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British Journal of Pharmacology

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https://www.readbyqxmd.com/read/28635081/understanding-and-improving-photo-control-of-ion-channels-in-nociceptors-with-azobenzene-photoswitches
#1
Alexandre Mourot, Christian Herold, Michael A Kienzler, Richard H Kramer
BACKGROUND AND PURPOSE: We previously developed a photoisomerizable local anaesthetic, named QAQ, to gain rapid, optical control over pain signaling without involving genetic modification. In darkness or in green light, trans-QAQ blocks voltage-gated K(+) and Na(+) channels and silences action potentials in pain-sensing neurons. Upon photoisomerization to cis with near UV light, QAQ blockade is rapidly relieved and neuronal activity is restored. However, the molecular mechanism of cis and trans QAQ blockade is not known...
June 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28635080/neuroadaptations-of-presynaptic-and-postsynaptic-gabab-receptor-function-in-the-paraventricular-nucleus-in-response-to-chronic-unpredictable-stress
#2
Yonggang Gao, Jing-Jing Zhou, Yun Zhu, Li Wang, Therese A Kosten, Xiangjian Zhang, De-Pei Li
BACKGROUND: Chronic stress induces an impaired GABAA (γ-aminobutyric acid type A) receptor-mediated inhibition in the hypothalamic paraventricular nucleus (PVN). It is not clear whether GABAB receptor function is altered in chronic stress. We hypothesize that chronic stress alters GABAB receptor function in PVN corticotrophin-releasing hormone (CRH) neurons to control hypothalamus-pituitary-adrenal (HPA) axis activity. EXPERIMENTAL APPROACH: Whole cell patch-clamp recording was performed on PVN-CRH neurons expressing eGFP driven by CRH promoter in brain slices from unstressed rats and rats that had been subjected to chronic unpredictable mild stress (CUMS)...
June 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28631302/l-hcy-induced-cathepsin-v-mediates-the-vascular-endothelial-inflammation-in-hyperhomocysteinemia
#3
Yi-Ping Leng, Ye-Shuo Ma, Xiao-Gang Li, Rui-Fang Chen, Ping-Yu Zeng, Xiao-Hui Li, Cheng-Feng Qiu, Ya-Pei Li, Zhen Zhang, Alex F Chen
BACKGROUND AND PURPOSE: Vascular inflammation, including the expression of inflammatory cytokines in endothelial cells, plays a critical role in hyperhomocysteinemia-associated vascular diseases. Cathepsin V, specifically expressed in humans, is involved in vascular diseases through its elastolytic and collagenolytic activities. The aim of this study was to determine the effects of cathepsin V on the L-homocysteine (L-Hcy)-induced vascular inflammation. EXPERIMENTAL APPROACH: A high methionine diet-induced hyperhomocysteinemic mice model was used to assess the cathepsin V expression and vascular inflammation...
June 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28631296/hydrogen-sulphide-as-a-signaling-molecule-regulating-physiopathological-processes-in-gastrointestinal-motility
#4
REVIEW
M Jimenez, V Gil, M Martinez-Cutillas, N Mañé, D Gallego
The biology of H2 S is an emerging area of research since several biological functions have been recently attributed to this gaseous molecule in a vast number of regions including the cardiovascular, urogenital, respiratory, digestive and central nervous system. H2 S exerts anti-inflammatory effects and can be considered an endogenous mediator with potential effects on gastrointestinal motility. During the last years, our research group has investigated the role of H2 S as a regulator of gastrointestinal motility using both animal and human tissues...
June 20, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28627773/oleanolic-acid-derivative-dks26-exerts-antidiabetic-and-hepatoprotective-effects-in-diabetic-mice-and-promotes-glp-1-secretion-and-expression-in-intestinal-cells
#5
Fei-Fei Chen, Jian-Ta Wang, Li-Xia Zhang, Shu-Fang Xing, Yun-Xia Wang, Kai Wang, Shu-Li Deng, Ji-Quan Zhang, Lei Tang, Hao-Shu Wu
BACKGROUND AND PURPOSE: Glucagon-like peptide-1 (GLP-1) is an important target for diabetes therapy based on its key role in maintaining glucose and lipid homeostasis. This study was designed to investigate antidiabetic and hepatoprotective effects of novel oleanolic acid derivative DKS26 in diabetic mice and elucidate its underlying GLP-1 related antidiabetic mechanisms in vitro and in vivo. EXPERIMENTAL APPROACH: The therapeutic effects of DKS26 were inspected in streptozotocin (STZ)-induced and db/db diabetic mouse models including levels of plasma glucose, glycosylated serum protein (GSP), lipid profiles, insulin, alanine aminotransferase (ALT) and aspartate aminotransferase (AST), oral glucose tolerance (OGT), pancreatic islets and hepatic histopathological morphology, liver lipid levels and expression of pro-inflammation cytokines...
June 19, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28626937/glutamatergic-regulation-of-cognition-and-functional-brain-connectivity-insights-from-pharmacological-genetic-and-translational-schizophrenia-research
#6
REVIEW
Maria R Dauvermann, Graham Lee, Neil Dawson
The pharmacological modulation of glutamatergic neurotransmission to improve cognitive function has been a focus of intensive research, particularly in relation to the cognitive deficits seen in schizophrenia. Despite this effort there has been little success in the clinical use of glutamatergic compounds as procognitive drugs. Here we review a selection of the drugs used to modulate glutamatergic signalling and how they impact on cognitive function in rodents and humans. We highlight how glutamatergic dysfunction, and NMDA receptor hypofunction in particular, is a key mechanism contributing to the cognitive deficits observed in schizophrenia, and outline some of the glutamatergic targets that have been tested as putative procognitive targets for the disorder...
June 18, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28622417/the-antimigraine-butterbur-ingredient-isopetasin-desensitises-peptidergic-nociceptors-via-the-transient-receptor-potential-ankyrin-1-channel
#7
Silvia Benemei, Francesco De Logu, Simone Li Puma, Ilaria Maddalena Marone, Elisabetta Coppi, Filippo Ugolini, Wolfgang Liedtke, Pollastro Federica, Giovanni Appendino, Pierangelo Geppetti, Serena Materazzi, Romina Nassini
BACKGROUND AND PURPOSE: The mechanism of the antimigraine action of butterbur [Petasites hybridus (L.) Gaertn.] is unknown. Here, we investigated the ability of isopetasin, a major butterbur constituent, to specifically target the transient receptor ankyrin 1 (TRPA1) channel and to affect functional responses relevant to migraine. EXPERIMENTAL APPROACH: Single cell calcium imaging and patch-clamp recordings in human and rodent TRPA1-expressing cells, neurogenic motor responses in isolated rat/mouse urinary bladder, release of calcitonin gene-related peptide (CGRP) from mouse spinal cord in vitro, and facial rubbing in mice and meningeal blood flow in rat were examined...
June 16, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28622411/using-automated-patch-clamp-electrophysiology-platforms-in-pain-related-ion-channel-research-insights-from-industry-and-academia
#8
REVIEW
Damian C Bell, Mark Dallas
Automated patch clamp (APC) technology was first developed at the turn of the millennium. The increased throughput it afforded promised a new paradigm in ion channel recordings: it offered the potential to overcome the time-consuming, low-throughput bottleneck arising from manual patch clamp (MPC) investigations. This has relevance to the fast-paced development of novel therapies for chronic pain. This review highlights the advances in technology, using select examples, that have facilitated APC usage in both industry and academia...
June 16, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28616865/isoacteoside-a-dihydroxyphenylethyl-glycoside-exhibits-anti-inflammatory-effects-through-blocking-tlr4-dimerization
#9
Hongwei Gao, Yankun Cui, Naixin Kang, Xin Liu, Yanli Liu, Yue Zou, Ziyu Zhang, Xiaoran Li, Shilin Yang, Ji Li, Chunming Wang, Qiong-Ming Xu, Xiuping Chen
BACKGROUND AND PURPOSE: Isoacteoside (ISO) is a phenylethanoid isolated from Monochasma savatieri Franch. ex Maxim., which is an anti-inflammatory herb widely used in traditional Chinese medicine. However, the exact mechanism of the anti-inflammatory activity of ISO is not completely understood. In this study, its anti-inflammatory mechanism in mouse macrophages was elucidated. EXPERIMENTAL APPROACH: The expression of the NF-κB pathway, MAPK pathway, iNOS, TNF-α, IL-6 and IL-1β was evaluated using western blotting, qRT-PCR or ELISA...
June 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28616863/contrasting-effects-of-phosphatidylinositol-4-5-bisphosphate-pip2-on-cloned-tmem16a-and-tmem16b-channels
#10
Chau M Ta, Kathryn E Acheson, Nils J G Rorsman, Remco C Jongkind, Paolo Tammaro
BACKGROUND AND PURPOSE: Ca(2+) -activated Cl(-) channels (CaCCs) are gated open by a rise in intracellular Ca(2+) concentration ([Ca(2+) ]i ), typically provoked by Gq -protein coupled receptor activation (Gq PCR). Gq PCR activation initiates depletion of plasmalemmal phosphatidylinositol 4,5-bisphosphate (PIP2 ). Here we ask whether PIP2 acts as a signalling lipid for CaCCs coded by the TMEM16A and TMEM16B genes. EXPERIMENTAL APPROACH: Patch-clamp electrophysiology, in conjunction with genetically-encoded systems to control cellular PIP2 content, was used to define the mechanism of action of PIP2 on TMEM16A and TMEM16B channels...
June 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28616862/loops-d-e-and-g-in-the-drosophila-d%C3%AE-1-subunit-contribute-to-high-neonicotinoid-sensitivity-of-d%C3%AE-1-chicken-%C3%AE-2-nicotinic-acetylcholine-receptor
#11
Makoto Ihara, Mai Hikida, Hiroyuki Matsushita, Kyosuke Yamanaka, Yuya Kishimoto, Kazuki Kubo, Shun Watanabe, Mifumi Sakamoto, Koutaro Matsui, Akihiro Yamaguchi, Daiki Okuhara, Shogo Furutani, David B Sattelle, Kazuhiko Matsuda
BACKGROUND AND PURPOSE: Neonicotinoid insecticides interact with the orthosteric site formed at subunit interfaces of insect nicotinic acetylcholine receptors (insect nACh receptors). However, their interactions with the orthosteric sites at α-non α and α-α subunit interfaces remain poorly understood. The aim of this study was to elucidate the mechanism of neonicotinoid actions using the Drosophila Dα1-chicken β2 hybrid nACh receptor. EXPERIMENTAL APPROACH: Computer models of the (Dα1)3 (β2)2 nACh receptor in complex with imidacloprid and thiacloprid were generated...
June 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28613414/the-arg-phe-amide-peptide-26rfa-qrfp-and-its-receptor-iuphar-review
#12
REVIEW
Jérôme Leprince, Didier Bagnol, Ronan Bureau, Shoji Fukusumi, Riccarda Granata, Shuji Hinuma, Dan Larhammar, Stefany Primeaux, Jana Sopkova-de Oliveiras Santos, Kazuyoshi Tsutsui, Kazuyoshi Ukena, Hubert Vaudry
26RFa is an RFamide neuropeptide that was first isolated from the brain of the European green frog on the basis of a cross-reactivity with antibodies raised against bovine NPFF. 26RFa and its N-terminally extended form QRFP have been identified as cognate ligands of the former orphan receptor GPR103, now renamed QRFPR. The 26RFa/QRFP precursor has been characterized in various mammalian and non-mammalian species. In the brain of mammals, including human, 26RFa/QRFP mRNA is almost exclusively expressed in hypothalamic nuclei...
June 14, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28608595/a-novel-individual-cell-based-mathematical-model-based-on-multicellular-tumour-spheroids-for-evaluating-doxorubicin-related-delivery-in-avascular-regions
#13
Jiali Liu, Fangrong Yan, Hongzhu Chen, Wenjie Wang, Wenyue Liu, Kun Hao, Guangji Wang, Fang Zhou, Jingwei Zhang
BACKGROUND AND PURPOSE: Effective drug delivery in the avascular regions of tumours, which is crucial for the promising antitumour activity of doxorubicin-related therapy, is governed by two inseparable processes: intercellular diffusion and intracellular retention. To accurately evaluate doxorubicin-related delivery in the avascular regions, these two processes should be assessed together; however, no appropriate assessment method currently exists. EXPERIMENTAL APPROACH: An individual-cell-based mathematical model based on multicellular tumour spheroids was developed that describes the different intercellular diffusion and intracellular retention kinetics of doxorubicin in each cell layer...
June 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28608537/inhibition-of-human-n-and-t-type-calcium-channels-by-an-ortho-phenoxyanilide-derivative-moniro-1
#14
Jeffrey R McArthur, Leonid Motin, Ellen C Gleeson, Sandro Spiller, Richard J Lewis, Peter J Duggan, Kellie L Tuck, David J Adams
BACKGROUND AND PURPOSE: Voltage-gated calcium channels are involved in peripheral and central nervous system nociception. N-type (Cav 2.2) and T-type (Cav 3.1, Cav 3.2 and Cav 3.3) voltage-gated calcium channels are particularly important in studying and treating pain and epilepsy. EXPERIMENTAL APPROACH: In this study, whole-cell patch clamp electrophysiology was used to assess the potency and mechanism of action of a novel ortho-phenoxylanilide derivative, MONIRO-1, against a panel of voltage-gated calcium channels including Cav 1...
June 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28608534/recent-advances-in-the-development-of-t-type-calcium-channel-blockers-for-pain-intervention
#15
REVIEW
Terrance P Snutch, Gerald W Zamponi
Cav3.2 T-type calcium channels are important regulators of pain signals in afferent pain pathway, and their activities are dysregulated during various chronic pain states. Therefore it stands to reason that inhibiting T-type calcium channels in dorsal root ganglion neurons and in the spinal dorsal horn can be targeted for pain relief. This is supported by early pharmacological studies with T-type channel blockers such as ethosuximide, and by analgesic effects of siRNA depletion of Cav3.2 channels. In the past five years, considerable effort has been applied towards identifying novel classes of T-type calcium channel blockers...
June 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28608532/%C3%AE-opioid-receptor-dopamine-d1-receptor-heteromers-modulate-opioid-induced-locomotor-sensitization-in-a-dopamine-independent-manner
#16
Yi-Min Tao, Chuan Yu, Wei-Sheng Wang, Yuan-Yuan Hou, Xue-Jun Xu, Zhi-Qiang Chi, Yu-Qiang Ding, Yu-Jun Wang, Jing-Gen Liu
BACKGROUND AND PURPOSE: Exposure to opiates induces locomotor sensitization in rodents, which has been proposed to correspond to the compulsive drug-seeking behavior. Numerous studies have demonstrated that locomotor sensitization can occur in a dopamine transmission-independent manner, however, the underlying mechanisms are unclear. EXPERIMENTAL APPROACH: The coimmunoprecipitation, BRET and cross-antagonism assays were used to demonstrating the existence of receptor heterodimers...
June 13, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28603838/compartmentalized-camp-responses-to-prostaglandin-ep2-receptor-activation-in-human-airway-smooth-muscle-cells
#17
Shailesh R Agarwal, Kathryn Miyashiro, Htun Latt, Rennolds S Ostrom, Robert D Harvey
BACKGROUND AND PURPOSE: Previous studies indicate that prostaglandin EP2 receptors (EP2 Rs) selectively couple to adenylyl cyclase type 2 (AC2) in non-lipid raft domains of airway smooth muscle (ASM) cells, where they regulate specific cAMP-dependent responses. The goal of the present study was to identify the cellular microdomains where EP2 Rs stimulate cAMP production. EXPERIMENTAL APPROACH: FRET-based cAMP biosensors were targeted to different subcellular locations of primary human ASM cells...
June 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28602044/the-dynamic-interaction-between-pain-and-opioid-misuse
#18
REVIEW
Adrianne R Wilson-Poe, Jose A Moron
In 2014, drug overdose surpassed automobile accidents as the number one cause of accidental death for the first time in US history. The overdose epidemic is largely driven by opioids, and genuine prescription opioid analgesics play the biggest role in this phenomenon. Despite advancements in abuse deterrent formulations, prescription drug monitoring programs, and clinical assessments for the detection of abuse potential, drug overdoses continue to escalate. The CDC has recently issued new guidelines for opioid prescription, yet even these recommendations have their shortcomings...
June 11, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28600847/the-fifth-subunit-of-the-%C3%AE-4%C3%AE-2-2-%C3%AE-2-nicotinic-acetylcholine-receptor-modulates-maximal-ach-responses
#19
Karina New, Silvia Garcia Del Villar, Simone Mazzaferro, Constanza Alcaino, Isabel Bermudez
BACKGROUND AND PURPOSE: The fifth subunit in the (α4β2)2 α4 nicotinic acetylcholine receptor (nAChR) plays a determining role in the pharmacology of this nAChR type. Here, we have examined the role of the fifth subunit in the ACh responses of the (α4β2)2 β2 nAChR type. EXPERIMENTAL APPROACH: The role of the fifth subunit in receptor function was explored using two-electrode voltage-clamp electrophysiology, along with subunit-targeted mutagenesis and the substituted cysteine scanning method applied to fully linked (α4β2)2 β2 receptors...
June 10, 2017: British Journal of Pharmacology
https://www.readbyqxmd.com/read/28593738/sex-differences-in-the-regulation-of-porcine-coronary-artery-tone-by-perivascular-adipose-tissue-a-role-of-adiponectin
#20
Abdulla A Ahmad, Michael D Randal, Richard E Roberts
BACKGROUND AND PURPOSE: As there is sexual dimorphism in the regulation of vascular tone, the aim of this present study was to determine whether there are sex differences in perivascular adipose tissue (PVAT) - mediated regulation of the porcine coronary artery (PCA) tone. EXPERIMENTAL APPROACH: Isometric tension recording system was used to record changes in tone in PCAs. Western blot analysis was performed to examine the expression of adiponectin in PVAT and adiponectin receptors and adiponectin binding protein (APPL1) in PCA...
June 8, 2017: British Journal of Pharmacology
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