Drugs online research references
J Colloid Interface Sci. 1996 Dec 25;184(2):658-62.
Self-Association of Phenothiazine Drugs: Influence of the Counterion on the Mode of Association
Attwood D, Mosquera V V, Lopez-Fontan JL, Garcia M, Sarmiento F.
Department of Pharmacy, University of Manchester, Manchester, M13 9PL, United Kingdom
The association characteristics of the phenothiazine drug trimeprazine tartrate in water and aqueous electrolyte solution have been examined using static and dynamic light scattering techniques and compared with those reported for the structurally related drug promethazine hydrochloride, to identify differences in association pattern arising from differences in the counterions of the two drugs. The association of trimeprazine tartrate was micellar in water and in the presence of added electrolyte. A progressive increase of aggregation number and micellar radius was observed with increase of sodium chloride concentration over the range 0.05 to 0.60 M NaCl. This behavior is in contrast to that of promethazine hydrochloride which exhibits continuous association above the critical concentration in electrolyte of concentrations >/=0.2 M NaCl. Moreover, static light scattering curves for trimeprazine tartrate showed a single discontinuity corresponding to the onset of micellization, whereas the association behavior of promethazine hydrochloride (and other phenothiazine drugs with chloride counterions), in water and dilute electrolyte (0.05-0.1 M NaCl), is complex, with discontinuities in solution properties at several critical concentrations. The results of this study highlight the influence of the counterion on the association characteristics of this class of amphiphile.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8978571&dopt=Abstract [PubMed - as supplied by publisher]
J Environ Pathol Toxicol Oncol. 1996;15(1):41-50.
Effect of hexavalent chromium on drug-metabolizing enzymes in male domesticated rabbits.
Anjum F, Shakoori AR, Gorrod JW.
Department of Zoology, University of the Punjab, Lahore, Pakistan.
We studied the effect of chromium on the drug-metabolizing enzymes (DME) in male New Zealand white rabbits, Oryctolagus cuniculus, with and without pretreatment with phenobarbitone (PB) and promethazine (PM). The activities of cytochrome P-450 (183%), aniline hydroxylase (ANH, 265%), acetanilide hydroxylase (ACH, 160%), benzphetamine demethylase (BD, 112%), aminopyrine demethylase (AD, 97%), N,N,-dimethyl aniline demethylase (DAD, 72%), and cytochrome-c-reductase (100%) were increased after PB treatment. The activities of cytochrome b5 and N,N,-dimethyl aniline N-oxide (DAO) were, however, decreased 79% and 47%, respectively. Most of the DME remained unaffected after PM treatment except for the increase in ANH (55%), ACH (56%), and BD (16%). Potassium dichromate administered to rabbits at a dose of 8 mg/kg body weight/day for 5 days resulted in an increase in the activities of ANH (108%), BD (76%), AD (25%), and DAD (49%), while that of cytochrome b5 and DAO were inhibited 81 and 77%, respectively. There was no effect on the activities of cytochrome P-450, ACH, and cytochrome-c-reductase. Chromium, administered to PB-pretreated animals decreased the activities of ANH (41%), ACH (35%), BD (34%), AD (30%), DAD (51%), cytochrome-c-reductase (72%), and DAO (62%). Other enzymes remained unaffected. When administered to PM-pretreated animals, the activities of ANH, BD, AD, and DAD increased 34, 69, 24 and 54%, respectively, whereas activities of cytochrome b5 and DAO were decreased 96 and 68%, respectively. All other DME remained unaffected.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9037263&dopt=Abstract
Anticancer Res. 1997 Jan-Feb;17(1A):381-5.
Antimutagenicity of phenothiazine-metal co-ordination complexes in chemically induced mutagenesis.
Tanaka M, Molnar J, Kidd S.
Faculty of Medicine, Institute of Microbiology, Albert Szent-Gyorgyi Medical University, Szeged, Hungary.
Phenothiazines are heterocyclic organic compounds in which nitrogen and sulfur are incorporated in the tricyclic system, and are known to have antimutagenic activity by shielding DNA-base pairs. Inorganic metals have also been intensively studied for DNA-adduct formation as potential anticancer agents. Phenothiazine, promethazine, promazine and chlorpromazine were complexed either with copper, palladium or gold. The antimutagenicity of twelve phenothiazine-metal complexes, four phenothiazines and three inorganic metals was examined on Salmonella typhimurium TA98 strain treated with a strain-specific, direct-acting mutagen, 4-nitro-o-phenylene-diamine, and the ligand-DNA interaction was analyzed by ultraviolet (UV) spectrophotometry. Phenothiazine-metal co-ordination complexes generally increased their antimutagenic activity, compared to their parent compounds, and the enhanced antimutagenicity was attributed to their interaction with DNA as evidenced by the UV spectra.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=9066681&dopt=Abstract
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