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N-type calcium channels antagonists

Brian M Bruel, Allen W Burton
OBJECTIVE: The increasing incidence of cancer survivorship has shifted treatment of cancer-related pain from short-term analgesia to long-term chronic pain management. As a result, alternatives to oral analgesics, such as intrathecal therapy, may be beneficial for patients with cancer-related pain. The authors review the use of intrathecal therapy in the management of cancer-related pain. METHODS: The Medline database was searched for English-language articles that included "ziconotide" or "morphine" AND ("cancer" OR "malignant") AND "intrathecal" in title or abstract...
December 2016: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
D D Zerbino, E A Zimba, N N Bagry
Thromboangiitis obliterans (Buerger's disease) is systemic vasculitis with predominant development of thrombotic occlusions of small-to-medium diameter arteries of distal portions of both upper and lower limbs. A distinctive feature of Buerger's disease from other vasculitides is the involvement of the venous bed into the pathological process in the form of migrating thrombophlebitis. The disease is encountered more often in young adult males, predominantly tobacco smokers. The clinical pattern is presented by symptoms of increasing insufficiency of blood supply of tissues of extremities...
2016: Angiologii︠a︡ i Sosudistai︠a︡ Khirurgii︠a︡, Angiology and Vascular Surgery
Senad Pesto, Zijo Begic, Sabina Prevljak, Ehlimana Pecar, Nihad Kukavica, Edin Begic
Pulmonary hypertension is a pathophysiological state hemodynamically defined as the increase of the mean pulmonary arterial pressure above 25, or 30 mmHg at rest, measured by catheterization of the right heart. Laboratory findings usually reveals polycythemia, the ECG right ventricle hypertrophy, and x-ray characteristic of diseased branches (echocardiography and biomarkers such as B-type natriuretic peptide (BNP) and N-terminal pro-BNP hormones are potentially helpful tools in identifying PH). Echocardiography can be found the increase of the right atrium and ventricle, right ventricular hypertrophy, abnormal contraction of the interventricular septum, left ventricular diastolic dysfunction and decreased left ventricular size, with reduced volumes of systole and end diastole...
July 27, 2016: Medical Archives
Naoki Tsuno, Akira Yukimasa, Osamu Yoshida, Yusuke Ichihashi, Takatsugu Inoue, Tatsuhiko Ueno, Hiroki Yamaguchi, Hidetoshi Matsuda, Satoko Funaki, Natsue Yamanada, Miki Tanimura, Daiki Nagamatsu, Yoko Nishimura, Tetsuji Ito, Masahiko Soga, Narumi Horita, Miyuki Yamamoto, Mikie Hinata, Masayuki Imai, Yasuhide Morioka, Toshiyuki Kanemasa, Gaku Sakaguchi, Yasuyoshi Iso
A novel series of 2',4'-dimethyl-[4,5'-bithiazol]-2-yl amino derivatives were found by high throughput screening of the TRPV4 receptor, at which these compounds showed competitive antagonist potential against 4α-phorbol 12,13-didecanoate (4αPDD) as the selective TRPV4 agonist and showed excellent selectivity for TRPV1, N-type and L-type calcium ion channels, but poor ADME profile. In our SAR strategy, we found that the lead molecule 1 also having the unique 3-oxa-9-azabicyclo [3.3.1] nonan-7-one on the right part showed potent TRPV4 antagonist activity, good solubility at pH 6...
October 15, 2016: Bioorganic & Medicinal Chemistry Letters
Eileen Rodriguez-Tapia, Alberto Perez-Medina, Xiaochun Bian, James J Galligan
Enteric inhibitory motoneurons use nitric oxide and a purine neurotransmitter to relax gastrointestinal smooth muscle. Enteric P/Q-type Ca(2+) channels contribute to excitatory neuromuscular transmission; their contribution to inhibitory transmission is less clear. We used the colon from tottering mice (tg/tg, loss of function mutation in the α1A pore-forming subunit of P/Q-type Ca(2+) channels) to test the hypothesis that P/Q-type Ca(2+) channels contribute to inhibitory neuromuscular transmission and colonic propulsive motility...
October 1, 2016: American Journal of Physiology. Gastrointestinal and Liver Physiology
Luana Heimfarth, Fernanda da Silva Ferreira, Paula Pierozan, Samanta Oliveira Loureiro, Moara Rodrigues Mingori, José Cláudio Fonseca Moreira, João Batista Teixeira da Rocha, Regina Pessoa-Pureur
BACKGROUND: Diphenylditelluride (PhTe)2 is a potent neurotoxin disrupting the homeostasis of the cytoskeleton. METHODS: Cultured astrocytes and neurons were incubated with (PhTe)2, receptor antagonists and enzyme inhibitors followed by measurement of the incorporation of [32P]orthophosphate into intermediate filaments (IFs). RESULTS: (PhTe)2 caused hyperphosphorylation of glial fibrillary acidic protein (GFAP), vimentin and neurofilament subunits (NFL, NFM and NFH) from primary astrocytes and neurons, respectively...
November 2016: Biochimica et Biophysica Acta
Wendie N Marks, Quentin Greba, Stuart M Cain, Terrance P Snutch, John G Howland
The role of T-type calcium channels in brain diseases such as absence epilepsy and neuropathic pain has been studied extensively. However, less is known regarding the involvement of T-type channels in cognition and behavior. Prepulse inhibition (PPI) is a measure of sensorimotor gating which is a basic process whereby the brain filters incoming stimuli to enable appropriate responding in sensory rich environments. The regulation of PPI involves a network of limbic, cortical, striatal, pallidal and pontine brain areas, many of which show high levels of T-type calcium channel expression...
September 22, 2016: Neuroscience
Katrin Kistner, Norbert Siklosi, Alexandru Babes, Mohammad Khalil, Tudor Selescu, Katharina Zimmermann, Stefan Wirtz, Christoph Becker, Markus F Neurath, Peter W Reeh, Matthias A Engel
We demonstrate a novel dual strategy against inflammation and pain through body-wide desensitization of nociceptors via TRPA1. Attenuation of experimental colitis by capsazepine (CPZ) has long been attributed to its antagonistic action on TRPV1 and associated inhibition of neurogenic inflammation. In contrast, we found that CPZ exerts its anti-inflammatory effects via profound desensitization of TRPA1. Micromolar CPZ induced calcium influx in isolated dorsal root ganglion (DRG) neurons from wild-type (WT) but not TRPA1-deficient mice...
2016: Scientific Reports
Wendie N Marks, Stuart M Cain, Terrance P Snutch, John G Howland
Childhood absence epilepsy (CAE) is often comorbid with behavioral and cognitive symptoms, including impaired visual memory. Genetic Absence Epilepsy Rats from Strasbourg (GAERS) is an animal model closely resembling CAE; however, cognition in GAERS is poorly understood. Crossmodal object recognition (CMOR) is a recently developed memory task that examines not only purely visual and tactile memory, but also requires rodents to integrate sensory information about objects gained from tactile exploration to enable visual recognition...
October 2016: Neurobiology of Disease
Takuma Nishijo, Toshihiko Momiyama
Modulatory roles of serotonin (5-HT) in GABAergic transmission onto basal forebrain cholinergic neurons were investigated, using whole-cell patch-clamp technique in the rat brain slices. GABAA receptor-mediated inhibitory postsynaptic currents (IPSCs) were evoked by focal stimulation. Bath application of 5-HT (0.1-300 μm) reversibly suppressed the amplitude of evoked IPSCs in a concentration-dependent manner. Application of a 5-HT1B receptor agonist, CP93129, also suppressed the evoked IPSCs, whereas a 5-HT1A receptor agonist, 8-OH-DPAT had little effect on the evoked IPSCs amplitude...
July 2016: European Journal of Neuroscience
Brian M Bruel, Allen W Burton
OBJECTIVE: The increasing incidence of cancer survivorship has shifted treatment of cancer-related pain from short-term analgesia to long-term chronic pain management. As a result, alternatives to oral analgesics, such as intrathecal therapy, may be beneficial for patients with cancer-related pain. The authors review the use of intrathecal therapy in the management of cancer-related pain. METHODS: The Medline database was searched for English-language articles that included "ziconotide" or "morphine" AND ("cancer" OR "malignant") AND "intrathecal" in title or abstract...
April 28, 2016: Pain Medicine: the Official Journal of the American Academy of Pain Medicine
Helena Viola, Victoria Johnstone, Henrietta Cserne Szappanos, Tara Richman, Tatiana Tsoutsman, Aleksandra Filipovska, Christopher Semsarian, Livia Hool
KEY POINTS: Genetic mutations in cardiac troponin I (cTnI) are associated with development of hypertrophic cardiomyopathy characterized by myocyte remodelling, disorganization of cytoskeletal proteins and altered energy metabolism. The L-type Ca(2+) channel is the main route for calcium influx and is crucial to cardiac excitation and contraction. The channel also regulates mitochondrial function in the heart by a functional communication between the channel and mitochondria via the cytoskeletal network...
July 15, 2016: Journal of Physiology
Yu V Karpets, Yu E Kolupaev, T O Yastreb
The effects of functional interplay of calcium ions, reactive oxygen species (ROS) and nitric oxide (NO) in the cells of wheat plantlets roots (Triticum aestivum L.) at the induction of their heat resistance by a short-term influence of hyperthermia (heating at the temperature of 42 degrees C during 1 minute) have been investigated. The transitional increase of NO and H2O2 content, invoked by heating, was suppressed by the treatment of plantlets with the antagonists of calcium EGTA (chelator of exocellular calcium), lanthanum chloride (blocker of calcium channels of various types) and neomycin (inhibitor of phosphatidylinositol-dependent phospholipase C)...
November 2015: Ukrainian Biochemical Journal
Andrew O Jo, Monika Lakk, Amber M Frye, Tam T T Phuong, Sarah N Redmon, Robin Roberts, Bruce A Berkowitz, Oleg Yarishkin, David Križaj
Fluid secretion by the ciliary body plays a critical and irreplaceable function in vertebrate vision by providing nutritive support to the cornea and lens, and by maintaining intraocular pressure. Here, we identify TRPV4 (transient receptor potential vanilloid isoform 4) channels as key osmosensors in nonpigmented epithelial (NPE) cells of the mouse ciliary body. Hypotonic swelling and the selective agonist GSK1016790A (EC50 ∼33 nM) induced sustained transmembrane cation currents and cytosolic [Formula: see text] elevations in dissociated and intact NPE cells...
April 5, 2016: Proceedings of the National Academy of Sciences of the United States of America
Ha Thi Thanh Nguyen, Hai Thanh Nguyen, Md Zahorul Islam, Takeshi Obi, Pitchaya Pothinuch, Phyu Phyu Khine Zar, De Xing Hou, Thanh Van Nguyen, Tuong Manh Nguyen, Cuong Van Dao, Mitsuya Shiraishi, Atsushi Miyamoto
ETHNOPHARMACOLOGICAL RELEVANCE: In Vietnamese traditional herbalism, there are conflicting opinions about the effect of Artemisia vulgaris L. (AVL, English name: mugwort) on hypertension. Some ethnic doctors recommend the use of AVL for treatment of hypertension, whereas others advise against it. The purpose of this study was to clarify the pharmacological characteristics of AVL in isolated arteries to explain the conflicts surrounding the use of AVL for treatment of hypertension. MATERIALS AND METHODS: We initially performed a functional study using an organ bath system to investigate the effect of AVL extract on isolated porcine basilar artery...
April 22, 2016: Journal of Ethnopharmacology
Thomas Stueber, Mirjam J Eberhardt, Christoph Hadamitzky, Annette Jangra, Stefan Schenk, Felicia Dick, Carsten Stoetzer, Katrin Kistner, Peter W Reeh, Alexander M Binshtok, Andreas Leffler
BACKGROUND: The relatively membrane-impermeable lidocaine derivative QX-314 has been reported to permeate the ion channels transient receptor potential vanilloid 1 (TRPV1) and transient receptor potential cation channel, subfamily A, member 1 (TRPA1) to induce a selective inhibition of sensory neurons. This approach is effective in rodents, but it also seems to be associated with neurotoxicity. The authors examined whether the human isoforms of TRPV1 and TRPA1 allow intracellular entry of QX-314 to mediate sodium channel inhibition and cytotoxicity...
May 2016: Anesthesiology
Alessia Bertamino, Carmine Ostacolo, Paolo Ambrosino, Simona Musella, Veronica Di Sarno, Tania Ciaglia, Maria Virginia Soldovieri, Nunzio Iraci, Asia Fernandez Carvajal, Roberto de la Torre-Martinez, Antonio Ferrer-Montiel, Rosario Gonzalez Muniz, Ettore Novellino, Maurizio Taglialatela, Pietro Campiglia, Isabel Gomez-Monterrey
Pharmacological modulation of the transient receptor potential melastatin type 8 (TRPM8) is currently under investigation as a new approach for the treatment of pain and other diseases. In this study, a series of N-substituted tryptamines was prepared to explore the structural requirements determining TRPM8 modulation. Using a fluorescence-based screening assay, we identified two compounds acting as an activator (2-(1H-indol-3-yl)-N-(4-phenoxybenzyl)ethanamine, 21) or an inhibitor (N,N-dibenzyl-2-(1H-indol-3-yl)ethanamine, 12) of calcium influx in HEK293 cells...
March 10, 2016: Journal of Medicinal Chemistry
David L S Washburn, Alastair V Ferguson
1 Here we have characterized Ca(2+) currents in rat subfornical organ neurones, and their modulation by angiotensin II. Currents were of the high voltage-activated (HNA) subtype, as the threshold for activation was near -30 mV (mid-point potential (V50 ) of activation -14 mV). Using Ba(2+) as the charge carrier, little inactivation was observed, and it occurred only at depolarized potentials (V50 of inactivation -12 mV). More inactivation was observed using Ca(2+) as the charge carrier, indicating that Ca(2+) -dependent inactivation plays a role in regulating Ca(2+) channel function in subfornical organ (SFO) neurones...
November 2001: Journal of Physiology
J C Poncer, R A McKinney, B H Gáhwiler, S M Thompson
1 Paired recordings from monosynaptically connected CA3 interneurons and pyramidal cells of rat hippocampal slice cultures were used to compare the modulation of GABA release at synapses from distinct interneurons. 2 The group II metabotropic glutamate receptor (mGluR) agonist (2S,2'R,3'R)-2-(2',3'-dicarboxylcyclopropyl) glycine (DCG-IV, 5 μm) reduced the amplitude of IPSPs originating from stratum radiatum but not stratum oriens interneurons. In contrast, the GABAB receptor agonist (-)baclofen (10 μm) reduced the amplitude of unitary IPSPs elicited by all interneurons...
October 2000: Journal of Physiology
Géza Berecki, Leonid Motin, David J Adams
Elucidating the mechanisms that modulate calcium channels via opioid receptor activation is fundamental to our understanding of both pain perception and how opioids modulate pain. Neuronal voltage-gated N-type calcium channels (Cav2.2) are inhibited by activation of G protein-coupled opioid receptors (ORs). However, inhibition of R-type (Cav2.3) channels by μ- or κ-ORs is poorly defined and has not been reported for δ-ORs. To investigate such interactions, we coexpressed human μ-, δ-, or κ-ORs with human Cav2...
January 2016: Molecular Pharmacology
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