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chloride channel blockers

Ruilong Hu, Katie A Ferguson, Christina B Whiteus, Dimphna H Meijer, Ricardo C Araneda
An important contribution to neural circuit oscillatory dynamics is the ongoing activation and inactivation of hyperpolarization-activated currents (Ih). Network synchrony dynamics play an important role in the initial processing of odor signals by the main olfactory bulb (MOB) and accessory olfactory bulb (AOB). In the mouse olfactory bulb, we show that Ih is present in granule cells (GCs), the most prominent inhibitory neuron in the olfactory bulb, and that Ih underlies subthreshold resonance in GCs. In accord with the properties of Ih, the currents exhibited sensitivity to changes in extracellular K(+) concentration and ZD7288 (4-ethylphenylamino-1,2-dimethyl-6-methylaminopyrimidin chloride), a blocker of Ih...
September 2016: ENeuro
Mun Fei Yam, Chu Shan Tan, Mariam Ahmad, Ruan Shibao
Orthosiphon stamineus Benth. (Lamiaceae) is an important plant in traditional folk medicine that is used to treat hypertension and kidney stones. In humans, this plant has been tested as an addition regiment for antihypertensive treatment. Among the treatments for hypertension, O. stamineus had been to have diuretic and vasorelaxant effects in animal models. There is still very little information regarding the vasorelaxant effect of O. stamineus. Therefore, the present study was designed to investigate the vasorelaxant activity and mechanism of action of the fractions of O...
October 27, 2016: American Journal of Chinese Medicine
Laurence D Picton, Keith T Sillar
Dopamine plays important roles in the development and modulation of motor control circuits. Here we show that dopamine exerts potent effects on the central pattern generator circuit controlling locomotory swimming in post-embryonic Xenopus tadpoles. Dopamine (0.5-100 μM) reduced fictive swim bout occurrence and caused both spontaneous and evoked episodes to become shorter, slower and weaker. The D2-like receptor agonist quinpirole mimicked this repertoire of inhibitory effects on swimming, whilst the D4 receptor antagonist, L745,870, had the opposite effects...
October 20, 2016: Scientific Reports
Houcemeddine Othman, Silke Andrea Wieninger, Mohamed ElAyeb, Michael Nilges, Najet Srairi-Abid
Glioblastoma is the deadliest type of brain cancer. Treatment could target the Matrix metalloproteinase-2 (MMP-2), which is known to be involved in the invasion process of glioblastoma cells. But current available inhibitors are not selective to MMP-2 due to their interaction with the catalytic binding site, which is highly conserved in all MMPs structures. Interestingly, members of the chloride channel blocker scorpion toxins, such as chlorotoxin (ClTx) and AaCTx, inhibit glioblastoma cell invasion and show a promising therapeutic potential...
September 28, 2016: Journal of Biomolecular Structure & Dynamics
S-H Tang, H-Y Wang, H Sun, N An, L Xiao, Q Sun, D-B Zhao
BACKGROUND: Propofol is a widely used intravenous general anesthetic. Acetylcholine (ACh) is critical in controlling epithelial ion transport. This study was to investigate the effects of propofol on ACh-evoked secretion in rat ileum epithelium. METHODS: The Ussing chamber technique was used to investigate the effects of propofol on carbachol (CCh)-evoked short-circuit currents (Isc). KEY RESULTS: Propofol (10(-2) -10(-6)  mol/L) attenuated CCh-evoked Isc of rat ileum mucosa in a dose-dependent manner...
August 30, 2016: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
Isabella Salzer, Enkhbileg Gantumur, Arsalan Yousuf, Stefan Boehm
Serotonin (5HT) is a constituent of the so-called "inflammatory soup" that sensitizes nociceptors during inflammation. Nevertheless, receptors and signaling mechanisms that mediate an excitation of dorsal root ganglion (DRG) neurons by 5HT remained controversial. Therefore, capsaicin-sensitive nociceptive neurons dissociated from rat DRGs were used to investigate effects of 5HT on membrane excitability and currents through ligand- as well as voltage-gated ion channels. In 58% of the neurons tested, 5HT increased action potential firing, an effect that was abolished by the 5HT2 receptor antagonist ritanserin, but not by the 5HT3 antagonist tropisetron...
November 2016: Neuropharmacology
Som Niyogi, Tamzin A Blewett, Trevor Gallagher, Sandra Fehsenfeld, Chris M Wood
Waterborne zinc (Zn) is known to cause toxicity to freshwater animals primarily by disrupting calcium (Ca) homeostasis during acute exposure, but its effects in marine and estuarine animals are not well characterized. The present study investigated the effects of salinity on short-term Zn accumulation and sub-lethal toxicity in the euryhaline green shore crab, Carcinus maenas. The kinetic and pharmacological properties of short-term branchial Zn uptake were also examined. Green crabs (n=10) were exposed to control (no added Zn) and 50μM (3...
September 2016: Aquatic Toxicology
Michihiro Kudou, Atsushi Shiozaki, Toshiyuki Kosuga, Daisuke Ichikawa, Hirotaka Konishi, Ryo Morimura, Shuhei Komatsu, Hisashi Ikoma, Hitoshi Fujiwara, Kazuma Okamoto, Shigekuni Hosogi, Takashi Nakahari, Yoshinori Marunaka, Eigo Otsuji
Background : Hypotonic shock induces cytocidal effects through cell rupture, and cancer therapy based on this mechanism has been clinically administered to hepatocellular carcinoma patients. We herein investigated the effectiveness of hypotonic shock combined with the inhibition of regulatory volume decrease as cancer therapy for hepatocellular carcinoma. Methods : Morphological changes in human hepatocellular carcinoma cell lines were observed under a differential interference contrast microscope connected to a high-speed digital video camera...
2016: Journal of Cancer
Purum Kang, Kang-Hyun Ryu, Jeong-Min Lee, Hyo-Keun Kim, Geun Hee Seol
Neroli, the essential oil of Citrus aurantium L. var. amara, is a well-characterized alleviative agent used to treat cardiovascular symptoms. However, because it has been found to have multiple effects, its mechanism of action requires further exploration. We sought to clarify the mechanism underlying the actions of neroli in mouse aorta. In aortic rings from mice precontracted with prostaglandin F2 alpha, neroli induced vasodilation. However, relaxation effect of neroli was decreased in endothelium-denuded ring or pre-incubation with the nitric oxide synthase inhibitor NG-Nitro-l-arginine-methyl ester (L-NAME)...
August 2016: Biomedicine & Pharmacotherapy, Biomédecine & Pharmacothérapie
Yang Zhang, Sipei Pan, Xiaolu Zheng, Qi Wan
The present study was to analyze the mechanism of cytomembrane ATP-sensitive K(+) channels (KATP) in the neurovascular unit treatment of ischemic stroke in the recovery period. A total of 24 healthy adult male Wistar rats of 5-8 weeks age, weighing 160-200 g were randomly divided into the control (sham-operation group), model, KATP blocker and KATP opener groups (n=6 rats per group). Nylon cerebral artery occlusion was conducted using nylon monofilament coated with Poly-L-lysine, which was used to produce a cerebral infarction model...
August 2016: Experimental and Therapeutic Medicine
Dayne Laskey, Rajesh Vadlapatla, Katherine Hart
CONTEXT: High-dose insulin has become a first-line therapy for treating severe calcium channel blocker and beta blocker toxicity. Insulin infusions used to treat other conditions (e.g., diabetic ketoacidosis) may be used, but this may lead to pulmonary compromise due to fluid volume overload. An obvious solution would be to use a more concentrated insulin infusion; however, data describing the stability of insulin in polyvinyl chloride bags at concentrations >1 unit/mL are not readily available...
November 2016: Clinical Toxicology
Nan-Lin Xiang, Jun Liu, Yun-Jian Liao, You-Wei Huang, Zheng Wu, Zhi-Quan Bai, Xi Lin, Jian-Hua Zhang
This study investigated the function of a chloride channel blocker, DIDS. Both in vitro and in vivo studies found that DIDS significantly inhibits lipopolysaccharide (LPS)-induced release of proin flammatory cytokines. Here, we show that DIDS inhibits LPS-induced inflammation, as shown by downregulation of inflammatory cytokines via inhibition of the TLR4/NF-κB pathway. Furthermore, we show that ClC-3siRNA transfection reduces LPS-induced pro-inflammation in Raw264.7 cells, indicating that ClC-3 is involved in the inhibitory effect of DIDS during LPS-induced cytokines release...
2016: Scientific Reports
Giedrius Kanaporis, Lothar A Blatter
Cardiac alternans, defined beat-to-beat alternations in contraction, action potential (AP) morphology or cytosolic Ca transient (CaT) amplitude, is a high risk indicator for cardiac arrhythmias. We investigated mechanisms of cardiac alternans in single rabbit ventricular myocytes. CaTs were monitored simultaneously with membrane currents or APs recorded with the patch clamp technique. A strong correlation between beat-to-beat alternations of AP morphology and CaT alternans was observed. During CaT alternans application of voltage clamp protocols in form of pre-recorded APs revealed a prominent Ca(2+)-dependent membrane current consisting of a large outward component coinciding with AP phases 1 and 2, followed by an inward current during AP repolarization...
November 2016: Channels
Xiao-Xue Zhang, Xiao-Chun Min, Xu-Lin Xu, Min Zheng, Lian-Jun Guo
The selective hyperpolarization-activated cyclic nucleotide-gated (HCN) channel blocker 4-(N-ethyl-N-phenylamino)-1,2-dimethyl-6-(methylamino) pyrimidinium chloride (ZD7288) blocks the induction of long-term potentiation in the perforant path-CA3 region in rat hippocampus in vivo. To explore the mechanisms underlying the action of ZD7288, we recorded excitatory postsynaptic potentials in perforant path-CA3 synapses in male Sprague-Dawley rats. We measured glutamate content in the hippocampus and in cultured hippocampal neurons using high performance liquid chromatography, and determined intracellular Ca(2+) concentration [Ca(2+)]i) using Fura-2...
May 2016: Neural Regeneration Research
Shun-Fan Wu, Xi-Chao Mu, Yao-Xue Dong, Li-Xiang Wang, Qi Wei, Cong-Fen Gao
BACKGROUND: Glutamate-gated chloride channels (GluCl) mediate fast inhibitory neurotransmission in invertebrate nervous systems. Although only one GluCls gene was presented in insects, it showed diverse alternative splicing that was speculated could impact on channel function and pharmacology. RESULTS: In this study, we isolated GluCl cDNAs from adult of the small brown planthopper (SBPH, Laodelphax striatellus) and showed that six L. striatellus GluCls variants (LsGluCl-AS, LsGluCl-BS, LsGluCl-CS, LsGluCl-AL, LsGluCl-BL and LsGluCl-CL) were present in the SBPH...
June 15, 2016: Pest Management Science
Shan-Wen Liu, Yuan Li, Li-Li Zou, Yu-Tao Guan, Shuang Peng, Li-Xin Zheng, Shun-Mei Deng, Lin-Yan Zhu, Li-Wei Wang, Li-Xin Chen
Human spermatozoa encounter an osmotic decrease from 330 to 290 mOsm l-1 when passing through the female reproductive tract. We aimed to evaluate the role of chloride channels in volume regulation and sperm motility from patients with asthenozoospermia. Spermatozoa were purified using Percoll density gradients. Sperm volume was measured as the forward scatter signal using flow cytometry. Sperm motility was analyzed using computer-aided sperm analysis (CASA). When transferred from an isotonic solution (330 mOsm l-1 ) to a hypotonic solution (290 mOsm l-1 ), cell volume was not changed in spermatozoa from normozoospermic men; but increased in those from asthenozoospermic samples...
June 3, 2016: Asian Journal of Andrology
Chiara Sabbadin, Decio Armanini
Pseudohyperaldosteronism is characterized by a clinical picture of hyperaldosteronism with suppression of renin and aldosterone. It can be due to endogenous or exogenous substances that mimic the effector mechanisms of aldosterone, leading not only to alterations of electrolytes and hypertension, but also to an increased inflammatory reaction in several tissues. Enzymatic defects of adrenal steroidogenesis (deficiency of 17α-hydroxylase and 11β-hydroxylase), mutations of mineralocorticoid receptor (MR) and alterations of expression or saturation of 11-hydroxysteroid dehydrogenase type 2 (apparent mineralocorticoid excess syndrome, Cushing's syndrome, excessive intake of licorice, grapefruits or carbenoxolone) are the main causes of pseudohyperaldosteronism...
September 2016: High Blood Pressure & Cardiovascular Prevention: the Official Journal of the Italian Society of Hypertension
Paola Imbrici, Antonella Liantonio, Giulia M Camerino, Michela De Bellis, Claudia Camerino, Antonietta Mele, Arcangela Giustino, Sabata Pierno, Annamaria De Luca, Domenico Tricarico, Jean-Francois Desaphy, Diana Conte
In the human genome more than 400 genes encode ion channels, which are transmembrane proteins mediating ion fluxes across membranes. Being expressed in all cell types, they are involved in almost all physiological processes, including sense perception, neurotransmission, muscle contraction, secretion, immune response, cell proliferation, and differentiation. Due to the widespread tissue distribution of ion channels and their physiological functions, mutations in genes encoding ion channel subunits, or their interacting proteins, are responsible for inherited ion channelopathies...
2016: Frontiers in Pharmacology
Jianguo Li, Quanzhong Chang, Xiaoming Li, Xiawen Li, Jiantian Qiao, Tianming Gao
Cerebral ischemia induces delayed, selective neuronal death in the CA1 region of the hippocampus. The underlying molecular mechanisms remain unclear, but it is known that apoptosis is involved in this process. Chloride efflux has been implicated in the progression of apoptosis in various cell types. Using both the inside-out and whole-cell configurations of the patch-clamp technique, the present study characterized an outwardly rectifying chloride channel (ORCC) in acutely dissociated pyramid neurons in the hippocampus of adult rats...
August 1, 2016: Brain Research
Lei Zhao, L I Li, Ke-Tao Ma, Yang Wang, Jing Li, Wen-Yan Shi, H E Zhu, Zhong-Shuang Zhang, Jun-Qiang Si
The ability of non-steroidal anti-inflammatory drugs (NSAIDs) to modulate γ-aminobutyrate (GABA)-activated currents via Ca(2+)-activated Cl(-) channels in rat dorsal root ganglion neurons (DRG), was examined in the present study. During the preparation of DRG neurons harvested from Sprague-Dawley rats, the whole-cell recording technique was used to record the effect of NSAIDs on GABA-activated inward currents, and the expression levels of the TMEM16A and TMEM16B subunits were revealed. In the event that DRG neurons were pre-incubated for 20 sec with niflumic acid (NFA) and 5-nitro-2-(3-phenylpropylamino) benzoic acid (NPPB) prior to the administration of GABA, the GABA-induced inward currents were diminished markedly in the majority of neurons examined (96...
May 2016: Experimental and Therapeutic Medicine
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