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Seiji Yamasaki, Takuma Fujioka, Katsuhiko Hayashi, Suguru Yamasaki, Mitsuko Hayashi-Nishino, Kunihiko Nishino
A large number of drug efflux transporters have been identified in Salmonella enterica serovar Typhimurium, and increased expression of these transporters confers drug resistance in this organism. Here we compared the respiration activities of the wild-type strain and a mutant with nine deleted transporters by phenotype microarray analysis. The mutant was susceptible to 66 structurally unrelated compounds including many antibiotics, dyes, detergents, antihistamine agents, plant alkaloids, antidepressants, antipsychotic drugs, and antiprotozoal drugs...
May 20, 2016: Journal of Infection and Chemotherapy: Official Journal of the Japan Society of Chemotherapy
Tarek S Belal, Karim M Abdel-Hay, C Randall Clark
A novel simple, direct and selective gas chromatography-mass spectrometry (GC/MS) procedure was developed for the determination of the antihistamine drug dimenhydrinate (DMH) in presence of six of its related substances and potential impurities, namely, diphenylmethane, diphenylmethanol, benzophenone, orphenadrine, caffeine and 8-chlorocaffeine. The method involved resolution of the underivatized compounds using a trifluoropropylmethyl polysiloxane (Rtx-200) capillary column and the mass spectrometric detection was carried out in the electron-impact (EI) mode...
January 2016: Journal of Advanced Research
Ravindra Kumar, Yoichi Hoshimoto, Hayato Yabuki, Masato Ohashi, Sensuke Ogoshi
A highly enantioselective synthesis of 3-aryl-, vinyl-, and alkynyl-2,1-benzoxasiloles (up to 99.9% ee and 99% yield) was achieved via the sequential activation of an aldehyde and a silane by nickel(0). This strategy was applied to a simultaneous generation of carbon- and silicon-stereogenic centers with excellent selectivity (dr = 99:1) via diastereotopic aryl transfer. Initial mechanistic studies revealed the complete switching of an aryl-transfer process from an intermolecular (racemic synthesis in the presence of IPr) to an intramolecular (enantioselective synthesis using chiral NHC, L5) fashion...
September 16, 2015: Journal of the American Chemical Society
Mary Hongying Cheng, Ethan Block, Feizhuo Hu, Murat Can Cobanoglu, Alexander Sorkin, Ivet Bahar
Human dopamine (DA) transporter (hDAT) regulates dopaminergic signaling in the central nervous system by maintaining the synaptic concentration of DA at physiological levels, upon reuptake of DA into presynaptic terminals. DA translocation involves the co-transport of two sodium ions and the channeling of a chloride ion, and it is achieved via alternating access between outward-facing (OF) and inward-facing states of DAT. hDAT is a target for addictive drugs, such as cocaine, amphetamine (AMPH), and therapeutic antidepressants...
2015: Frontiers in Neurology
Yong-Sook Park, Young-Baeg Kim, Jeong-Min Kim
Nefopam, a centrally acting analgesic, has been used to control postoperative pain. Reported adverse effects are anticholinergic, cardiovascular or neuropsychiatric. Neurologic adverse reactions to nefopam are confusion, hallucinations, delirium and convulsions. There are several reports about fatal convulsive seizures, presumably related to nefopam. A 71-year-old man was admitted for surgery for a lumbar spinal stenosis. He was administered intravenous analgesics : ketorolac, tramadol, orphenadrine citrate and nefopam HCl...
November 2014: Journal of Korean Neurosurgical Society
Bassem Sadek, Seyedeh Soha Khanian, Abrar Ashoor, Tatiana Prytkova, Mohammad A Ghattas, Noor Atatreh, Syed M Nurulain, Keun-Hang Susan Yang, Frank Christopher Howarth, Murat Oz
Effects of the histamine H₁ receptor (H1R) antagonists (antihistamines), promethazine (PMZ), orphenadrine (ORP), chlorpheniramine (CLP), pyrilamine (PYR), diphenhydramine (DPH), citerizine (CTZ), and triprolidine (TRP) on the functional properties of the cloned α7 subunit of the human nicotinic acetylcholine receptor expressed in Xenopus oocytes were investigated. Antihistamines inhibited the α7-nicotinic acetylcholine receptor in the order PYR>CLP>TRP>PMZ>ORP≥DPH≥CTZ. Among the antihistamines, PYR showed the highest reversible inhibition of acetylcholine (100 µM)-induced responses with IC₅₀ of 6...
January 5, 2015: European Journal of Pharmacology
Ali M Yehia, Mohamed K Abd El-Rahman
Normalized spectra have a great power in resolving spectral overlap of challenging Orphenadrine (ORP) and Paracetamol (PAR) binary mixture, four smart techniques utilizing the normalized spectra were used in this work, namely, amplitude modulation (AM), simultaneous area ratio subtraction (SARS), simultaneous derivative spectrophotometry (S(1)DD) and ratio H-point standard addition method (RHPSAM). In AM, peak amplitude at 221.6nm of the division spectra was measured for both ORP and PAR determination, while in SARS, concentration of ORP was determined using the area under the curve from 215nm to 222nm of the regenerated ORP zero order absorption spectra, in S(1)DD, concentration of ORP was determined using the peak amplitude at 224nm of the first derivative ratio spectra...
March 5, 2015: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Jessica L Knittel, Shawn P Vorce, Barry Levine, Rhome L Hughes, Thomas Z Bosy
A multidrug fatality involving sumatriptan is reported. Sumatriptan is a tryptamine derivative that acts at 5-HT(1B/1D) receptors and is used for the treatment of migraines. The decedent was a 21-year-old white female found dead in bed by her spouse. No signs of physical trauma were observed and a large number of prescription medications were discovered at the scene. Toxicological analysis of the central blood revealed sumatriptan at a concentration of 1.03 mg/L. Following therapeutic dosing guidelines, sumatriptan concentrations do not exceed 0...
January 2015: Journal of Analytical Toxicology
Yu-Wen Chen, Jann-Inn Tzeng, Yu-Chung Chen, Ching-Hsia Hung, Jhi-Joung Wang
The purpose of this study was to estimate the local anesthetic effect of orphenadrine, an anti-muscarinic agent, in spinal anesthesia and its comparison with the local anesthetic lidocaine. After the rat was injected intrathecally, the spinal block of orphenadrine and lidocaine was constructed in a dosage-dependent fashion. The potency and duration of spinal anesthesia with orphenadrine were compared with that of lidocaine. Our data demonstrated that orphenadrine and lidocaine elicited dose-dependent spinal blockades on the motor function, sensory, and proprioception...
November 5, 2014: European Journal of Pharmacology
Marta Maltese, Giuseppina Martella, Graziella Madeo, Irene Fagiolo, Annalisa Tassone, Giulia Ponterio, Giuseppe Sciamanna, Pierre Burbaud, P Jeffrey Conn, Paola Bonsi, Antonio Pisani
Broad-spectrum muscarinic receptor antagonists have represented the first available treatment for different movement disorders such as dystonia. However, the specificity of these drugs and their mechanism of action is not entirely clear. We performed a systematic analysis of the effects of anticholinergic drugs on short- and long-term plasticity recorded from striatal medium spiny neurons from DYT1 dystonia knock-in (Tor1a(+/Δgag) ) mice heterozygous for ΔE-torsinA and their controls (Tor1a(+/+) mice). Antagonists were chosen that had previously been proposed to be selective for muscarinic receptor subtypes and included pirenzepine, trihexyphenydil, biperiden, orphenadrine, and a novel selective M1 antagonist, VU0255035...
November 2014: Movement Disorders: Official Journal of the Movement Disorder Society
Emmanuela Marchi, Leonardo Furi, Stefania Arioli, Ian Morrissey, Valeria Di Lorenzo, Diego Mora, Luciana Giovannetti, Marco Rinaldo Oggioni, Carlo Viti
Staphylococcus aureus strains harboring QacA, QacB, QacC, QacG transporters and norA promoter up-regulating mutations were characterized by phenotype microarray (PM), standard methods for susceptibility testing, and ethidium bromide efflux assays, in order to increase knowledge on phenotypes associated to efflux pumps and their substrates. PM data and standard susceptibility testing lead to the identification of new potential efflux targets, such as guanidine hydrochloride or 8-hydroxyquinoline for QacA and QacC pumps, respectively...
January 2015: Microbiological Research
Iu I Hubs'kyĭ, T A Bukhtiarova, H H Horiushko, N V Litvinova, H I Paramonova, T M Kurapova, O M Velychko, L P Babenko
Methods of fluorescent probing, spectrophotometry and microcalorimetry were applied to investigate the alterations in biophysical parameters of erythrocytes membranes, and specifically microviscosity, surface charge, molecular organization of lipid bilayer and lipid-protein interactions under conditions of acute pain syndrome produced by experimental chemical lesion. The distinctive features of non-opiod analgesics interactions and binding to the erythrocytes membranes of rats subjected to acute nociceptive pain accompanied with oxidative stress development were investigated...
May 2014: Ukrainian Biochemical Journal
Konrad Rejdak, Dorota Nieoczym, Mirosław Czuczwar, Jacek Kiś, Piotr Wlaź, Waldemar A Turski
BACKGROUND: Identification of new molecular targets as well as the new models recapitulating different aspects of pathophysiology of status epilepticus (SE) in humans might prove essential for the breakthrough in the efforts against pharmacoresistance in epilepsy. Recently, we described a new model of generalized convulsive SE induced with orphenadrine (ORPH) in rats with unique characteristics [5]. The current study was aimed at assessing the efficacy of a new generation antiepileptic drugs (AEDs) and some of the experimental agents in suppressing ORPH-evoked seizures in rats...
June 2014: Pharmacological Reports: PR
Jean-François Desaphy, Roberta Carbonara, Teresa Costanza, Diana Conte Camerino
Although the sodium channel blocker mexiletine is considered the first-line drug in myotonia, some patients experiment adverse effects, while others do not gain any benefit. Other antimyotonic drugs are thus needed to offer mexiletine alternatives. In the present study, we used a previously-validated rat model of myotonia congenita to compare six marketed sodium channel blockers to mexiletine. Myotonia was induced in the rat by injection of anthracen-9-carboxylic acid, a muscle chloride channel blocker. The drugs were given orally and myotonia was evaluated by measuring the time of righting reflex...
May 2014: Experimental Neurology
Xuexuan Wang, Laura Black
This ex vivo human percutaneous absorption study evaluated a set of six model drugs (ketamine hydrochloride, bupivacaine hydrochloride, diclofenac sodium, gabapentin, orphenadrine citrate, pentoxifylline) from two popular formulations for topically applied compounding preparations. The compounded preparations used in this study were Versatile cream and a reference cream. Each formulation was applied to human trunk skin mounted on Franz Diffusion Cells, 50 mg/chamber (or 28.2 mg/cm2). Serial dermal receiver solutions were collected for 48 hours...
November 2013: International Journal of Pharmaceutical Compounding
Maha M Abdelrahman
Comparable double divisor ratio spectra derivative, area under curve of derivative ratio and mean centering of ratio spectra spectrophotometric methods were introduced for determination of orphenadrine citrate (ORPH), caffeine (CAF) and aspirin (ASP); a combination for symptomatic relief of mild to moderate pain of acute musculoskeletal disorders; with evident accuracy and precision. The suggested methods have the advantage over the previously published spectrophotometric method for determination of the same combination in that they did not require a preliminary separation step and able to resolve the ternary mixture, with severe overlapping spectra, with competent sensitivity and selectivity...
April 24, 2014: Spectrochimica Acta. Part A, Molecular and Biomolecular Spectroscopy
Leonore Wetzel, Markus Zadrazil, Tatjana Paternostro-Sluga, Georg Authried, Sibylle Kozek-Langenecker, Gisela Scharbert
BACKGROUND: Addition of nonopioid analgesic drugs reduces pain and opioid requirements in acute low back pain. In noncancer chronic low back pain (CLBP), the efficacy of a combined regimen to reduce breakthrough pain has not been proven so far. OBJECTIVE: Evaluation of the effects of intravenous (i.v.) nonopioid analgesic drugs on pain intensity and lumbar mobility in CLBP patients on chronic opioid therapy. DESIGN: Randomised, placebo-controlled, double blinded, crossover study...
January 2014: European Journal of Anaesthesiology
Dana N Haj-Ali, Imad I Hamdan
A validated method using capillary electrophoresis was developed, for the determination of orphenadrine citrate in its tablet formulations, in the presence of paracetamol. The method employs a running buffer of 30 mM pentane sulfonate sodium, dissolved in 20 mM MOPS buffer pH 7.7. Samples were injected using hydrodynamic sample injection mode (25 mbar, for 25 s), using positive polarity of 25 kV, at a constant temperature of 30 °C. Samples of orphenadrine citrate alone or in mixture solutions with paracetamol were exposed to various degradation conditions, and were electrophoresed using the recommended condition...
October 2010: Saudi Pharmaceutical Journal: SPJ: the Official Publication of the Saudi Pharmaceutical Society
Lorena M A Silva, Elenilson G A Filho, Sérgio S Thomasi, Bianca F Silva, Antonio G Ferreira, Tiago Venâncio
The informal (and/or illegal) e-commerce of pharmaceutical formulations causes problems that governmental health agencies find hard to control, one of which concerns formulas sold as natural products. The purpose of this work was to explore the advantages and limitations of DOSY and HPLC-UV-SPE-NMR. These techniques were used to identify the components of a formula illegally marketed in Brazil as an herbal medicine possessing anti-inflammatory and analgesic properties. DOSY was able to detect the major components present at higher concentrations...
September 2013: Magnetic Resonance in Chemistry: MRC
Lucía Asensi-Bernardi, Laura Escuder-Gilabert, Yolanda Martín-Biosca, Salvador Sagrado, María José Medina-Hernández
The estimation of apparent binding constants and limit mobilities of the complexes of the enantiomers that characterize the interaction of enantiomers with chiral selectors, in this case highly sulfated β-cyclodextrin, was approached using a simple and economic electrophoretic modality, the complete filling technique (CFT) in counter-current mode. The enantiomers of eight psychoactive drugs, four antihistamines (dimethindene, promethazine, orphenadrine and terfenadine) and four antidepressants (bupropion, fluoxetine, nomifensine and viloxazine) were separated for the first time for this cyclodextrin (CD)...
January 2014: Biomedical Chromatography: BMC
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