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Pharmacological inertness

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https://www.readbyqxmd.com/read/28866743/effects-of-oral-%C3%AE-9-tetrahydrocannabinol-on-the-cerebral-processing-of-olfactory-input-in-healthy-non-addicted-subjects
#1
Carmen Walter, Bruno G Oertel, Lisa Felden, Ulrike Nöth, Johannes Vermehren, Ralf Deichmann, Jörn Lötsch
BACKGROUND: Considering the increasing acknowledgment of the human sense of smell as a significant component of the quality of life, olfactory drug effects gain potential clinical importance. A recent observation in a human experimental context indicated that Δ(9)-tetrahydrocannabinol (THC) impaired the subject's performance in olfactory tests. To further analyze the role of THC in human olfaction, the present report addresses its effects on the central processing of olfactory stimuli...
September 2, 2017: European Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28794102/optogenetics-and-pharmacogenetics-principles-and-applications
#2
Jingwei Jiang, Huxing Cui, Kamal Rahmouni
Remote and selective spatiotemporal control of the activity of neurons to regulate behavior and physiological functions has been a long-sought goal in system neuroscience. Identification and subsequent bioengineering of light-sensitive ion channels (e.g., channelrhodopsins, halorhodopsin and archaerhodopsins) from the bacteria has made it possible to utilize light to artificially modulate neuronal activity, namely optogenetics. Recent advance in genetics has also allowed development of novel pharmacological tools to selectively and remotely control neuronal activity using engineered G-protein coupled receptors which can be activated by otherwise inert drug-like small molecules such as the Designer Receptors Exclusively Activated by Designer Drug (DREADD) - a form of chemogenetics...
August 9, 2017: American Journal of Physiology. Regulatory, Integrative and Comparative Physiology
https://www.readbyqxmd.com/read/28761201/the-impact-of-methylphenidate-on-motor-performance-in-children-with-both-attention-deficit-hyperactivity-disorder-and-developmental-coordination-disorder-a-randomized-double-blind-crossover-clinical-trial
#3
Robabeh Soleimani, Maryam Kousha, Homa Zarrabi, Seyede Mahnaz Tavafzadeh-Haghi, Mir Mohammad Jalali
BACKGROUND: Children with attention deficit hyperactivity disorder/developmental coordination disorder (ADHD/DCD) suffer from problems associated with gross and fine motor skills. There is no effective pharmacological therapy for such patients. We aimed to assess the impact of methylphenidate (MPH) on motor performance of children with ADHD/DCD. METHODS: In this double-blind placebo-controlled, 17 children (12 boys) with ADHD/DCD with a mean age of 7 years 6 months were recruited in Shafa Hospital, Rasht, Iran...
July 2017: Iranian Journal of Medical Sciences
https://www.readbyqxmd.com/read/28727700/therapeutic-role-of-placebo-evolution-of-a-new-paradigm-in-understanding-research-and-clinical-practice
#4
Laxmaiah Manchikanti, Mark V Boswell, Alan D Kaye, Standiford Helm Ii, Joshua A Hirsch
Research into interventional techniques in managing chronic spinal pain continues to be challenging, mystifying, confusing, and biased. Insight, or lack thereof, into placebo and nocebo phenomena contributes mightily to these difficulties. Unfortunately, placebo-nocebo responses are the subject of numerous controversies and challenges from not only a research perspective, but also clinical perspective. While interventionalists consider the biggest threat to interventional pain management research is inappropriate and outdated interpretation of the data, a greater problem is the misuse of the placebo response in research, with the declaration that all and everything as a placebo effect: with a misinterpretation of the nature of the placebo the, associated conclusions can be inaccurate...
July 2017: Pain Physician
https://www.readbyqxmd.com/read/28670327/asthma-pressurised-metered-dose-inhaler-performance-propellant-effect-studies-in-delivery-systems
#5
William F S Sellers
BACKGROUND: Current pressurised metered dose asthma inhaler (pMDI) propellants are not inert pharmacologically as were previous chlorofluorocarbons, have smooth muscle relaxant' partial pressure effects in the lungs and inhaled hydrofluoroalkane 134a (norflurane) has anaesthetic effects. Volumes of propellant gas per actuation have never been measured. METHODS: In-vitro studies measured gas volumes produced by pMDIs on air oxygen (O2) levels in valved holding chambers (VHC) and the falls in O2% following actuation into lung ventilator delivery devices...
2017: Allergy, Asthma, and Clinical Immunology
https://www.readbyqxmd.com/read/28423064/biochemical-evaluation-of-the-anticancer-potential-of-the-polyamine-based-nanocarrier-nano11047
#6
Tracy Murray-Stewart, Elena Ferrari, Ying Xie, Fei Yu, Laurence J Marton, David Oupicky, Robert A Casero
Synthesizing polycationic polymers directly from existing drugs overcomes the drug-loading limitations often associated with pharmacologically inert nanocarriers. We recently described nanocarriers formed from a first-generation polyamine analogue, bis(ethyl)norspermine (BENSpm), that could simultaneously target polyamine metabolism while delivering therapeutic nucleic acids. In the current study, we describe the synthesis and evaluation of self-immolative nanocarriers derived from the second-generation polyamine analogue PG-11047...
2017: PloS One
https://www.readbyqxmd.com/read/28383527/activation-of-the-hypoglossal-to-tongue-musculature-motor-pathway-by-remote-control
#7
Garret A Horton, Jimmy J Fraigne, Zoltan A Torontali, Matthew B Snow, Jennifer L Lapierre, Hattie Liu, Gaspard Montandon, John H Peever, Richard L Horner
Reduced tongue muscle tone precipitates obstructive sleep apnea (OSA), and activation of the tongue musculature can lessen OSA. The hypoglossal motor nucleus (HMN) innervates the tongue muscles but there is no pharmacological agent currently able to selectively manipulate a channel (e.g., Kir2.4) that is highly restricted in its expression to cranial motor pools such as the HMN. To model the effect of manipulating such a restricted target, we introduced a "designer" receptor into the HMN and selectively modulated it with a "designer" drug...
April 6, 2017: Scientific Reports
https://www.readbyqxmd.com/read/28165442/antimicrobial-efficacy-of-probiotic-containing-toothpastes-an-in-vitro-evaluation
#8
Miro Klarić, Vjekoslav Mandić, Sanjin Lovrić, Martina Krešić Ćorić, Nikolina Zovko
Most people have heard of the placebo effect, while relatively few have heard of nocebo, even within the circles of medical staff. Placebo effect means positive results by treatment via pharmacological inert substances. In contrast to placebo, by nocebo effect, due to negative beliefs and expectations, opposite results are achieved. Said in a more formal manner, what a sick person expects, unfortunately, he/she most often gets. It is a fact that a high number of medical staff is still uninterested in placebo and nocebo effects, although they would benefit from them...
February 1, 2017: Medicinski Glasnik
https://www.readbyqxmd.com/read/28131852/interaction-of-pharmaceutical-excipients-with-organic-cation-transporters
#9
Sirima Soodvilai, Sunhapas Soodvilai, Varanuj Chatsudthipong, Tanasait Ngawhirunpat, Theerasak Rojanarata, Praneet Opanasopit
Increasing evidences have shown that many pharmaceutical excipients are not pharmacologically inert but instead have effects on several transport function of uptake and efflux drug transporters. Herein, we investigated whether the excipients frequently used in many drug formulations affect transport function of organic cation transporters (OCTs) that are responsible for elimination of cationic drugs. Our finding revealed that solubilizing agents, Tweens, showed the most significant effect rbOCT1/2-mediated [(3)H]-MPP(+) uptake in heterologous expressing cells...
January 25, 2017: International Journal of Pharmaceutics
https://www.readbyqxmd.com/read/28068474/chemoselective-hydrodehalogenation-of-organic-halides-utilizing-two-dimensional-anionic-electrons-of-inorganic-electride-ca2n-%C3%A2-e
#10
Ye Ji Kim, Sun Min Kim, Chunghyeon Yu, YoungMin Yoo, Eun Jin Cho, Jung Woon Yang, Sung Wng Kim
Halogenated organic compounds are important anthropogenic chemicals widely used in chemical industry, biology, and pharmacology; however, the persistence and inertness of organic halides cause human health problems and considerable environmental pollution. Thus, the elimination or replacement of halogen atoms with organic halides has been considered a central task in synthetic chemistry. In dehalogenation reactions, the consecutive single-electron transfer from reducing agents generates the radical and corresponding carbanion and thus removes the halogen atom as the leaving group...
January 20, 2017: Langmuir: the ACS Journal of Surfaces and Colloids
https://www.readbyqxmd.com/read/27996095/biological-and-pharmacological-evaluation-of-dimethoxycurcumin-a-metabolically-stable-curcumin-analogue-with-a-promising-therapeutic-potential
#11
Manouchehr Teymouri, Nastaran Barati, Matteo Pirro, Amirhosein Sahebkar
Dimethoxycurcumin (DiMC) is a synthetic analog of curcumin with superior inter-related pro-oxidant and anti-cancer activity, and metabolic stability. Numerous studies have shown that DiMC reserves the biologically beneficial features, including anti-inflammatory, anti-carcinogenic, and cytoprotective properties, almost to the same extent as curcumin exhibits. DiMC lacks the phenolic-OH groups as opposed to curcumin, dimethoxycurcumin, and bis-demethoxycurcumin that all vary in the number of methoxy groups per molecule, and has drawn the attentions of researchers who attempted to discover the structure-activity relationship (SAR) of curcumin...
December 20, 2016: Journal of Cellular Physiology
https://www.readbyqxmd.com/read/27906137/in-vitro-toxicity-of-carbon-nanotube-polylysine-colloids-to-colon-cancer-cells
#12
Alejandro Ansón-Casaos, Laura Grasa, Desirée Pereboom, José Emilio Mesonero, Alvaro Casanova, María Divina Murillo, María Teresa Martínez
Single-walled carbon nanotubes (SWCNTs) are thoroughly purified and dispersed in an aqueous solution of high molecular weight poly-L-lysine (pLlys). Human intestinal epithelial Caco-2/TC7 cells are incubated with the SWCNT dispersions in pLlys, and their effects on cell viability are studied by image flow cytometry. No significant changes are observed in the cell culture wells up to pLlys concentrations of 10 μg ml(-1). However, high mortality is detected at pLlys concentrations of 100 μg ml(-1). The presence of oxygen-free SWCNTs does not modify the effects of pLlys on cell cultures at any of the tested concentrations (≤1 μg ml(-1))...
December 2016: IET Nanobiotechnology
https://www.readbyqxmd.com/read/27514542/how-valid-is-placebo-in-the-indian-setting
#13
Himanshu Sharma, Bharti Sharma
BACKGROUND: The Placebo is defined as an inert substance with a potent therapeutic effect. Its effect is attributed to its psychological and neurobiological effect. Its use in Psychiatric drug practice, drug trials and clinical practice is common, especially in India. Currently there is a debate whether to use it or not as there are ethical, moral and legal issues. Also, its mechanism of action is not known. DISCUSSION: The Indian Psychiatry scenario is muddled in relation to use of placebo in Randomized Controlled Trials or Psychiatric clinical practice...
2017: Central Nervous System Agents in Medicinal Chemistry
https://www.readbyqxmd.com/read/27461895/deciphering-and-modulating-g-protein-signalling-in-c-elegans-using-the-dreadd-technology
#14
Simone Prömel, Franziska Fiedler, Claudia Binder, Jana Winkler, Torsten Schöneberg, Doreen Thor
G-protein signalling is an evolutionary conserved concept highlighting its fundamental impact on developmental and functional processes. Studies on the effects of G protein signals on tissues as well as an entire organism are often conducted in Caenorhabditis elegans. To understand and control dynamics and kinetics of the processes involved, pharmacological modulation of specific G protein pathways would be advantageous, but is difficult due to a lack in accessibility and regulation. To provide this option, we designed G protein-coupled receptor-based designer receptors (DREADDs) for C...
2016: Scientific Reports
https://www.readbyqxmd.com/read/27404844/chemogenetic-silencing-of-the-midline-and-intralaminar-thalamus-blocks-amygdala-kindled-seizures
#15
Evan Wicker, Patrick A Forcelli
Temporal lobe epilepsy is the most common form of medically-intractable epilepsy. While seizures in TLE originate in structures such as hippocampus, amygdala, and temporal cortex, they propagate through a crucial relay: the midline/intralaminar thalamus. Prior studies have shown that pharmacological inhibition of midline thalamus attenuates limbic seizures. Here, we examined a recently developed technology, Designer Receptors Exclusively Activated by Designer Drugs (DREADDs), as a means of chemogenetic silencing to attenuate limbic seizures...
September 2016: Experimental Neurology
https://www.readbyqxmd.com/read/27189887/stable-and-biocompatible-cystine-knot-peptides-from-the-marine-sponge-asteropus-sp
#16
Mingzhi Su, Huayue Li, Haibo Wang, Eun La Kim, Hyung Sik Kim, Eun-Hee Kim, Jaewon Lee, Jee H Jung
Two new cystine knot peptides, asteropsins F (ASPF) and G (ASPG), were isolated from the marine sponge Asteropus sp. ASPF and ASPG are composed of 33 and 32 amino acids, respectively, and contain six cysteines which are involved in three disulfide bonds. They shared the characteristic features of the asteropsin family, such as, N-terminal pyroglutamate modification, incorporation of cis prolines, and the unique anionic profile, which distinguish them from other knottin families. Tertiary structures of the peptides were determined by high resolution NMR...
July 1, 2016: Bioorganic & Medicinal Chemistry
https://www.readbyqxmd.com/read/27184579/the-effects-of-pharmaceutical-excipients-on-gastrointestinal-tract-metabolic-enzymes-and-transporters-an-update
#17
COMMENT
Wenpeng Zhang, Yanyan Li, Peng Zou, Man Wu, Zhenqing Zhang, Tao Zhang
Accumulating evidence from the last decade has shown that many pharmaceutical excipients are not pharmacologically inert but instead have effects on metabolic enzymes and/or drug transporters. Hence, the absorption, distribution, metabolism, and elimination (ADME) of active pharmaceutical ingredients (APIs) may be altered due to the modulation of their metabolism and transport by excipients. The impact of excipients is a potential concern for Biopharmaceutics Classification System (BCS)-based biowaivers, particularly as the BCS-based biowaivers have been extended to class 3 drugs in certain dosage forms...
2016: AAPS Journal
https://www.readbyqxmd.com/read/27152864/endothelial-cells-use-a-formin-dependent-phagocytosis-like-process-to-internalize-the-bacterium-listeria-monocytogenes
#18
Michelle Rengarajan, Arnold Hayer, Julie A Theriot
Vascular endothelial cells act as gatekeepers that protect underlying tissue from blood-borne toxins and pathogens. Nevertheless, endothelial cells are able to internalize large fibrin clots and apoptotic debris from the bloodstream, although the precise mechanism of such phagocytosis-like uptake is unknown. We show that cultured primary human endothelial cells (HUVEC) internalize both pathogenic and non-pathogenic Listeria bacteria comparably, in a phagocytosis-like process. In contrast with previously studied host cell types, including intestinal epithelial cells and hepatocytes, we find that endothelial internalization of Listeria is independent of all known pathogenic bacterial surface proteins...
May 2016: PLoS Pathogens
https://www.readbyqxmd.com/read/27062187/treatment-history-and-placebo-responses-to-experimental-and-clinical-pain-in-chronic-pain-patients
#19
M Müller, S Kamping, J Benrath, H Skowronek, J Schmitz, R Klinger, H Flor
BACKGROUND: Placebo analgesia refers to the reduction in pain due to the administration of an inert treatment. It is induced by expectations of pain relief which are enhanced by learning mechanisms. In healthy humans, prior positive experiences enhance the placebo response. However, the effects of patients' prior experiences with treatment on placebo responses have not yet been examined. This study investigated how verbal information, learning and treatment history influence the magnitude of placebo analgesia in chronic pain...
October 2016: European Journal of Pain: EJP
https://www.readbyqxmd.com/read/27055943/the-role-of-the-equatorial-ligands-for-the-redox-behavior-mode-of-cellular-accumulation-and-cytotoxicity-of-platinum-iv-prodrugs
#20
Simone Göschl, Hristo P Varbanov, Sarah Theiner, Michael A Jakupec, Markus Galanski, Bernhard K Keppler
The current study aims to elucidate the possible reasons for the significantly different pharmacological behavior of platinum(IV) complexes with cisplatin-, carboplatin- or nedaplatin-like cores and how this difference can be related to their main physicochemical properties. Chlorido-containing complexes are reduced fast (within hours) by ascorbate and are able to unwind plasmid DNA in the presence of ascorbate, while their tri- and tetracarboxylato analogs are generally inert under the same conditions. Comparison of the lipophilicity, cellular accumulation and cytotoxicity of the investigated platinum compounds revealed the necessity to define new structure-property/activity relationships (SPRs and SARs)...
July 2016: Journal of Inorganic Biochemistry
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