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Showing papers in "Biochemical Pharmacology in 1978"


Journal ArticleDOI
TL;DR: It is concluded that spiperone is a more suitable ligand than haloperidol for studying the neuroleptic receptors.

522 citations




Journal ArticleDOI
TL;DR: The usefulness of the concept of the existence of two functionally distinct forms of the enzyme is assessed, without exploring the possible nature of any such forms.

234 citations


Journal ArticleDOI
TL;DR: The possible involvement of mono-oxygenase in biotransformation in methoxychlor into estrogenic metabolites in vivo is discussed and the demethylated products were resolved by thin-layer chromatography into three chromatographically distinct components more polar than methoxy chlor.

223 citations


Journal ArticleDOI
TL;DR: Hepatocytes isolated from mouse and rat catalyzed the formation of glucuronide, sulphate, glutathione and cysteine conjugates of paracetamol, which was directly correlated with loss of intracellular glutATHione (GSH) and induced rate was only half of that in hepatocytes from control mouse.

218 citations


Journal ArticleDOI
TL;DR: These anthracycline-resistant cell lines are resistant by virtue of decreased retention of the drugs, particularly for adriamycin and daunorubicin.

214 citations


Journal ArticleDOI
TL;DR: A role for VIP as a neuromodulatory or neuro-transmitter compound in the central nervous system, (CNS), mediating its action through the adenylate cyclase/cAMP system is supported.

175 citations


Journal ArticleDOI
TL;DR: In the rat, phenylethylamine and dopamine are both substrates for a deprenyl-resistant enzyme with a distribution similar to BzAO, but in man these amines are solely oxidized by MAO, and Semicarbazide, procarbazine and carbidopa are potent inhibitors of BzO and inhibit it selectively, leaving MAO substantially unaffected.

174 citations


Journal ArticleDOI
TL;DR: It is concluded that spiperone is a ligand of choice for in vivo studies of neuroleptic receptors because it correlates with the distribution of neuroLEptic receptors when measured under in vitro conditions.

168 citations


Journal ArticleDOI
TL;DR: Encapsulation resulted in a large increase in the total amount of drug equivalents retained by the tissues at various times after injection, with tissues rich in reticuloendothelial cells, such as liver and spleen, being the favored sites of uptake.




Journal ArticleDOI
TL;DR: It is suggested that the relative inefficiency of aminoglycoside antibiotics to act against intracellular bacteria is due to the acid pH prevailing in lysosomes, which depress the antibacterial activity of these drugs and defeat their accumulation in those organelles.

Journal ArticleDOI
TL;DR: It is concluded that the GSH S-transferase system is inducible, but in contrast to the induction of the mixed function oxidase system, qualitative differences between the inducing effects of PB and MC were not observed.

Journal ArticleDOI
TL;DR: It appears that genetically hypertensive rats, particularly the SHR-SP substrain, have a defect in taurine metabolism, and that this may be related to the severity of hypertension.



Journal ArticleDOI
TL;DR: It is suggested that inhibition of thymidylate synthetase activity by endogenously synthesized 5-fluoro-2′-deoxyuridylic acid is a possible mechanism by which5-fluorocytosine exerts its antifungal effect.

Journal ArticleDOI
TL;DR: The transport of DNR, ADR, and RBD was studied in Ehrlich ascites tumour cells in vitro, indicating a carrier mediated inward transport mechanism and a high structural specificity for influx.

Journal ArticleDOI
TL;DR: Experiments with horseradish peroxidase, beef liver catalase and inorganic catalysts of H 2 O 2 decomposition indicate that the elemental mercury atom serves as an electron donor for complex I ofCatalase which is formed from the first reaction of catalases with H 2O 2 .

Journal ArticleDOI
TL;DR: The results indicate that reduced metronidazole causes a loss of DNA helix content, strand breakage, and a concomitant impairment of its function as an enzyme template which may be due to the presence of altered bases or a drug-base complex.


Journal ArticleDOI
TL;DR: A close relationship was observed between the cellular content of glutathione (GSH) and glucose utilization, and induction of a peroxidative metabolism within these cells, coupled with glucose oxidation, appears to be a major effect of insulin.

Journal ArticleDOI
TL;DR: A structure-activity relationship study has revealed the importance of the aromatic ring and the optimum length of the chain between the aromatic rings and the nitrogen for the selective inhibition of MAO-B and HCl seems to be the most promising selective inhibitor.


Journal ArticleDOI
TL;DR: The results are suggestive of a possible role for l -glutamic acid in the nervous system during ethanolism and the post-withdrawal reaction.

Journal ArticleDOI
TL;DR: A relationship is shown between the ulcerogenicity of NSAI drugs and the inhibitory effects on gastric mucus biosynthesis, and aspirin stimulates the incorporation of [ 35 S]sulphate into intestinal mucus glycoproteins.

Journal ArticleDOI
TL;DR: Comparison of uptake inhibitors as antagonists of PCA is strongly influenced by the pharmacokinetics of the drugs involved.