone drugs, such as carbazilquinone, mitomycin C, aclacinomycin A and adriamycin, has been confirmed by two methods.

TL;DR: It is concluded that there is no correlation between the adrenoceptor agonist feature of noradrenaline and its stimulatory effect on Na,K-ATPase activity of rat brain homogenate and endogenous lipid peroxidation of considerable extent.

TL;DR: An attempt was made to identify those structural changes which ameliorate the cardiotoxic effects measured in other test systems while permitting the expression of antitumor properties.