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Sonika Batra, Ravi Bhushan
Bupropion, a tricyclic aminoketone, is used primarily in the treatment of depression, the management of patients with bipolar and schizo-affective disorder, and the treatment of Parkinson's disease. Bupropion is marketed as a racemate, but the racemic mixture is known to have several disadvantages while the two isomers of bupropion and its metabolite differ significantly in their pharmacological activities. Therefore, the stereoselective determination of the drug enantiomers in pharamaceutical dosages, plasma or urine is of potential clinical and analytical importance...
May 2016: Biomedical Chromatography: BMC
Takeshi Yamashita, Takeshi Saitoh, Masaru Matsushita
BACKGROUND: In Japan, intravenous digoxin was previously recommended as a standard drug for acute control of the heart rate in atrial fibrillation (AF)/atrial flutter (AFL) patients with chronic heart failure (CHF). Treatment alternatives for such cases were limited and new drugs for this purpose are needed. In November 2013, landiolol hydrochloride (Onoact(®) 50 for Injection, Ono Pharamaceutical, Osaka, Japan) was approved with the indication for "tachyarrhythmia (AF/AFL) in patients with cardiac dysfunction...
July 2015: Journal of Cardiology
Atanu Modak, Uttam Dutta, Rajesh Kancherla, Soham Maity, Mohitosh Bhadra, Shaikh M Mobin, Debabrata Maiti
An intramolecular dehydrogenative (sp(3))C-O bond formation in salicylamides can be initiated by an active Cu/O2 species to generate pharamaceutically relevant dihydro-oxazinones. Experimental findings suggest that stereoelectronic parameters in both coupling partners are controlling factors for site selectivity in bond formation. Mechanistic investigations including isotope labeling, kinetic studies helped to propose a catalytic cycle. The method provides a convenient synthesis of an investigational new medicine CX-614, which has potential in finding treatment for Parkinson's and Alzheimer's diseases...
May 16, 2014: Organic Letters
Vishakha Grover, Ranjan Malhotra, Anoop Kapoor, Jasvinder Singh, Sonia Sachdeva
Periodontal diseases are comprised of a group of inflammatory conditions that result in the destruction of the supporting structures of the dentition. Emphasis has traditionally been placed on the deleterious actions of lipid mediators, such as prostanoids and leukotrienes, in propagating the inflammatory response and enhancing tissue destruction. Recently, the emerging understanding of the molecular basis of inflammation has elucidated that return of tissue homeostasis, triggered as part of a normal inflammatory response i...
February 2013: Infectious Disorders Drug Targets
Jeffrey William Prescott
The importance of medical imaging for clinical decision making has been steadily increasing over the last four decades. Recently, there has also been an emphasis on medical imaging for preclinical decision making, i.e., for use in pharamaceutical and medical device development. There is also a drive towards quantification of imaging findings by using quantitative imaging biomarkers, which can improve sensitivity, specificity, accuracy and reproducibility of imaged characteristics used for diagnostic and therapeutic decisions...
February 2013: Journal of Digital Imaging: the Official Journal of the Society for Computer Applications in Radiology
Tsuyoshi Inoue, Hiroaki Adachi, Satoshi Murakami, Kazufumi Takano, Hiroyoshi Matsumura, Yusuke Mori, Yoshifumi Fukunishi, Haruki Nakamura, Takayoshi Kinoshita, Isao Nakanishi, Yasushi Okuno, Satoshi Minakata, Shinji Shimojo, Tsuneaki Sakata
We have recently established a Pharamaceutical Innovation Value Chain in collaboration with the SOSHO project ( and BioGrid Project ( to accelerate new drug development. The SOSHO project provides novel crystallization technology with laser-irradiation and stirring growth methods, and the BioGrid Project is developing the software necessary for the in silico screening of promising drugs and the simulation of biological responses to proteins. In this paper, we report the recent research work on the crystallization of membrane proteins and the development of a method for in silico drug discovery...
April 2008: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
G Hopfgartner, C Husser, M Zell
Off-line solid phase extraction with C18 disk plates and turbulent flow chromatography were evaluated versus on-line solid phase extraction using column-switching HPLC as sample preparation techniques for high-throughput analysis of pharmaceutical compounds and their metabolites by LC-MS/MS. Turbulent flow chromatography was found to be very straightforward in its applicaton, but the LOQs were more than fivefold higher compared with off-line or other on-line solid phase extraction methods. Solid phase extraction (SPE) on disk was found to be fast and sufficient efficient to minimize matrix effects and therefore an apprach to provide sensitive and reliable LC-MS/MS methods...
February 2002: Therapeutic Drug Monitoring
M B Cohen, L Spolter, C C Chang, D Behrendt, J Cook, N S Macdonald
Methods using 5 and 6 enzymes were devised to synthesize L-[11C]glutamic acid (GA), labeled on the carboxyl group of either the alpha-(AGA) or gamma-(GGA) carbon atom. The distribution of the 11C-labeled AGA or GGA in rabbits was compared with that of L-[13N]glutamic acid. The results show that AGA was rapidly decarboxylated with loss of the 11C-label, and that GGA was also decarboxylated, but to a lesser degree. Thus, the radiolabel distribution may not reflect the distribution of the original compound. The results also demonstrate that positron labeled pharamaceuticals may be rapidly synthesized via complex enzymatic pathways...
August 1982: International Journal of Applied Radiation and Isotopes
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