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Calcium Antagonist

Amanda Sánchez-Recillas, Laura Rivero-Medina, Rolffy Ortiz-Andrade, Jesus Alfredo Araujo-León, J Salvador Flores-Guido
ETHNOPHARMACOLOGICAL RELEVANCE: The fight against chronic respiratory diseases needs the exploration of new active compounds with properties that contribute to diminish the symptoms or resolve the disease alongside current therapy. MATERIALS AND METHODS: Eight extracts obtained from the bark and leaves of a Mayan medicinal plant used to treat asthma, Cordia dodecandra A. DC., were investigated for their relaxant effect on rat isolated tracheal rings pre-contracted with carbachol [1µM]...
October 17, 2018: Journal of Ethnopharmacology
Seiji Wada, Baoguo Shen, Emi Kawano-Yamashita, Takashi Nagata, Masahiko Hibi, Satoshi Tamotsu, Mitsumasa Koyanagi, Akihisa Terakita
Lower vertebrate pineal organs discriminate UV and visible light. Such color discrimination is typically considered to arise from antagonism between two or more spectrally distinct opsins, as, e.g., human cone-based color vision relies on antagonistic relationships between signals produced by red-, green-, and blue-cone opsins. Photosensitive pineal organs contain a bistable opsin (parapinopsin) that forms a signaling-active photoproduct upon UV exposure that may itself be returned to the signaling-inactive "dark" state by longer-wavelength light...
October 15, 2018: Proceedings of the National Academy of Sciences of the United States of America
Keita Sonoda, Teppei Matsui, Haruhiko Bito, Kenichi Ohki
Astrocytes are known to contact with a great number of synapses and may integrate sensory inputs. In the ferret primary visual cortex, astrocytes respond to a visual stimulus with a delay of several seconds with respect to the surrounding neurons. However, in the mouse visual cortex, it remains unclear whether astrocytes respond to visual stimulations. In this study, using dual-color simultaneous in vivo two-photon calcium imaging of neurons and astrocytes in the awake mouse visual cortex, we examined the visual response of astrocytes and their precise response timing relative to the surrounding neurons...
October 12, 2018: Biochemical and Biophysical Research Communications
Jorge De La Chapa, Prajjal Kanti Singha, Mckay Sallaway, Kristen Self, Ranna Nasreldin, Ramesh Dasari, Matthew Hart, Alexander Kornienko, Jeremy Just, Jason A Smith, Alex C Bissember, Cara B Gonzales
Polygodial, a drimane sesquiterpenoid dialdehyde isolated as a pungent component of the water pepper Persicaria hydropiper, exhibits antifeedant, antimicrobial, anti-inflammatory and anticancer effects. Polygodial also activates transient receptor potential vanilloid subtype 1 (TRPV1) channels. Previously, we described the synthesis of a C12-Wittig derivative of polygodial, termed P3, with significant antiproliferative effects against multiple cancer types including oral squamous cell carcinoma (OSCC). In the present study, a more potent derivative, P27, with superior anti-proliferative effects in vitro and antitumor effects in Cal-27 derived xenografts is described...
October 5, 2018: International Journal of Oncology
Piotr Sirko, Jonathan E Gale, Jonathan F Ashmore
Intercellular Ca2+ waves are increases in cytoplasmic Ca2+ levels that propagate between cells Periodic Ca2+ waves have been linked to gene regulation and are thought to play a crucial role in the development of our hearing epithelium the organ of Corti and the acquisition of hearing We have observed regular periodic intercellular Ca2+ waves in supporting cells of an ex vivo preparation of the adult mouse organ of Corti, the waves were found to propagate independently of extracellular ATP and were inhibited by the gap junction blockers 1-octanol and carbenoxolone...
October 15, 2018: Journal of Physiology
Shujue Li, Yu Lan, Wenzheng Wu, Xiaolu Duan, Zhenzhen Kong, Wenqi Wu, Guohua Zeng
The differentiated phenotype of renal tubular epithelial cell exerts significant effect on crystal adherence. Peroxisome proliferator-activated receptor γ (PPARγ) has been shown to be critical for the regulation of cell transdifferentiation in many physiological and pathological conditions; however, little is known about its role in kidney stone formation. In the current study, we found that temporarily high oxalate concentration significantly decreased PPARγ expression, induced Madin Darby Canine Kidney cell dedifferentiation, and prompted subsequent calcium oxalate (CaOx) crystal adhesion in vitro...
October 14, 2018: Journal of Cellular Physiology
Luna Ge, Yazhou Cui, Kai Cheng, Jinxiang Han
Isopsoralen (IPRN), one of the main effective ingredients in Psoralea corylifolia Linn, has a variety of biological effects, including antiosteoporotic effects. In vivo studies show that IPRN can increase bone strength and trabecular bone microstructure in a sex hormone deficiency-induced osteoporosis model. However, the mechanism underlying this osteogenic potential has not been investigated in detail. In the present study, we investigated the molecular mechanism of IPRN-induced osteogenesis in MC3T3-E1 cells...
October 11, 2018: Molecules: a Journal of Synthetic Chemistry and Natural Product Chemistry
Chun-Yu Chen, Yung-Fong Tsai, Wei-Ju Huang, Shih-Hsin Chang, Tsong-Long Hwang
Critically ill patients have a high risk of sepsis. Various studies have demonstrated that propofol has anti-inflammatory effects that may benefit critically ill patients who require anesthesia. However, the mechanism and therapeutic effect remain incompletely understood. Our previous data suggest that propofol can act as a formyl peptide receptor 1 (FPR1) antagonist. Here, we hypothesize that propofol mitigates sepsis-induced acute lung injury (ALI) by inhibiting mitochondria-derived N-formyl peptide-mediated neutrophil activation...
October 10, 2018: Free Radical Biology & Medicine
Jeanette E Villanueva, Ling Gao, Hong C Chew, Mark Hicks, Aoife Doyle, Min Ru Qui, Kumud K Dhital, Peter S Macdonald, Andrew Jabbour
The ryanodine receptor antagonist dantrolene inhibits calcium release from the sarcoplasmic reticulum and reduces cardiac ischaemia-reperfusion injury (IRI) in global warm ischaemia models however the cardioprotective potential of dantrolene under hypothermic conditions is unknown. This study addresses whether the addition of dantrolene during cardioplegia and hypothermic storage of the donor heart can improve functional recovery and reduce IRI. Using an ex vivo isolated working heart model, Wistar rat (3 month and 12 month) hearts were perfused to acquire baseline haemodynamic measurements of aortic flow, coronary flow, cardiac output, pulse pressure and heart rate...
2018: PloS One
Sarah Kim, Yun Kyung Hahn, Elizabeth M Podhaizer, Virginia D McLane, Shiping Zou, Kurt F Hauser, Pamela E Knapp
BACKGROUND: The collective cognitive and motor deficits known as HIV-associated neurocognitive disorders (HAND) remain high even among HIV+ individuals whose antiretroviral therapy is optimized. HAND is worsened in the context of opiate abuse. The mechanism of exacerbation remains unclear but likely involves chronic immune activation of glial cells resulting from persistent, low-level exposure to the virus and viral proteins. We tested whether signaling through C-C chemokine receptor type 5 (CCR5) contributes to neurotoxic interactions between HIV-1 transactivator of transcription (Tat) and opiates and explored potential mechanisms...
October 10, 2018: Journal of Neuroinflammation
Megumi Taketo
The hippocampal marginal zone contains Cajal-Retzius (C-R) cells and participates in the regulation of cortical development. Two subtypes of group I metabotropic glutamate receptors (mGluRs), mGluR1 and mGluR5, are found in the central nervous system and are considered to regulate neuronal excitability. The release of Ca2+ from intracellular stores is thought to be a main consequence of activation of these receptor subtypes. In hippocampal C-R cells, the expression of mGluR1 has been showed using immunohistochemical techniques but its function has not been elucidated...
October 10, 2018: European Journal of Neuroscience
Oleg Palygin, Bradley S Miller, Yoshinori Nishijima, David X Zhang, Alexander Staruschenko, Andrey Sorokin
Adaptor protein p66Shc is overexpressed in smooth muscle cells of renal resistance vessels of hypertensive salt-sensitive rats and is involved in the regulation of renal vascular tone. We applied 2-photon laser scanning fluorescence microscopy to analyze spontaneous dynamic fluctuations in intracellular calcium concentrations ([Ca2+ ]i ) in smooth muscle cells embedded in the walls of freshly isolated renal resistance arteries. The amplitude, number of events, and frequency of spontaneous [Ca2+ ]i oscillations triggered by endogenously released endothelin-1 were recorded in smooth muscle cells of the renal arteries...
October 10, 2018: FASEB Journal: Official Publication of the Federation of American Societies for Experimental Biology
Lu Wang, Lijun Xie, Sufeng Zhou, Yuanyuan Wang, Juan Chen, Yanli Zhou, Yun Liu, Hongwen Zhang, Mingxue Tao, Ning Ou, Feng Shao
Tylerdipine hydrochloride is a novel L-type and T-type dual calcium channel antagonist that has the potential effects of expanding blood vessels and lowering blood pressure. It is expected to reduce the side effect of ankle edema observed with other drugs in the same class. A randomized, open-label, crossover phase 1 study was performed to evaluate the effect of food on the bioavailability of tylerdipine. Fourteen healthy male volunteers were enrolled. The administration of tylerdipine after a high-fat meal increased the bioavailability of tylerdipine...
October 10, 2018: Clinical Pharmacology in Drug Development
Lin Yan, Qincai Tang, Xiaojing Quan, Haixia Ren, Wei Chen, Hong Xia, Hesheng Luo
BACKGROUND: Glucagon-like peptide-1 (GLP-1) receptor (GLP-1R) agonists modulate gastrointestinal motility; however, the effects of GLP-1R agonists on colonic motility are still controversial, and the molecular mechanism is unclear. Exendin-4 shares 53% homology with GLP-1 and is a full agonist of GLP-1R. In this study, our aims were to explore the role and mechanism of exendin-4 in isolated rat colonic tissues and cells. METHODS: An organ bath system was used to examine the spontaneous contractions of smooth muscle strips...
October 10, 2018: Neurogastroenterology and Motility: the Official Journal of the European Gastrointestinal Motility Society
Acharaporn Duangjai, Bey-Hing Goh, Learn-Han Lee, Surasak Saokaew
Azadirachta indica A. Juss var. siamensis Valeton or commonly known as Siamese neem is one of the most well-known plant in traditional Ayurvedic medicine. The aim of the present study was to investigate the relaxant effects of A. indica on isolated rat ileum contractions and its potential underlying mechanisms involved. The isometric contractions of ileum segments were investigated in organ baths for spontaneous activity and response to aqueous extract of Siamese neem flower (SNF). The spasmolytic action of the extract was also assessed on contraction induced by acetylcholine and high potassium...
October 2018: Journal of Traditional and Complementary Medicine
Qianhui Zhang, Hanping Qi, Yonggang Cao, Pilong Shi, Chao Song, Lina Ba, Yunping Chen, Jingquan Gao, Shuzhi Li, Baiyan Li, Hongli Sun
Cardiac hypertrophy is a compensatory response to mechanical stimuli and neurohormonal factors, ultimately progresses to heart failure. The proteins of some transient receptor potential (TRP) channels, Ca2+ -permeable nonselective cation channel, are highly expressed in cardiomyocytes, and associated with the occurrence of cardiac hypertrophy. Transient receptor potential vanilloid 3 (TRPV3) is a member of TRP, however, the functional role of TRPV3 in cardiac hypertrophy remains unclear. TRPV3 was elevated in pathological cardiac hypertrophy, but not in swimming exercise-induced physiological cardiac hypertrophy in rats...
October 9, 2018: Journal of Cellular and Molecular Medicine
Andrew J Brown, Irene Castellano-Pellicena, Carl P Haslam, Paula L Nichols, Simon J Dowell
BACKGROUND/AIMS: CID16020046 blocks the effect of the lipid lysophosphatidylinositol (LPI) at its receptor, GPR55. CID16020046 and another antagonist, ML193, have been used to investigate GPR55-mediated effects of LPI on cells, tissues, and in vivo. Here we describe the structure-activity relationship of CID16020046. METHODS: Yeast or human cells were engineered to express GPR55 or control receptors. Cells were pretreated with a test agent before agonist challenge...
October 8, 2018: Pharmacology
Jennifer A Honeycutt, James J Chrobak
A marked decrease in parvalbumin (PV), a calcium-binding protein specific to a subset of GABAergic neurons, is a consistent finding in postmortem schizophrenic brain tissue. This reduction is selective to PV and is regionally specific, occurring primarily in the prefrontal cortex and hippocampus (HPC) of patients. Rodent models of NMDA receptor hypofunction utilizing NMDA antagonist treatments - e.g. ketamine (KET) - show schizophrenia-like cognitive and behavioral impairments with parallel changes in PV. While decreased PV is considered a hallmark of neuropathology in schizophrenia, previous work elucidating the effects of KET administration on PV are contradictory, with findings suggesting decreased, increased, or no change in PV expression...
October 6, 2018: Neuroscience
Saori Ohtani, Satoshi Fujita, Koki Hasegawa, Hiromasa Tsuda, Morio Tonogi, Masayuki Kobayashi
Neural responses to a ligand vary widely between neurons; however, the mechanisms underlying this variation remain unclear. One possible mechanism is a variation in the number of receptors expressed in each neural membrane. Here, we synthesized a rhodamine-labeled orexin A compound, enabling us to quantify the amount of orexin binding to its receptors, OX1 and OX2 , which principally couple to the Gq/11 protein. The rhodamine intensity and calcium response were measured under tetrodotoxin application from insular cortical glutamatergic neurons in Thy1-GCaMP6s transgenic mice using an in vivo two-photon microscope...
September 22, 2018: Journal of Pharmacological Sciences
Erin J Kodis, Sophie Choi, Eric Swanson, Gonzalo Ferreira, George S Bloom
INTRODUCTION: Alzheimer's disease (AD) symptoms reflect synaptic dysfunction and neuron death. Amyloid-β oligomers (AβOs) induce excess calcium entry into neurons via N-methyl-D-aspartate receptors (NMDARs), contributing to synaptic dysfunction. The study described here tested the hypothesis that AβO-stimulated calcium entry also drives neuronal cell cycle reentry (CCR), a prelude to neuron death in AD. METHODS: Pharmacologic modulators of calcium entry and gene expression knockdown were used in cultured neurons and AD model mice...
October 2018: Alzheimer's & Dementia: the Journal of the Alzheimer's Association
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