Anthramycin: A broad-spectrum spectrum antineoplastic antibiotic isolated from Streptomyces refuineus var. thermotolerans. It has low toxicity, some activity against Trichomonas and Endamoeba, and inhibits RNA and DNA synthesis. It binds irreversibly to DNA.BenzodiazepinonesPatents as Topic: Exclusive legal rights or privileges applied to inventions, plants, etc.Case-Control Studies: Studies which start with the identification of persons with a disease of interest and a control (comparison, referent) group without the disease. The relationship of an attribute to the disease is examined by comparing diseased and non-diseased persons with regard to the frequency or levels of the attribute in each group.Temperature: The property of objects that determines the direction of heat flow when they are placed in direct thermal contact. The temperature is the energy of microscopic motions (vibrational and translational) of the particles of atoms.Blood Transfusion: The introduction of whole blood or blood component directly into the blood stream. (Dorland, 27th ed)Body Temperature: The measure of the level of heat of a human or animal.Body Temperature Regulation: The processes of heating and cooling that an organism uses to control its temperature.Foramen Ovale, Patent: A condition in which the FORAMEN OVALE in the ATRIAL SEPTUM fails to close shortly after birth. This results in abnormal communications between the two upper chambers of the heart. An isolated patent ovale foramen without other structural heart defects is usually of no hemodynamic significance.Intercalating Agents: Agents that are capable of inserting themselves between the successive bases in DNA, thus kinking, uncoiling or otherwise deforming it and therefore preventing its proper functioning. They are used in the study of DNA.Vibration: A continuing periodic change in displacement with respect to a fixed reference. (McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)DNA: A deoxyribonucleotide polymer that is the primary genetic material of all cells. Eukaryotic and prokaryotic organisms normally contain DNA in a double-stranded state, yet several important biological processes transiently involve single-stranded regions. DNA, which consists of a polysugar-phosphate backbone possessing projections of purines (adenine and guanine) and pyrimidines (thymine and cytosine), forms a double helix that is held together by hydrogen bonds between these purines and pyrimidines (adenine to thymine and guanine to cytosine).Peritoneal Lavage: Washing out of the peritoneal cavity. The procedure is a diagnostic as well as a therapeutic technique following abdominal trauma or inflammation.Bisbenzimidazole: A benzimidazole antifilarial agent; it is fluorescent when it binds to certain nucleotides in DNA, thus providing a tool for the study of DNA replication; it also interferes with mitosis.Diagnostic and Statistical Manual of Mental Disorders: Categorical classification of MENTAL DISORDERS based on criteria sets with defining features. It is produced by the American Psychiatric Association. (DSM-IV, page xxii)X-Ray Diffraction: The scattering of x-rays by matter, especially crystals, with accompanying variation in intensity due to interference effects. Analysis of the crystal structure of materials is performed by passing x-rays through them and registering the diffraction image of the rays (CRYSTALLOGRAPHY, X-RAY). (From McGraw-Hill Dictionary of Scientific and Technical Terms, 4th ed)Nuclear Reprogramming: The process that reverts CELL NUCLEI of fully differentiated somatic cells to a pluripotent or totipotent state. This process can be achieved to a certain extent by NUCLEAR TRANSFER TECHNIQUES, such as fusing somatic cell nuclei with enucleated pluripotent embryonic stem cells or enucleated totipotent oocytes. GENE EXPRESSION PROFILING of the fused hybrid cells is used to determine the degree of reprogramming. Dramatic results of nuclear reprogramming include the generation of cloned mammals, such as Dolly the sheep in 1997.Epigenesis, Genetic: A genetic process by which the adult organism is realized via mechanisms that lead to the restriction in the possible fates of cells, eventually leading to their differentiated state. Mechanisms involved cause heritable changes to cells without changes to DNA sequence such as DNA METHYLATION; HISTONE modification; DNA REPLICATION TIMING; NUCLEOSOME positioning; and heterochromatization which result in selective gene expression or repression.Inventions: A novel composition, device, or process, independently conceived de novo or derived from a pre-existing model.Lower Gastrointestinal Tract: The segment of GASTROINTESTINAL TRACT that includes the small intestine below the DUODENUM, and the LARGE INTESTINE.Phenotype: The outward appearance of the individual. It is the product of interactions between genes, and between the GENOTYPE and the environment.Fibrocystic Breast Disease: A common and benign breast disease characterized by varying degree of fibrocystic changes in the breast tissue. There are three major patterns of morphological changes, including FIBROSIS, formation of CYSTS, and proliferation of glandular tissue (adenosis). The fibrocystic breast has a dense irregular, lumpy, bumpy consistency.Equipment Design: Methods of creating machines and devices.Magnetite Nanoparticles: Synthesized magnetic particles under 100 nanometers possessing many biomedical applications including DRUG DELIVERY SYSTEMS and CONTRAST AGENTS. The particles are usually coated with a variety of polymeric compounds.Nanoparticles: Nanometer-sized particles that are nanoscale in three dimensions. They include nanocrystaline materials; NANOCAPSULES; METAL NANOPARTICLES; DENDRIMERS, and QUANTUM DOTS. The uses of nanoparticles include DRUG DELIVERY SYSTEMS and cancer targeting and imaging.Magnetic Resonance Spectroscopy: Spectroscopic method of measuring the magnetic moment of elementary particles such as atomic nuclei, protons or electrons. It is employed in clinical applications such as NMR Tomography (MAGNETIC RESONANCE IMAGING).Magnetics: The study of MAGNETIC PHENOMENA.Sensitivity and Specificity: Binary classification measures to assess test results. Sensitivity or recall rate is the proportion of true positives. Specificity is the probability of correctly determining the absence of a condition. (From Last, Dictionary of Epidemiology, 2d ed)Sphingosine: An amino alcohol with a long unsaturated hydrocarbon chain. Sphingosine and its derivative sphinganine are the major bases of the sphingolipids in mammals. (Dorland, 28th ed)Phosphotransferases (Alcohol Group Acceptor): A group of enzymes that transfers a phosphate group onto an alcohol group acceptor. EC 2.7.1.Lysophospholipids: Derivatives of PHOSPHATIDIC ACIDS that lack one of its fatty acyl chains due to its hydrolytic removal.Receptors, Lysosphingolipid: A subfamily of lysophospholipid receptors with specificity for LYSOSPHINGOLIPIDS such as sphingosine-1-phosphate and sphingosine phosphorylcholine.Propylene Glycols: Derivatives of propylene glycol (1,2-propanediol). They are used as humectants and solvents in pharmaceutical preparations.Curriculum: A course of study offered by an educational institution.Fullerenes: A polyhedral CARBON structure composed of around 60-80 carbon atoms in pentagon and hexagon configuration. They are named after Buckminster Fuller because of structural resemblance to geodesic domes. Fullerenes can be made in high temperature such as arc discharge in an inert atmosphere.Nuclear Magnetic Resonance, Biomolecular: NMR spectroscopy on small- to medium-size biological macromolecules. This is often used for structural investigation of proteins and nucleic acids, and often involves more than one isotope.Lewis Acids: Any chemical species which accepts an electron-pair from a LEWIS BASE in a chemical bonding reaction.Isomerism: The phenomenon whereby certain chemical compounds have structures that are different although the compounds possess the same elemental composition. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 5th ed)Nanostructures: Materials which have structured components with at least one dimension in the range of 1 to 100 nanometers. These include NANOCOMPOSITES; NANOPARTICLES; NANOTUBES; and NANOWIRES.Carbon: A nonmetallic element with atomic symbol C, atomic number 6, and atomic weight [12.0096; 12.0116]. It may occur as several different allotropes including DIAMOND; CHARCOAL; and GRAPHITE; and as SOOT from incompletely burned fuel.Pharmacology, Clinical: The branch of pharmacology that deals directly with the effectiveness and safety of drugs in humans.Personnel Staffing and Scheduling Information Systems: Computer-based systems for use in personnel management in a facility, e.g., distribution of caregivers with relation to patient needs.National Cancer Institute (U.S.): Component of the NATIONAL INSTITUTES OF HEALTH. Through basic and clinical biomedical research and training, it conducts and supports research with the objective of cancer prevention, early stage identification and elimination. This Institute was established in 1937.BostonEducation, Graduate: Studies beyond the bachelor's degree at an institution having graduate programs for the purpose of preparing for entrance into a specific field, and obtaining a higher degree.Physics: The study of those aspects of energy and matter in terms of elementary principles and laws. (From McGraw-Hill Dictionary of Scientific and Technical Terms, 6th ed)Laboratories: Facilities equipped to carry out investigative procedures.Widowhood: The state of having lost a marital partner by death.IrelandAortic Aneurysm, Thoracic: An abnormal balloon- or sac-like dilatation in the wall of the THORACIC AORTA. This proximal descending portion of aorta gives rise to the visceral and the parietal branches above the aortic hiatus at the diaphragm.Northern IrelandCoroners and Medical Examiners: Physicians appointed to investigate all cases of sudden or violent death.Awards and PrizesAbortion, Legal: Termination of pregnancy under conditions allowed under local laws. (POPLINE Thesaurus, 1991)

Characterization of a duocarmycin-DNA adduct-recognizing protein in cancer cells. (1/25)

Duocarmycins have been reported to derive their potent antitumor activity through a sequence-selective minor groove alkylation of N3 adenine in double-stranded DNA. We have used gel mobility shift assays to detect proteins that bind to DNA treated in vitro with duocarmycin SA and identified a protein, named duocarmycin-DNA adduct recognizing protein (DARP), which binds with increased affinity to duocarmycin-damaged DNA. Examination with partially purified DARP revealed that the protein recognized not only the DNA adduct of structurally related drug, CC-1065, but unexpectedly, the protein also recognized the DNA adduct of another chemotype of minor groove binder, anthramycin. These results demonstrate that DARP recognizes the structural alteration of DNA induced by these potent DNA-alkylating drugs, suggesting the possibility that the protein might modulate the antitumor activity of these drugs.  (+info)

A comparison of the rates of reaction and function of UVRB in UVRABC- and UVRAB-mediated anthramycin-N2-guanine-DNA repair. (2/25)

The repair of anthramycin-DNA adducts by the UVR proteins in Escherichia coli follows two pathways: the adducts may be incised by the combined actions of UVRA, UVRB, and UVRC, or alternatively, the anthramycin may be removed by UVRA and UVRB in the absence of UVRC and with no DNA strand incision. To assess the competition between these two competing pathways, the rate of UVRABC-mediated excision repair of anthramycin-N2-guanine DNA adducts and the rate of UVRAB-mediated removal of the adduct were measured with single end-labeled DNAs under identical reaction conditions. UVR protein concentrations of 15 nM UVRA, 100 nM UVRB, and 10 nM UVRC protein were chosen to mimic in vivo concentrations. With these UVR protein concentrations and anthramycin-DNA concentrations of 1-2 nM the incision reaction and the release reactions are described by first-order kinetics. The rate of the UVRABC reaction, measured as the increase in incised fragments, was six to seven times faster than the rate of the UVRAB reaction, measured as the decrease in incised fragments. The UVRABC incision rate on anthramycin-modified linear DNA was four to five times the incision rate measured on the same DNA irradiated with ultraviolet light. We also investigated the role of the ATPase function of UVRB in UVRAB-mediated anthramycin removal. We found that a UVRB analogue with alanine at arginine 51, which retains near wild type ATPase activity, supported removal of anthramycin in the presence of UVRA, whereas a UVRB analogue with alanine at lysine 45, which abolishes the ATPase activity, did not. UVRB*, a specific proteolytic cleavage product of UVRB which retains the ATPase activity, did support removal of anthramycin in the presence of UVRA.  (+info)

Lesion selectivity in blockage of lambda exonuclease by DNA damage. (3/25)

Various kinds of DNA damage block the 3' to 5' exonuclease action of both E. coli exonuclease III and T4 DNA polymerase. This study shows that a variety of DNA damage likewise inhibits DNA digestion by lambda exonuclease, a 5' to 3' exonuclease. The processive degradation of DNA by the enzyme is blocked if the substrate DNA is treated with ultraviolet irradiation, anthramycin, distamycin, or benzo[a]-pyrene diol epoxide. Furthermore, as with the 3' to 5' exonucleases, the enzyme stops at discrete sites which are different for different DNA damaging agents. On the other hand, digestion of treated DNA by lambda exonuclease is only transiently inhibited at guanine residues alkylated with the acridine mustard ICR-170. The enzyme does not bypass benzo[a]-pyrene diol epoxide or anthramycin lesions even after extensive incubation. While both benzo[a]-pyrene diol epoxide and ICR-170 alkylate the guanine N-7 position, only benzo[a]-pyrene diol epoxide also reacts with the guanine N-2 position in the minor groove of DNA. Anthramycin and distamycin bind exclusively to sites in the minor groove of DNA. Thus lambda exonuclease may be particularly sensitive to obstructions in the minor groove of DNA; alternatively, the enzyme may be blocked by some local helix distortion caused by these adducts, but not by alkylation at guanine N-7 sites.  (+info)

DNA binding properties of a new class of linked anthramycin analogs. (4/25)

We have investigated the DNA binding properties of the anthramycin analogues 4, 5, and 6 using fluorescence spectroscopy. A considerable fluorescence enhancement occurs when pyrrolo [1,4] benzodiazepines (P[1,4]Bs) are covalently attached to duplex DNA, which was used to show that neither the presence of RNA, single-stranded DNA, or protein had any effect on the degree of fluorescence enhancement resulting from the incubation of 5 and 6 with DNA. The enhancement was found to be dependent on the presence of the imine functionality in each of the compounds. A wavelength of 320 nm was used to excite the chromophore and its emission wavelength maximum was 420 nm. Additionally, we have discovered that the P[1,4]B ring system exhibits exceptionally favorable fluorescence polarization anisotropy (FPA) decay characteristics. For these more detailed fluorescence measurements, we used the structurally simpler analogue 4,. The time resolved maximum FPA for 4 in glycerol at 25 degrees C is 0.28. This result indicates that the P[1,4]B family of antibiotics could serve as sensitive probes of DNA dynamics in the 0.1 to 35 ns time scale.  (+info)

Benzodiazepine biosynthesis in Streptomyces refuineus. (5/25)

Anthramycin is a benzodiazepine alkaloid with potent antitumor and antibiotic activity produced by the thermophilic actinomycete Streptomyces refuineus sbsp. thermotolerans. In this study, the complete 32.5 kb gene cluster for the biosynthesis of anthramycin was identified by using a genome-scanning approach, and cluster boundaries were estimated via comparative genomics. A lambda-RED-mediated gene-replacement system was developed to provide supporting evidence for critical biosynthetic genes and to validate the boundaries of the proposed anthramycin gene cluster. Sequence analysis reveals that the 25 open reading frame anthramycin cluster contains genes consistent with the biosynthesis of the two halves of anthramycin: 4 methyl-3-hydroxyanthranilic acid and a "dehydroproline acrylamide" moiety. These nonproteinogenic amino acid precursors are condensed by a two-module nonribosomal peptide synthetase (NRPS) terminated by a reductase domain, consistent with the final hemiaminal oxidation state of anthramycin.  (+info)

Dissociation of minor groove binders from DNA: insights from metadynamics simulations. (6/25)

 (+info)

Adenylation enzyme characterization using gamma -(18)O(4)-ATP pyrophosphate exchange. (7/25)

 (+info)

Biosynthesis, synthesis, and biological activities of pyrrolobenzodiazepines. (8/25)

 (+info)

0048] Chemotherapeutic agents include, but are not limited to, the following sub-classes of compounds: Antineoplastic agents such as: Acivicin; Aclarubicin; Acodazole Hydrochloride; Acronine; Adozelesin; Adriamycin; Aldesleukin; Altretamine; Ambomycin; Ametantrone Acetate; Aminoglutethimide; Amsacrine; Anastrozole; Anthramycin; Asparaginase; Asperlin; Azacitidine; Azetepa; Azotomycin; Batimastat; Buniodepa; Bicalutamide; Bisantrene Hydrochloride; Bisnafide Dimesylate; Bizelesin; Bleomycin Sulfate; Brequinar Sodium; Bropirimine; Busulfan; Cactinomycin; Calusterone; Caracemide; Carbetimer; Carboplatin; Carmustine; Carubicin Hydrochloride; Carzelesin; Cedefingol; Chlorombucil; Cirolemycin; Cisplatin; Cladribine; Crisnatol Mesylate; Cyclophosphamide; Cytarabine; Dacarbazine; DACA (N-[2-(Dimethyl-amino)ethyl]acridine-4-carboxamide); Dactinomycin; Daunorubicin Hydrochloride; Daunomycin; Decitabine; Dexormaplatin; Dezaguanine; Dezaguanine Ifesylate; Diaziquone; Docetaxel; Doxorubicin; Doxorubicin ...
0363] In certain embodiments, the compounds of the present invention can be formulated in a pharmaceutical dosage form in combination with anticancer agents. Suitable anticancer agents include, but are not limited to, acivicin; aclarubicin; acodazole hydrochloride; acronine; adozelesin; aldesleukin; altretamine; ambomycin; ametantrone acetate; aminoglutethimide; amsacrine; anastrozole; anthramycin; asparaginase; asperlin; azacitidine; azetepa; azotomycin; batimastat; benzodepa; bicalutamide; bisantrene hydrochloride; bisnafide dimesylate; bizelesin; bleomycin sulfate; brequinar sodium; bropirimine; busulfan; cactinomycin; calusterone; caracemide; carbetimer; carboplatin; carmustine; carubicin hydrochloride; carzelesin; cedefingol; chlorambucil; cirolemycin; cisplatin; cladribine; crisnatol mesylate; cyclophosphamide; cytarabine; dacarbazine; dactinomycin; daunorubicin hydrochloride; decitabine; dexormaplatin; dezaguanine; dezaguanine mesylate; diaziquone; docetaxel; doxorubicin; doxorubicin ...
Earlier today, Synaffix, a Netherlands based biotechnology company focusing on the development of industry-leading antibody-drug conjugate technology platforms, confirmed receiving a key patent covering its HydraSpace™ spacer technology. The patent was granted by the United States Patent and Trademark Office (US 9,636,421 B2).. This patent secures the companys end-to-end patent protection of its ADC technology platform. The Synaffix portfolio of patents covering the core areas of the companys ADC technology including GlycoConnect™, HydraSpace™ and metal-free click chemistry.. Synaffix HydraSpace is a compact and highly polar spacer, which is designed to enhance ADC stability (reduced aggregation) and expand the therapeutic index of an ADC, beyond what is achieved by GlycoConnect alone. The spacer was originally designed to enable efficient attachment of the most challenging hydrophobic payloads, such as pyrrolobenzodiazepines (PBDs), to an antibody. Additionally, the branching ...
More than 50 ancient and rare relics were uncovered in a tomb excavation in Guxian County, Anhui province. The 53-tomb complex is believed to have been under construction over many dynastic periods dating back to the Eastern Han Dynasty nearly 2,000 years ago. The tomb complex was discovered accidentally on a construction site. It contains over 50 brick tombs from the Eastern Han, Tang and Song dynasties.. Experts identified the type of people who were buried there.Zhao Lanhui, deputy researcher of the Bengbu Cultural Relics Institute, said, "lying south to north would perhaps be people of four generations. Due to its size, we know the tombs come from the Song Dynasty. Its small with a simple style.. The tombs hold a unique character that were built in an animal shape."Though some tombs have been plundered over the years, precious relics have emerged, such as bronze mirrors, gold and silver garments, along with pottery boxes.Many people buried here were considered common people, until the ...
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The IUPHAR/BPS Guide to Pharmacology. CC-885 ligand page. Quantitative data and detailed annnotation of the targets of licensed and experimental drugs.
L-Tyrosine is a non-essential amino acid that can be synthesized by the body. It can be used to regulate mood and stimulate the nervous system. Its a...
マウス・モノクローナル抗体 ab16794 交差種: Rat,Hu,Mk 適用: IHC-P,IHC-Fr,Flow Cyt,ICC/IF…APC抗体一覧…画像、プロトコール、文献などWeb上の情報が満載のアブカムの Antibody…
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N-Acetyl L-Tyrosine is a cognitive enhancer that has gained notoriety recently as a powerful mind enhancer. N-Acetyl L-Tyrosine is actually an acetylated form of L-Tyrosine...
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A method of forming a CBI CC-1065 analog utilizes NH2 as a starting material, where R3 is H or alkyl and R6 is H, substituted or unsubstituted lower alkyl, cyano, or alkoxy. Intermediates (I) are used and are claimed.
The state government welcomes the process of investigation by the Nigeria Police, which is ongoing, to unravel the mystery behind the allegation and ensure the security of all the citizens of the state.. "However, intelligence report at my disposal indicates plans by some supporters of Senator Dino Melaye to stage a protest at Aiyetoro-Gbedde, in support of the senator on Saturday.. I am equally aware that some hoodlums and thugs are being recruited within and outside the state to join in the protest. "As much as we do not want the rights of the protesters inhibited, the implications of such a protest in the middle of investigations into the senators allegations may be grave, as some hoodlums may hijack the process to foment trouble and disturb public peace".. The security adviser said he was equally not unaware that some anti-Melaye group were also drumming up a counter protest of theirs on same day, stressing that these will likely lead to chaos, He said that he had already briefed the ...
The initial doses of premazepam given to human test subjects demonstrated similar psychological test results to those produced by diazepam. It was also demonstrated that initial dosing with premazepam produces similar sedative effects as compared with diazepam, although psychomotor impairments are greater with premazepam than with diazepam after initial dosing. However, with repeated dosing for more than one day premazepam causes less sedation and less psychomotor impairment than diazepam. Premazepam possesses sedative and anxiolytic properties. Premazepam produces more slow wave and less fast wave EEG changes than diazepam. Tests have shown that 7.5 mg of premazepam is approximately equivalent to 5 mg of diazepam.[2] ...
... is a nootropic drug invented in 2009 by a team working for Hoffmann-La Roche, which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It has good selectivity for the α5 subtype and did not produce convulsant or anxiogenic effects in animal studies, making it a promising potential nootropic.[1][2][3] Ro4938581 and a related derivative basmisanil (RG-1662, RO5186582) have subsequently been investigated for the alleviation of cognitive dysfunction in Down syndrome.[4][5] ...
... (also known as clonitrazolam) is a benzodiazepine that has had very little research done about its effects and metabolism, and has been sold online as a designer drug.[1][2][3][4][5] The synthesis of clonazolam was first reported in 1971 and the drug was described as the most active compound in the series tested.[6][7] Clonazolam is reported to be highly potent, and concerns have been raised that clonazolam and flubromazolam in particular may pose comparatively higher risks than other designer benzodiazepines, due to their ability to produce strong sedation and amnesia at oral doses of as little as 0.5 mg.[8] ...
... was invented by Schlesinger Walter in the U.S. It was marketed as an anti-anxiety agent in 1981. However, Halazepam is not commercially available in the United States because it was withdrawn by its manufacturer for poor sales.[1] ...
Moosmann, Bjoern; Bisel, Philippe; Franz, Florian; Huppertz, Laura M.; Auwärter, Volker (2016). "Characterization and in vitro phase I microsomal metabolism of designer benzodiazepines - an update comprising adinazolam, cloniprazepam, fonazepam, 3-hydroxyphenazepam, metizolam, and nitrazolam". Journal of Mass Spectrometry. 51 (11): 1080-1089. doi:10.1002/jms.3840. ISSN 1096-9888. PMID 27535017 ...
... is a thienobenzodiazepine acting as selective M1 antimuscarinic. It is used in the treatment of peptic ulcers.[1] Telenzepine is atropisomeric, in other words the molecule has a stereogenic C-N-axis. In neutral aqueous solution it displays a half-life for racemization of the order of 1000 years. The enantiomers have been resolved. The activity is related to the (+)-isomer which is about 500-fold more active than the (-)-isomer at muscarinic receptors in the rat cerebral cortex.[2] ...
... , also called misuse or abuse,[1] is the use of benzodiazepines without a prescription, often for recreational purposes, which poses risks of dependence, withdrawal and other long-term effects.[2][3] Benzodiazepines are one of the more common prescription drugs used recreationally. When used recreationally benzodiazepines are usually administered orally but sometimes they are taken intranasally or intravenously. Recreational use produces effects similar to alcohol intoxication.[3][4] In tests in pentobarbital trained rhesus monkeys benzodiazepines produced effects similar to barbiturates.[5] In a 1991 study, triazolam had the highest self-administration rate in cocaine trained baboons, among the five benzodiazepines examined: alprazolam, bromazepam, chlordiazepoxide, lorazepam, triazolam.[6] A 1985 study found that triazolam and temazepam maintained higher rates of self-injection than a variety of other benzodiazepines.[7] A 1991 study indicated that diazepam, in ...
... is also an intermediate in the synthesis of oxazepam; it is also used in one of the syntheses of medazepam. It can be considered directly analogous/synonoymous with the synthesis of chlordiazepoxide, with the exception that instead of methylamine, hydroxide ion is the choice of base; here acid is not used for the cyclodehydration step though. ...
... [1] (marketed under the brand name Talis) is a drug which is a benzodiazepine derivative.[2][3] It is a relatively selective anxiolytic with less sedative or muscle relaxant properties than other benzodiazepines such as diazepam or bromazepam.[4] It has an active metabolite N-desmethylmetaclazepam, which is the main metabolite of metaclazepam.[5] There is no significant difference in metabolism between younger and older individuals.[6] Metaclazepam is slightly more effective as an anxiolytic than bromazepam,[7] or diazepam,[8] with a 15 mg dose of metaclazepam equivalent to 4 mg of bromazepam.[9] Metaclazepam can interact with alcohol producing additive sedative-hypnotic effects.[6][10] Fatigue is a common side effect from metaclazepam at high doses.[11] Small amounts of metaclazepam as well as its metabolites enter into human breast milk.[12] ...
van Gerven JM, Roncari G, Schoemaker RC, Massarella J, Keesmaat P, Kooyman H, Heizmann P, Zell M, Cohen AF, Dingemanse J. Integrated pharmacokinetics and pharmacodynamics of Ro 48-8684, a new benzodiazepine, in comparison with midazolam during first administration to healthy male subjects. British Journal of Clinical Pharmacology. 1997 Nov;44(5):487-93. .mw-parser-output cite.citation{font-style:inherit}.mw-parser-output .citation q{quotes:"\"""\"""'""'"}.mw-parser-output .citation .cs1-lock-free a{background:url("//upload.wikimedia.org/wikipedia/commons/thumb/6/65/Lock-green.svg/9px-Lock-green.svg.png")no-repeat;background-position:right .1em center}.mw-parser-output .citation .cs1-lock-limited a,.mw-parser-output .citation .cs1-lock-registration a{background:url("//upload.wikimedia.org/wikipedia/commons/thumb/d/d6/Lock-gray-alt-2.svg/9px-Lock-gray-alt-2.svg.png")no-repeat;background-position:right .1em center}.mw-parser-output .citation .cs1-lock-subscription ...
... [1] is a drug which is a benzodiazepine derivative. It has sedative and anxiolytic effects similar to those produced by other benzodiazepine derivatives, but is mainly notable for its strong muscle relaxant properties.[2] Fletazepam is most closely related to other N-trifluoroethyl substituted benzodiazepines such as halazepam and quazepam.[3] ...
They belong to the pyrrolo(1,4)benzodiazepine, or anthramycin, group which includes other antibiotics such as anthramycin, ... "DNA binding properties of a new class of linked anthramycin analogs" (PDF). Nucleic Acids Res. 19: 899-903. doi:10.1093/nar/ ... "DNA binding properties of a new class of linked anthramycin analogs" (PDF). Nucleic Acids Res. 19: 899-903. doi:10.1093/nar/ ... "DNA binding properties of a new class of linked anthramycin analogs" (PDF). Nucleic Acids Res. 19: 899-903. doi:10.1093/nar/ ...
... anthramycin MeSH D03.438.079.080.070.110 --- bromazepam MeSH D03.438.079.080.070.150 --- clonazepam MeSH D03.438.079.080. ...
The cholesterol lowering agent lovastatin Discodermolide Aflatoxin Usnic acid Anthracimycin Anthramycin Esterase Nonribosomal ...
This derivative can be formed by recrystallization of anthramycin from hot methanol. The chemical structure of anthramycin was ... Anthramycin is an active anti-tumor agent and antibiotic. It works by inhibiting the synthesis of RNA and DNA of carcinoma ... Use of anthramycin has been largely limited due to a cardiotoxicity so high that it limits dosing. Acute tissue necrosis has ... It is a competitive inhibitor of cell-free RNA and DNA synthesis, and blocks the action of DNase I. Anthramycin-methyl-ether ( ...
This derivative can be formed by recrystallization of anthramycin from hot methanol. The chemical structure of anthramycin was ... Anthramycin is an active anti-tumor agent and antibiotic. It works by inhibiting the synthesis of RNA and DNA of carcinoma ... Use of anthramycin has been largely limited due to a cardiotoxicity so high that it limits dosing. Acute tissue necrosis has ... It is a competitive inhibitor of cell-free RNA and DNA synthesis, and blocks the action of DNase I. Anthramycin-methyl-ether ( ...
The initial doses of premazepam given to human test subjects demonstrated similar psychological test results to those produced by diazepam. It was also demonstrated that initial dosing with premazepam produces similar sedative effects as compared with diazepam, although psychomotor impairments are greater with premazepam than with diazepam after initial dosing. However, with repeated dosing for more than one day premazepam causes less sedation and less psychomotor impairment than diazepam. Premazepam possesses sedative and anxiolytic properties. Premazepam produces more slow wave and less fast wave EEG changes than diazepam. Tests have shown that 7.5 mg of premazepam is approximately equivalent to 5 mg of diazepam.[2] ...
Ro4938581 is a nootropic drug invented in 2009 by a team working for Hoffmann-La Roche, which acts as a subtype-selective inverse agonist at the α5 subtype of the benzodiazepine binding site on the GABAA receptor. It has good selectivity for the α5 subtype and did not produce convulsant or anxiogenic effects in animal studies, making it a promising potential nootropic.[1][2][3] Ro4938581 and a related derivative basmisanil (RG-1662, RO5186582) have subsequently been investigated for the alleviation of cognitive dysfunction in Down syndrome.[4][5] ...
Methods and compositions are described for treating contaminants in material intended for in vivo use, and in particular blood and blood products for human use. Contaminants in blood cell preparations are inactivated prior to long term storage and transfusion. Inactivation is accomplished using a device having a unique temperature control design.
Anthramycin and Tomaymycin.. 4.3. Ecteinascidins.. 4.4. Mitomycins.. 4.5. Intercalating Alkylators.. 5. Strand-Breaking Drugs. ...
... anthramycin; asparaginase; asperlin; azacitidine; azetepa; azotomycin; batimastat; benzodepa; bicalutamide; bisantrene ...
... anthramycin; asparaginase; asperlin; azacitidine; azetepa; azotomycin; batimastat; benzodepa; bicalutamide; bisantrene ...
Halazepam was invented by Schlesinger Walter in the U.S. It was marketed as an anti-anxiety agent in 1981. However, Halazepam is not commercially available in the United States because it was withdrawn by its manufacturer for poor sales.[1] ...
Devazepide[1] (L-364,718, MK-329) is benzodiazepine drug, but with quite different actions from most benzodiazepines, lacking affinity for GABAA receptors and instead acting as an CCKA receptor antagonist.[2] It increases appetite and accelerates gastric emptying,[3][4] and has been suggested as a potential treatment for a variety of gastrointestinal problems including dyspepsia, gastroparesis and gastric reflux.[5] It is also widely used in scientific research into the CCKA receptor.[6][7] ...
C-C bond cleavage in biosynthesis of 4-alkyl-L-proline precursors of lincomycin and anthramycin cannot precede C-methylation * ... Reply to C-C bond cleavage in biosynthesis of 4-alkyl-l-proline precursors of lincomycin and anthramycin cannot precede C- ...
Biosynthetic conversion of tyrosine to the C2- and C3-proline moieties of anthramycin, tomaymycin, and sibiromycin. / Hurley, ... Biosynthetic conversion of tyrosine to the C2- and C3-proline moieties of anthramycin, tomaymycin, and sibiromycin. In: ... Biosynthetic conversion of tyrosine to the C2- and C3-proline moieties of anthramycin, tomaymycin, and sibiromycin. ... Biosynthetic conversion of tyrosine to the C2- and C3-proline moieties of anthramycin, tomaymycin, and sibiromycin, ...
Anthramycin. A broad-spectrum spectrum antineoplastic antibiotic isolated from Streptomyces refuineus var. thermotolerans. It ...
Reassembly of anthramycin biosynthetic gene cluster by using recombinogenic cassettes.. Hu Y, Phelan VV, Farnet CM, Zazopoulos ...
... anthramycin; asparaginase; asperlin; azacitidine; azetepa; azotomycin; batimastat; benzodepa; bicalutamide; bisantrene ...
Anthramycin; Asparaginase; Asperlin; Azacitidine; Azetepa; Azotomycin; Batimastat; Benzodepa; Bicalutamide; Bisantrene ...
aminoglutethimide; aminolevulinic acid; amifostine; amsacrine; anastrozole; anthramycin; aprepitant; arsenic trioxide; ...
... anthramycin; asparaginase; asperlin; azacitidine; azetepa; azotomycin; batimastat; benzodepa; bicalutamide; bisantrene ...
Mutagenic and Recombinogenic Effects of the Antitumor Antibiotic Anthramycin. Mohammed A. Hannan, Laurence H. Hurley and ...
Streptomyces spadicogriseus produces anthramycin but bears no taxonomic relation to the known producer of the antibiotic: S. ... STREPTOMYCES SPADICOGRISEUS, A NEW SPECIES PRODUCING ANTHRAMYCIN. NOBUHIKO KOMATSU, KATSUKO KIMURA, SHIZUKO ABE, YOSHIO ...
Synthetic studies toward the total synthesis of (+)-anthramycin total syntheses of (+)-neothramycins A and B Lin, Shao-Cheng ( ...
Synthetic studies toward the total synthesis of (+)-anthramycin total syntheses of (+)-neothramycins A and B  Lin, Shao-Cheng ...
From anthramycin to pyrrolobenzodiazepine (PBD)-containing antibody-drug conjugates (ADCs). Angew Chem Int Ed Engl 2017;56:462- ...
Lubawy WC, Dallam RA, Hurley LH: Protection against anthramycin-induced toxicity in mice by coenzyme Q10. J Natl Cancer Inst 64 ...
Antibiotics -Actacinomveins - Actinomycin FI, Anthramycin, Azaserine, Bleomvyins,. Cactinomycin, Carubicin, Carzinophilin, ...
They belong to the pyrrolo(1,4)benzodiazepine, or anthramycin, group which includes other antibiotics such as anthramycin, ... "DNA binding properties of a new class of linked anthramycin analogs" (PDF). Nucleic Acids Res. 19: 899-903. doi:10.1093/nar/ ... "DNA binding properties of a new class of linked anthramycin analogs" (PDF). Nucleic Acids Res. 19: 899-903. doi:10.1093/nar/ ... "DNA binding properties of a new class of linked anthramycin analogs" (PDF). Nucleic Acids Res. 19: 899-903. doi:10.1093/nar/ ...
  • Parallel pathways from this central branch point compound lead by well-known biochemical transformations to the C 2 - and C 3 -proline units of anthramycin, tomaymycin, and sibiromycin. (elsevier.com)
  • The chemical structure of anthramycin was first elucidated by Leimgruber using nuclear magnetic resonance and ultraviolet spectroscopy. (wikipedia.org)
  • What we learn is being applied to the design of minor groove binding antitumor drugs based on netropsin, distamycin, and anthramycin. (ucla.edu)
  • More recently, in 1991, anthramycin derivatives, which are very similar to neothramycin, have been investigated for their ability to link DNA when dimerized. (wikipedia.org)