Benzothiazole derivatives corresponding to the general formula I ##STR1## wherein R.sup.1, R.sup.2, R.sup.3 and R.sup.4 represent, independently of one another, a hydrogen atom, a halogen atom, a linear C.sub.1 -C.sub.3 -alkyl group or a linear C.sub.1 -C.sub.3 -alkoxy group, R.sup.5 represents a hydrogen atom or a linear C.sub.1 -C.sub.3 -alkyl group, R.sup.6 represents a hydrogen atom, and R.sup.7 represents a formyl group, a carbalkoxy group of the formula ##STR2## wherein R.sup.8 denotes a linear or branch chained C.sub.1 -C.sub.4 -alkyl group, or it represents an acyl group of the formula ##STR3## wherein R.sup.9 denotes a linear C.sub.1 -C.sub.3 -alkyl group, or R.sup.6 and R.sup.7 together represent the group ##STR4## wherein R.sup.10 and R.sup.11 represent, independently of one another, a hydrogen atom or a linear C.sub.1 -C.sub.6 -alkyl group or R.sup.6 and R.sup.7 represent the group ##STR5## wherein R.sup.12 and R.sup
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Benzothiazole are important group of compounds reported to have various biological activities and hence the present study was undertaken in order to s..
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Patients with Parkinson disease are prescribed dopamine agonists such as pramipexole to improve motor symptoms. Several studies have found that patients taking dopaminergic medication develop impulse control disorders. In contrast, other studies suggest that some behaviors become less impulsive with pramipexole. We evaluated the performance of 20 young, healthy participants who received pramipexole (0.5 mg) and 20 participants who received placebo, on the Go/No-Go, the Stop Signal Task, and the Balloon Analogue Risk Task. We found that the pramipexole group had more timed out Go trials on the Go/No-Go task than the placebo group, suggesting reduced motor impulsivity. There were no differences between the two groups performance on the other impulsivity tasks. This pattern of results is in line with the theory that impulsivity consists of a motor and a cognitive aspect, and that pramipexole might decrease motor, but not cognitive impulsivity.
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Saccharin belongs to a class of cyclic sulfonamides and this is used as an artificial sweetener for a longtime. The benzothiazole and quinazoline derivatives form an important classes of fused heterocyclic compounds with a wide range of biological activities such as antimicrobial (Schwartz et al., 1992), anticancer (Wolfe et al., 1990), antiinflammatory (Tereshima et al., 1995). As a part of our studies in this area, the molecular and crystal structures of the title compound have been determined and the results are presented here.. The title compound comprises a benzothiazole ring fused with quinazoline ring. X-ray analysis confirms the molecular structure and atom connectivity as illustrated in Fig. 1. The benzothiazole ring system is essentially planar with a maximum deviation of -0.0127 (16)Å for the C7 atom. The quinazoline ring system is also essentially planar with the maximum deviation of -0.1588 (15)Å for the N1 atom. The dihedral angle between the benzothiazole and quinazoline ring ...
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2-[(5-Methylpyridin-2-yl)-piperazin-1-ylmethyl]-1,3-benzothiazole | C18H20N4S | CID 3580097 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
FAAH inhibitor 1 (Benzothiazole analog 3) is a potent fatty acid amide hydrolase (FAAH) inhibitor with an IC50 of 18±8 nM. - Mechanism of Action & Protocol.
A series of new benzothiazole derivatives containing dimethylpyrazole were synthesized and evaluated for their anticonvulsant activity, neurotoxicity and cytotoxicity by using the maximal electroshock (MES), rotarod neurotoxicity (TOX) and MTT colorimetric assay. Among the compounds studied, four compounds (6a, 6b, 6g and 6m) showed better anticonvulsant than the others at 300 mg/kg and they also showed anticonvulsant activity at the dose of 100 mg/kg. All the synthetic compounds showed lower neurotoxicity and little cytotoxicity, so that the compounds, which with better activities, also had higher protective index. In particular, the compound 6g, 2-(3,5-dimethyl-1H-pyrazol-1-yl)-6-((2-fluorobenzyl)oxy)benzo[d]thiazole showed better activity with an ED50 value of 160.4 mg/kg and higher protective index (PI) values of 2.74 in the MES test than the standard drugs sodium valproate, which used as positive controls in this study. After that the compound 6g demonstrated antagonistic activity against seizures
3-Ethyl-2-[[3-[3-[3-[(3-ethyl-1,3-benzothiazol-2-ylidene)methyl]-5,5-dimethylcyclohex-2-en-1-ylidene]prop-1-enyl]-5,5-dimethylcyclohex-2-en-1-ylidene]methyl]-1,3-benzothiazol-3-ium iodide/ACM15979198 can be provided in Alfa Chemistry. We are dedicated to provide our customers the best products and services.
This pathway was started by Janice Frias, University of Minnesota, BioC/MicE 5309, and completed by Carla Essenberg and Jiun-guo Yu, University of Minnesota. 2-Mercaptobenzothiazole (MBT) is used primarily as a vulcanization accelerator in the production of rubber, although it is also used to inhibit the corrosion of copper in water and as an ingredient in cutting oils and petroleum products (Whittaker et al., 2004, De Wever et al., 1998). The manufacture of MBT produces wastewaters with high levels of MBT and its derivatives, and these compounds can also be released into water by factories using MBT and by leaching from MBT-containing products, particularly rubber (De Wever et al., 1998). Many other industries also use benzothiazoles, which in some cases degrade to MBT. For example, MBT is a degradation product of a fungicide widely used in the leather and lumber industries, 2-(thiocyanomethylthio)benzothiazole (Reemtsma, Fiehn, Kalnowski, and Jekel (1995) Environ Sci Technol 29:478-485). MBT ...
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NVP-231: A Competitive CerK Inhibitor. We developed a homogeneous CerK assay for high-throughput screening based on a luminescent reaction measuring ATP consumption (Koresawa and Okabe, 2004; Klumpp et al., 2006). After miniaturization of this assay to a 1536-well plate format, we screened over a million compounds for inhibition of CerK. Primary hits active in the micromolar range were confirmed or invalidated by dose-response experiments, which also provided a preliminary ranking. The overlap to hit lists from other kinase inhibitor screens using the same assay principle was very limited, indicating specificity of the hit compounds for CerK. Although the screened libraries contained many typical protein kinase inhibitors, only a few of them inhibited CerK. Further hit validation was conducted using a direct enzymatic assay measuring the incorporation of radioactive phosphate into C1P.. One of the compounds identified as the benzothiazole derivative 1 (or NVP-231) showed an IC50 value of 12 ± 2 ...
TY - JOUR. T1 - Role of pramipexole in the management of Parkinsons disease. AU - Antonini, Angelo. AU - Barone, Paolo. AU - Ceravolo, Roberto. AU - Fabbrini, Giovanni. AU - Tinazzi, Michele. AU - Abbruzzese, Giovanni. PY - 2010. Y1 - 2010. N2 - The non-ergot dopamine agonist pramipexole is currently indicated for the treatment of the signs and symptoms of idiopathic Parkinsons disease and for the treatment of moderate-to-severe primary restless legs syndrome. A new extended-release formulation of pramipexole has now also been launched in Europe and the US to improve ease of use, compliance and provide a more continuous therapeutic effect over 24 hours. Before initiating any treatment, the benefit-risk ratio to the individual patient must be considered. For pramipexole in the treatment of Parkinsons disease, this means taking into account the available evidence regarding its symptomatic efficacy, effect on delaying long-term levodopa-related motor complications, beneficial effect on non-motor ...
2-(1,2-benzothiazol-3-yl)ethyl acetate | C11H11NO2S | CID 590633 - structure, chemical names, physical and chemical properties, classification, patents, literature, biological activities, safety/hazards/toxicity information, supplier lists, and more.
Learn more about 1-4-6-dimethyl-1-3-benzothiazol-2-yl-piperidine-3-carboxylic-acid. We enable science by offering product choice, services, process excellence and our people make it happen.
4AJN: rat LDHA in complex with 2-((4-(2-((3-((2-methyl-1,3-benzothiazol-6- yl)amino)-3-oxo-propyl)carbamoylamino)ethyl)phenyl)methyl) propanedioic acid
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Chau KY, Cooper JM, Schapira AH. Pramipexole reduces phosphorylation of α-synuclein at serine-129. J Mol Neurosci. 2013 Oct;51(2):573-80. PMID: 23681749.. Kitagawa K, Kitamura Y, Miyazaki T, et al. Effects of pramipexole on the duration of immobility during the forced swim test in normal and ACTH-treated rats. Naunyn Schmiedebergs Arch Pharmacol. 2009 Jul;380(1):59-66. PMID: 19274453.. Iravani MM, Sadeghian M, Leung CC, et al. Continuous subcutaneous infusion of pramipexole protects against lipopolysaccharide-induced dopaminergic cell death without affecting the inflammatory response. Exp Neurol. 2008 Aug;212(2):522-31. PMID: 18571649.. Zarate CA Jr, Payne JL, Singh J, et al. Pramipexole for bipolar II depression: a placebo-controlled proof of concept study. Biol Psychiatry. 2004 Jul 1;56(1):54-60. PMID: 15219473.. Ling ZD, Robie HC, Tong CW, et al. Both the antioxidant and D3 agonist actions of pramipexole mediate its neuroprotective actions in mesencephalic cultures. J Pharmacol Exp Ther. ...
Name: 6-Methoxybenzo[d]thiazol-2-amine CA Name: 2-Benzothiazolamine,6-methoxy- Molecular Structure: 6-Methoxybenzo[d]thiazol-2-amine,2-Benzothiazolamine,6-methoxy-,CAS 1747-60-0,180.23,C8H8N2OS 6-Methoxybenzo[d]thiazol-2-amine,2-Benzothiazolamine,6-methoxy-,CAS 1747-60-0,180.23,C8H8N2OS Molecular Formula:C8H8N2OS Molecular Weight: 180.23 CAS Registry Number: 1747-60-0
Background: The cerebrospinal fluid (CSF) amyloid-β (Aβ)1-42, total-tau (T-tau), and phosphorylated-tau (P-tau181P) profile has been established as a valuable biomarker for Alzheimers disease (AD). Objective: The current study aimed to determine CSF biomarker cut-points using positron emission tomography (PET) Aβ imaging screened subjects from the Australian Imaging, Biomarkers and Lifestyle (AIBL) study of aging, as well as correlate CSF analyte cut-points across a range of PET Aβ amyloid ligands. Methods: Aβ pathology was determined by PET imaging, utilizing 11C-Pittsburgh Compound B, 18F-flutemetamol, or 18F-florbetapir, in 157 AIBL participants who also underwent CSF collection. Using an INNOTEST assay, cut-points were established (Aβ1-42 ,544 ng/L, T-tau ,407 ng/L, and P-tau181P ,78 ng/L) employing a rank based method to define a positive CSF in the sub-cohort of amyloid-PET negative healthy participants (n = 97), and compared with the presence of PET demonstrated AD pathology. ...
(8S,9S,13S,14S)-3-hydroxy-13-methyl-2,4-dinitro-7,8,9,11,12,14,15,16-octahydro-6H-cyclopenta[a]phenanthren-17-one Butanedioic acid,(tetrahydro-2-furanyl)- 2-(chloromethylsulfanyl)benzothiazole 1,2-Benzenedicarboxylic acid, mixed esters with isooctanol and neopentyl glycol ethyl (Z)-3-diethoxyphosphoryloxy-3-phenyl-prop-2-enoate 36626-29-6 3-(7-methyl-6-azabicyclo[3.2.1]oct-1-yl)phenol hydrobromide Testosterone 17beta-carboxylic acid 1-Piperazineethanol, 4-(3-(diphenylamino)-1-oxopropyl)-, acetate (ester) 1-[5-fluoro-4-[4-(2-fluoro-5-methyl-4-nitro-phenyl)piperazin-1-yl]-2-methyl-phenyl]ethanone
Abstract: The experimental infrared (IR), nuclear magnetic resonance (NMR), and ultraviolet (UV) spectra, and density functional theory (DFT) calculations of the novel compound N, N-di[3-hydroxy-4-(2-benzothiazole) phenyl]urea (4-DHBTU) are presented. Compared with the UV spectra of the 2-(4-amino-2-hydroxyphenyl) benzothiazole (4-AHBT) monomer, the experimental spectra of 4-DHBTU, a dimer of 4-AHBT, show dualwavelength absorption with significantly enhanced absorption intensity and an obvious red shift of the maximum absorption peak. Analysis of the experimental spectra and the DFT calculations shows that the structures of cis-C11 and trans-C11 are the two most stable conformers, and that the main reason for the different UV spectral properties of the dimer and monomer is the coexistence of cis-C11, trans-C11, cis-C22, and trans-C22 in the 4-DHBTU sample. In addition, the DFT calculations indicate that a hydrogen-bonding interaction between 4-DHBTU and the dimethyl sulfoxide (DMSO) solvent ...
Should a spill occur while you are handling this chemical, FIRST REMOVE ALL SOURCES OF IGNITION, then you should dampen the solid spill material with 60-70% ethanol and transfer the dampened material to a suitable container. Use absorbent paper dampened with 60-70% ethanol to pick up any remaining material. Seal the absorbent paper, and any of your clothes, which may be contaminated, in a vapor-tight plastic bag for eventual disposal. Solvent wash all contaminated surfaces with 60-70% ethanol followed by washing with a soap and water solution. Do not reenter the contaminated area until the Safety Officer (or other responsible person) has verified that the area has been properly cleaned ...
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Pramipexole Dihydrochloride Miraprex Buy Cheap Pramipexole Dihydrochloride, Cheap Pramipexole Dihydrochloride. Pramipexole Dihydrochloride Monohydrate is prescribed to help treat the symptoms of Parkinsons disease. It may also be prescribed to help treat restless legs syndrome.
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Small-conductance (KCa2) and intermediate-conductance (KCa3.1) calcium-activated K+ channels are voltage-independent and share a common calcium/calmodulin-mediated gating mechanism. Existing positive gating modulators like EBIO, NS309, or SKA-31 activate both KCa2 and KCa3.1 channels with similar potency or, as in the case of CyPPA and NS13001, selectively activate KCa2.2 and KCa2.3 channels. We performed a structure-activity relationship (SAR) study with the aim of optimizing the benzothiazole pharmacophore of SKA-31 toward KCa3.1 selectivity. We identified SKA-111 (5-methylnaphtho[1,2-d]thiazol-2-amine), which displays 123-fold selectivity for KCa3.1 (EC50 111 ± 27 nM) over KCa2.3 (EC50 13.7 ± 6.9 μM), and SKA-121 (5-methylnaphtho[2,1-d]oxazol-2-amine), which displays 41-fold selectivity for KCa3.1 (EC50 109 nM ± 14 nM) over KCa2.3 (EC50 4.4 ± 1.6 μM). Both compounds are 200- to 400-fold selective over representative KV (KV1.3, KV2.1, KV3.1, and KV11.1), NaV (NaV1.2, NaV1.4, NaV1.5, and ...
The criteria for diagnosing Alzheimers disease (AD) have recently been revised to include the use of biomarkers for the in vivo presence of β-amyloid, one of the neuropathological hallmarks of AD. Examples of such biomarkers are positron emission tomography (PET) β-amyloid specific ligands, including [18F]flutemetamol. The aim of this thesis was to characterize the binding properties of [18F]flutemetamol from a tracer kinetic perspective as well as by validating binding measures through comparison with tissue pathology assessments. The applicability of previously developed kinetic models of tracer binding for voxel-based analysis was examined and compared to arterial input compartment modelling, the gold standard for PET quantification. Several voxel-based methods were found to exhibit high correlations with compartment modelling, including the semi-quantitative standardized uptake value ratio (SUVR). The kinetic components of [18F]flutemetamol uptake were also investigated without model ...
Patients should be instructed to take pramipexole dihydrochloride tablets only as prescribed. Patients should be alerted to the potential sedating effects associated with pramipexole dihydrochloride tablets, including somnolence and the possibility of falling asleep while engaged in activities of daily living. Since somnolence is a frequent adverse event with potentially serious consequences, patients should neither drive a car nor engage in other potentially dangerous activities until they have gained sufficient experience with pramipexole dihydrochloride tablets to gauge whether or not it affects their mental and/or motor performance adversely. Patients should be advised that if increased somnolence or new episodes of falling asleep during activities of daily living (e.g., watching television, passenger in a car, etc.) are experienced at any time during treatment, they should not drive or participate in potentially dangerous activities until they have contacted their physician. Because of ...
Two novel isosteric conjugates of guanidiniocarbonyl-pyrrole and 6-bromo-TO (thiazole orange) had been ready, differing solely in linker connectivity to cyanine (benzothiazole nitrogen vs. quinoline nitrogen). The quinoline analog was considerably extra vulnerable to aggregation in an aqueous medium, which resulted in induced round dichroism (ICD; λ = 450-550 nm) recognition between A-T(U) and G-C basepair …. Fluorimetric and CD Recognition between Various ds-DNA/RNA Depends on a Cyanine Connectivity in Cyanine-guanidiniocarbonyl-pyrrole Conjugate Read More ». ...
Two novel isosteric conjugates of guanidiniocarbonyl-pyrrole and 6-bromo-TO (thiazole orange) had been ready, differing solely in linker connectivity to cyanine (benzothiazole nitrogen vs. quinoline nitrogen). The quinoline analog was considerably extra vulnerable to aggregation in an aqueous medium, which resulted in induced round dichroism (ICD; λ = 450-550 nm) recognition between A-T(U) and G-C basepair …. Fluorimetric and CD Recognition between Various ds-DNA/RNA Depends on a Cyanine Connectivity in Cyanine-guanidiniocarbonyl-pyrrole Conjugate Read More ». ...
Information on Registered Substances comes from registration dossiers which have been assigned a registration number. The assignment of a registration number does however not guarantee that the information in the dossier is correct or that the dossier is compliant with Regulation (EC) No 1907/2006 (the REACH Regulation). This information has not been reviewed or verified by the Agency or any other authority. The content is subject to change without prior notice ...
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This study was designed to investigate the activity of CGP 20376, a benzothiazole derivative, against Brugia malayi in jirds and to illustrate the utility of parasite antigen detection as a means of monitoring drug efficacy in filariasis. Drug treatment was 100% effective in jirds treated 3 or 24 days after infection. Microfilaria and adult worm counts were reduced (relative to counts in sham-treated control animals) by 96% and 95%, respectively, in animals treated 153 days after infection. Four of 6 animals in this treatment group cleared their microfilaremias and were free of adult worms 5 mo after treatment. Thus, CGP 20376 was effective against all life cycle stages of B. malayi in jirds. Parasite antigen levels in jird sera were consistent with parasitological results in all treatment groups, but antigen clearance was incomplete in some cases after apparently successful treatment of mature and immature infections.
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In attempt to make significant pharmacologically active molecule, we report here the synthesis and in vitro antimicrobial and antitubercular activity of various series of 3-(3-pyridyl)-5-(4-nitrophenyl)-4-(N-substituted-1,3-benzothiazol-2-amino)-4H-1,2,4-triazole. The antimicrobial activity of title compounds were examined against two Gram-positive bacteria (Staphylococcus aureus, Streptococcus pyogenes), two Gram-negative bacteria (Escherichia coli, Pseudomonas aeruginosa), and three fungi (Candida albicans, Aspergillus niger, Aspergillus clavatus) using the broth microdilution method and antitubercular activity H(37)Rv using Lowenstein-Jensen agar method. ...
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Although the gold standard diagnostic tool for cardiac amyloidosis is endomyocardial biopsy (5), investigators have tried to assess this disease noninvasively with various imaging techniques. Although some molecular imaging-based methods have been successful (8,12), most of them have been unsuccessful for demonstrating amyloid deposits in the myocardium (13). The CMR has also been successful in the diagnosis of cardiac amyloidosis (14), but it may not be specific for amyloid deposits (15). Therefore, there is a clinical need to foster imaging-based diagnosis into clinical utility.. 11C-PiB has been used recently for early detection and for follow-up of Alzheimers dementia (16), a disease characterized by accumulation of β-amyloid plaque in the brain parenchyme. It is a radioactive derivative of benzothiazole that binds with conformational dependence to any type of β-amyloid sheet structure (7). Indeed, this has been demonstrated in various mouse models (17) and in human autopsy studies of the ...
2,2-Azino-bis(3-ethylbenzthiazoline-6-sulfonic acid) is a peroxidase substrate suitable for use in ELISA procedures. This substrate produces a soluble end product that is green in color and can be read spectrophotometrically at 405 nm. The reaction may be stopped with 1% sodium dodecyl sulfate (SDS). Recommended for ELISA (microwell) procedures, not recommended for membrane applications ...
Buy Pramipexole For Parkinsons Disease. Pramipexole is a non-ergoline medication belonging to the class of dopamine agonists. It is used for the treatment of Parkinsons disease, and sometimes for Restless Legs Syndrome in its initial stages. In some cases, it can be prescribed for the treatment of cluster headache, and also for counteracting sexual dysfunction problems in patients using SSRI antidepressants. Pramipexole depression medication can also be used for treating clinical depression in certain patients, and also for treating fibromyalgia.. How the drug works. For Parkinsons disease, it restores dopamine balance in your brain, leading to improvement in your movements, and reduction in your unsteadiness, stiffness, shakiness and slowed movements. With the use of this drug, you can receive less number of attacks known as on-off syndrome. During these attacks, you are not able to move your body. For Restless Legs Syndrome, it works by relieving the unpleasant feelings in your legs during ...
CALM-PD study found that Pramipexole can reduce the occurrence of motor complication compared with Levodopa used as initiative treatment, but it still remains debatable that initiation of which medication will be better for those patients with De Novo PD.. PDRP (Parkinsons disease-related spatial covariance pattern) is a biomarker which can represent the network activity of cortico-striato-pallido-thalamocortical pathways and highly reproducible with stable network activity in individual subjects. The study published in J Neuroscience in 2010 showed that the abnormal PDRP antecede the appearance of motor signs by about 2 years, indicating PDRP might be a very promising biomarker for identifying PD at its early stage. Moreover, PDRP is able to represent the progression and severity of PD as well. It was reported that Levodopa can reduce the PD-related network activity, and the degree of network suppression correlates with the clinical improvement. However, there is no study currently showing ...
Tozadenant RO-449351 SYN-115 Molecular Formula C19H26N4O4S Average mass 406.499 Da A2 (3); A2a-(3); RO4494351; RO4494351-000; RO4494351-002; SYN-115 Phase III clinical trials at Biotie Therapies for the treatment of Parkinsons disease as an adjunctive therapy with levodopa 1-Piperidinecarboxamide, 4-hydroxy-N-[4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl]-4-methyl- 4-Hydroxy-N-[4-methoxy-7-(4-morpholinyl)-1,3-benzothiazol-2-yl]-4-methyl-1-piperidinecarboxamide 4-Hydroxy-N-[4-methoxy-7-(4-morpholinyl)-2-benzothiazolyl]-4-methyl-1-piperidinecarboxamide 4-Hydroxy-4-methyl-piperidine-1-carboxylic acid(4-methoxy-7-morpholin-4-yl-benzothiazol-2-yl)-amide CAS 870070-55-6 Originator Roche Developer Acorda Therapeutics Class Amides; Antiparkinsonians; Benzothiazoles; Carboxylic acids; Morpholines; Piperidines; Small molecules Mechanism…
It is inherently undesirable for any chemical component of the rubber to migrate into a foodstuff during processing or storage. Rubber compounds are complex formulations that undergo chemical transformation during vulcanisation.. Rubber components that can potentially migrate include low molecular mass monomers, vulcanising agents, plasticisers, oils and waxes and their breakdown products. For example, polar plasticisers such as di-2-ethylhexyl phthalate are readily soluble in alcohol so plasticised rubbers should not be used in contact with alcoholic beverages.. The compounds 2-mercaptobenzothiazole (MBT) and benzothiazole (BT) may migrate from rubber during the manufacture and storage of food or drink. Research has shown that this might happen. Both MBT and BT migrated from rubber into laboratory solvents.. The main types of rubber components where residues of MBT and BT may be found include natural rubber or nitrile rubber seals and gaskets used in food processing equipment. MBT is formed ...
Stupp, R., Tosoni, A., Bromberg, J. E. C., Hau, Peter, Campone, M., Gijtenbeek, J., Frenay, M., Breimer, L., Wiesinger, H., Allgeier, A., van den Bent, M. J., Bogdahn, Ulrich, van der Graaf, W., Yun, H. J., Gorlia, T., Lacombe, D. and Brandes, A. A. (2011) Sagopilone (ZK-EPO, ZK 219477) for recurrent glioblastoma. A phase II multicenter trial by the European Organisation for Research and Treatment of Cancer (EORTC) Brain Tumor Group. Annals of oncology : official journal of the European Society for Medical Oncology / ESMO 22 (9), pp. 2144-2149 ...
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Purpose Inhibitors from the epidermal development aspect receptor (EGFR) tyrosine kinase possess demonstrated humble anticancer activity in advanced bronchioloalveolar carcinoma (BAC). launching dosage of 400 mg/m2 in week 1. The principal end stage was perseverance of response price. and mutations Pifithrin-alpha had been examined by pyrosequencing. Outcomes Seventy-two sufferers had been enrolled and 68 fulfilled eligibility requirements. Features of sufferers included median age group 71 years; sex 57 females; PS 0 or 1 88 of sufferers; and smoking position 19 never-smokers. Central pathology review verified the Pifithrin-alpha medical diagnosis in 45 of 49 obtainable specimens. Around 50% of sufferers received a lot more than two cycles of therapy (> eight weeks). Epidermis rash was the most frequent toxicity (quality 3 15 The verified response price was 7% and steady disease was seen in 35%. Pifithrin-alpha The median success and progression-free success had been 13 and 3.three months ...
The three organometallic complexes [(Cis-Pt^II (DDH) (2,5- Dihidroxibenzensulfonic)^2, Rh^I (CO)2 Cl(2- Aminobenzothiazole) and Rh^I (CO)2 Cl(5-Cl-2- Methilbenzothiazole)] used in this study had been previously found to have a high in vitro activity against promastigote and amastigote like forms of Leishmania donovani. Here, the cytotoxic effect of these new organometallic complexes on the J-774 macrophages were studied. Only the Rh^I(CO)2 Cl (2-Aminobenzothiazole) complex induced substantial toxicity in the cells.. Also, we assayed the effect of this complex on the parasite s biosynthesis of macromolecules. The Rh^I(CO)2Cl (5-Cl-2- Methylbenzothiazole) complex inhibited DNA, RNA, and protein synthesis. On the other hand, the two other compounds tested did not inhibit the incorporation of radioactive precursors. Finally important ultrastructural alterations in the parasites treated with the two non-cytotoxic complexes were observed ...
A number of compounds of interest as possible purine or pyrimidine antagonists have been assayed for anti-leukemic action against transplanted lymphoid leukemia (Ak 4) in mice.. The pyrimidines studied were uniformly inactive.. Of the 2,6-diaminopurine derivatives assayed, only the parent compound definitely increased survival time. Introduction of a hydroxy, mercapto, or iodo group at the 8-position of 2,6-diaminopurine apparently inactivates this anti-leukemic molecule.. Benzimidazole, 2-chloromethylbenzimidazole, 5-nitrobenzotriazole, indole, benzoxazole, benzothiazole, 2-methyl-4-hydroxyquinazoline, and 2,3,5-triphenyltetrazolium chloride were screened but showed no anti-leukemic activity.. ...
Nawrocki, S. T., K. D. Drake, C. F. Watson, G. D. Foster, and K. J. Maier. (2005). Comparative aquatic toxicity evaluation of 2-(thiocyanomethylthio) benzothiazole (TCMTB) and selected degradation products using Ceriodaphnia dubia. Arch. Environ. Contam. Toxicol. 48: 344-350. Maier, K. J., J. L. Stobbe and K. D. Drake. (2003) Response to Letter to the Editor (re: Stobbe et al., 2003). International Journal of Toxicology 22:475-478. Stobbe, J. L., K. D. Drake, and K. J. Maier. (2003). Comparison of in vivo (Draize method) and in vitro (Corrositex assay) dermal corrosion values for selected industrial chemicals. International Journal of Toxicology 22:99-107. Davis, S. M., K. D. Drake, and K. J. Maier. (2002). Toxicity of boron to the duckweed, Spirodella polyrrhiza. Chemosphere. 48: 615-620. Dethloff, G. M., H. C. Bailey and K. J. Maier. (2001). Effects of dissolved copper on select hematological, biochemical and immunological parameters of wild rainbow trout (Onchrhynchus mykiss). Arch. Environ. ...
In addition to tens of thousands useful reagents such as super dry solvents, coupling reagents, indicators, etc., we also supply specialized items to address research and development needs. For example, we are a long-time provider of amino acids used for stapling peptide chemistry. Such structurally constrained (stapled) peptides are being widely used to study protein-protein interactions which are implicated in diverse biological processes and disease states and, due to the greater peptide stability, bear promising clinical significance. Our fluorescent dye series has been used by leading institutes for biological research. Our list of heterocyclic compounds, such as benzothiazoles, pyridines, purines, pyrimidines, saccharides, etc. is growingly used in chemistry and pharmaceutical research. ...
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Haploinsufficiency of Meis1 is a potential model system for simulating RLS in mice. Here, we show that this Meis1 deficit causes a sex- and context-dependent RLS-related phenotype at middle age, impaired sensorimotor gating ability that was refractory to the D2/3R agonist pramipexole as well as increased social memory. These behavioral abnormalities occurred without differences in thermal sensitivity, plasma iron concentrations or dopaminergic neuron number in the SNpc/VTA. Thus, although Meis1 haploinsufficiency causes the RLS-related phenotype of motor restlessness in mice, the detailed nature of these effects is complex. Furthermore, it is characteristically distinct from other genetic RLS models (e.g. Btbd9 knock-out), highlighting the heterogeneous nature of the effects of these different risk genotypes in this disease.. Motor restlessness in these Meis1-haploinsufficient mice was detected previously in young adult male and female mice (Spieler et al., 2014). RLS is, however, more prevalent ...
The purpose of this study is to examine how non-ergot dopamine receptor agonist (DA) treatment with rotigotine, pramipexole LA or ropinirole CR influences
Description :Overview of ABX Pentra 120 ReticReticulocyte analysis is fully automated, thiazole orange staining, argon-ion laser and fluoro-flow cytometry technology is used, throughput of about 120 samples/hour (Retics or DIFF)FeaturesLiquid valves* ABX have volume accuracy and reliability. The Rotative mixing samples are efficient and smooth. Automatic sample re-run are programmable and selective (hematology factors and smears). DHSS* sequential measurement and focused flow cytometry. Balance Concept - Based on three self-determining channels leukocyte is controlled automatically. Reticulocyte profile: Argon-ion laser, fluorescence, impedance, thiazole orange. Impedance, flow cytometry, cytochemistry and absorbance are the methods of measurement used.
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Learn about Mirapex ER (Pramipexole Dihydrochloride Extended-Release Tablets) may treat, uses, dosage, side effects, drug interactions, warnings, patient labeling, reviews, and related medications.
The object of this study was to compare the relative bioavailability (rate and extent of absorption) of Pramipexole Dihydrochloride Tablets 0.25 mg by Barr Laboratories, Inc. with that of Mirapex® Tablets 0.25 mg distributed by Boehringer Ingelheim Pharmaceuticals, Inc. following a single oral dose in healthy adults under non-fasting conditions ...
Pramipexole (Mirapex) eases the symptoms of Parkinsons disease-a progressive disorder marked by muscle rigidity, weakness, shaking, tremor. Read More!
Pramipexole is used alone or with other medications to treat Parkinsons disease. It can improve your ability to move and can decrease shakiness (trem
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Eyebrows have been raised after Astellas Pharma decided to end its collaboration with Ambit Biosciences Corp to develop the latters acute myeloid leukaemia treatment quizartinib. - News - PharmaTimes
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Herbal medicine is an important part of health care system in most of the countries. Rubus fairholmianus is an unexplored berry in folkloric medicine. In this study, we aimed to understand the importance of R. fairholmianus in pharmaceutical industry for the development of cost-effective cancer therapeutic drugs using in vivo and in vitro analysis. Chemical characterization, antioxidant, antiproliferative and apoptosis inducing properties of R. fairholmianus root methanolic column subfraction (RFM) were investigated. The RFM displayed the presence of alpha-tocopherol, flavonol glycoside and apigenin in the chemical characterization. DPPH (2, 2-diphenyl-1-picrylhydrazyl) and ABTS (2, 2-azinobis-(3-ethylbenzothiazoline-6-sulfonic acid)) radical scavenging assays exhibited an activity of 7.56 g/mL (IC ) and 20514.7 M trolox equivalents/g respectively. The solid and ascites tumors in mice were reduced significantly upon 100 mg/kg RFM treatment by reducing the tumor volume (1.86 cm ), tumor weight ...
Millions of people worldwide living with RLS to benefit as treatment becomes globally available, , , , Ingelheim/Germany, 10 November 2006 - Boehringer Ingelheim announced today that the U.S. Food and Dr...
Introduction of lysine linkage in the conjugate between abasic site-binding ligands and thiazole orange significantly improved the binding affinity for target orphan adenine or uracil nucleobase in DNA/RNA hybrids.
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Detailed dosage guidelines and administration information for Mirapex ER (pramipexole dihydrochloride). Includes dose adjustments, warnings and precautions.
2-((2-Aminophenyl)thio)phenyl)(4-(2-(2-hydroxyethoxy)ethyl)piperazin-1-yl)methanone ;. CAS # 848814-27-7 ;. C21H27N3O3S ;. MW: 401.52 ;. ...