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Source: British Journal of Pharmacology

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Total 51 results found since Jan 2013.

Endocannabinoids modulate human blood‐brain barrier permeability in vitro
Conclusion and implicationThese data show that endocannabinoids may play an important modulatory role in normal BBB physiology, and also afford protection to the BBB during ischaemic stroke, through a number of target sites.
Source: British Journal of Pharmacology - February 5, 2015 Category: Drugs & Pharmacology Authors: William H Hind, Cristina Tufarelli, Maria Neophytou, Susan I Anderson, Timothy J England, Saoirse E O'Sullivan Tags: Research Paper Source Type: research

Inflammation in acute CNS injury: a focus on the role of substance P
Abstract Recently, a number of reports have shown that neurogenic inflammation may play a role in the secondary injury response following acute injury to the central nervous system (CNS), including traumatic brain injury (TBI) and stroke. In particular substance P (SP) release appears to be critically involved. Specifically, expression of the neuropeptide SP is increased in acute CNS injury, with the magnitude of SP release being related to both the frequency and magnitude of the insult. SP release is associated with an increase in blood‐brain barrier permeability and the development of vasogenic oedema as well as neuron...
Source: British Journal of Pharmacology - April 1, 2015 Category: Drugs & Pharmacology Authors: F Corrigan, R Vink, R J Turner Tags: Review Article – Inflammation: Maladies, Models, Mechanisms & Molecules Themed Issue Source Type: research

Endocannabinoids modulate human blood–brain barrier permeability in vitro
Conclusion and ImplicationThe endocannabinoids may play an important modulatory role in normal BBB physiology, and also afford protection to the BBB during ischaemic stroke, through a number of target sites.
Source: British Journal of Pharmacology - April 10, 2015 Category: Drugs & Pharmacology Authors: William H Hind, Cristina Tufarelli, Maria Neophytou, Susan I Anderson, Timothy J England, Saoirse E O'Sullivan Tags: RESEARCH PAPER Source Type: research

Cannabidiol protects an in vitro model of the blood brain barrier (BBB) from oxygen‐glucose deprivation via PPARγ and 5‐HT1A
CONCLUSIONS AND IMPLICATIONSThese data suggest that activity at the BBB could represent an as yet unrecognised mechanism of CBD‐induced neuroprotection in ischaemic stroke, mediated by PPARγ and 5‐HT1A. This article is protected by copyright. All rights reserved.
Source: British Journal of Pharmacology - October 1, 2015 Category: Drugs & Pharmacology Authors: William H Hind, Timothy J England, Saoirse E O'Sullivan Tags: RESEARCH PAPER Source Type: research

Cannabidiol protects an in vitro model of the blood–brain barrier from oxygen‐glucose deprivation via PPARγ and 5‐HT1A receptors
Conclusions and ImplicationsThese data suggest that preventing permeability changes at the BBB could represent an as yet unrecognized mechanism of CBD‐induced neuroprotection in ischaemic stroke, a mechanism mediated by activation of PPARγ and 5‐HT1A receptors.
Source: British Journal of Pharmacology - February 3, 2016 Category: Drugs & Pharmacology Authors: William H Hind, Timothy J England, Saoirse E O'Sullivan Tags: RESEARCH PAPER Source Type: research

Bisperoxovandium (pyridin ‐2‐squaramide) Targets Both PTEN and Erk1/2 to Confer Neuroprotection
Conclusions and ImplicationsbpV(pis) confers neuroprotection in OGD‐induced injury in vitro and in cerebral ischemia in vivo through suppressing PTEN and activating Erk1/2, respectively. Thus, bpV(pis) is a bi‐target neuroprotectant that may be developed as a drug candidate for stroke treatment.
Source: British Journal of Pharmacology - January 26, 2017 Category: Drugs & Pharmacology Authors: Zhi ‐Feng Zhang, Juan Chen, Xin Han, Ya Zhang, Hua‐Bao Liao, Rui‐Xue Lei, Yang Zhuang, Ze‐Fen Wang, Zhiqiang Li, Jin‐Cao Chen, Wei‐Jing Liao, Hai‐Bing Zhou, Fang Liu, Qi Wan Tags: RESEARCH PAPER Source Type: research

VIP and PACAP: Neuropeptide modulators of CNS inflammation, injury, and repair
Summary page Inflammatory processes play both regenerative and destructive roles in multiple sclerosis, stroke, CNS trauma, amyotrophic lateral sclerosis (ALS) and aging‐related neurodegenerative diseases such as Alzheimer's, Parkinson's, and Huntington's. Endogenous defense mechanisms against these pathologies include those that are directly neuroprotective, and those that modulate the expression of inflammatory mediators in microglia, astrocytes, and invading inflammatory cells. While a number of mechanisms and molecules have been identified that can directly promote neuronal survival, less is known about how the brain...
Source: British Journal of Pharmacology - March 20, 2013 Category: Drugs & Pharmacology Authors: J A Waschek Tags: Review Article Source Type: research

Effects of the Antianginal Drug, Ranolazine, on the Brain Sodium Channel NaV1.2 and Its Modulation By Extracellular Protons
Conclusions and ImplicationsOur work provides novel insights into the modulation of brain sodium channel, NaV1.2, by ranolazine. We demonstrate that ranolazine binds NaV1.2 in a state‐dependent manner, and that the effects of ranolazine are slowed but not abolished by protons. Our results suggest that further research performed on channels with epilepsy‐causing mutations may prove ranolazine to be an efficacious therapy.
Source: British Journal of Pharmacology - March 8, 2013 Category: Drugs & Pharmacology Authors: C H Peters, S Sokolov, S Rajamani, P C Ruben Tags: Research Paper Source Type: research

Targeting Hexokinase II to mitochondria to modulate energy metabolism and reduce ischemia‐reperfusion injury in heart
Summary Mitochondrially‐bound hexokinase II (mtHKII) has long been known to confer cancer cells with their resilience against cell death. More recently, mtHKII has emerged as a powerful protector against cardiac cell death. mtHKII protects against IR injury in skeletal muscle and heart, attenuates cardiac hypertrophy and remodelling, and is one of the major end‐effectors through which ischemic preconditioning protects against myocardial ischemia‐reperfusion injury. Mechanisms of mtHKII cardioprotection against reperfusion injury entail the maintenance of regulated OMM permeability during ischemia and reperfusion resu...
Source: British Journal of Pharmacology - August 30, 2013 Category: Drugs & Pharmacology Authors: Rianne Nederlof, Otto Eerbeek, Markus W Hollmann, Richard Southworth, Coert J Zuurbier Tags: Review Article Source Type: research

Characterization of a novel multi‐functional resveratrol derivative for the treatment of atrial fibrillation.
Conclusion and ImplicationsThese findings indicate that C1 is a promising multi‐functional small molecule that targets a number of key pathways involved in AF.
Source: British Journal of Pharmacology - September 17, 2013 Category: Drugs & Pharmacology Authors: Istvan Baczko, David Liknes, Wei Yang, Kevin C Hamming, Gavin Searle, Kristian Jaeger, Zoltan Husti, Viktor Juhasz, Gergely Klausz, Robert Pap, Laszlo Saghy, Andras Varro, Vernon Dolinsky, Shaohua Wang, Vivek Rauniyar, Dennis Hall, Jason R. Dyck, Peter E. Tags: Research Paper Source Type: research

Novel Analogues of Chlormethiazole are Neuroprotective in Four Cellular Models of Neurodegeneration by a Mechanism with Variable Dependence on GABAA Receptor Potentiation
Conclusions and ImplicationsThe results support the concept that CMZ does not contain a single pharmacophore, rather that broad‐spectrum neuroprotection results from a GABAA‐dependent mechanism represented by GN‐28, combined with a mechanism represented in GN‐38 that shows the least dependence on GABAA receptors. These findings allow further refinement of the neuroprotective pharmacophore and investigation into secondary mechanisms that will assist in identifying methiazole‐based compounds of use in treating neurodegeneration.
Source: British Journal of Pharmacology - October 10, 2013 Category: Drugs & Pharmacology Authors: Lawren VandeVrede, Ehsan Tavassoli, Jia Luo, Zhihui Qin, Lan Yue, David R. Pepperberg, Gregory R. Thatcher Tags: Research Paper Source Type: research

Mitochondrial metals as a potential therapeutic target in neurodegeneration
Summary Transition metals are critical for enzyme function and protein folding, but in excess can mediate neurotoxic oxidative processes. As mitochondria are particularly vulnerable to oxidative damage due to radicals generated during ATP production, mitochondrial biometal homeostasis must therefore be tightly controlled to safely harness the redox potential of metal enzyme cofactors. Dysregulation of metal functions is evident in numerous neurological disorders including Alzheimer's disease, stroke, Parkinson's disease, Huntington's disease, amyotrophic lateral sclerosis and Friedrich's Ataxia. This review describes the m...
Source: British Journal of Pharmacology - November 11, 2013 Category: Drugs & Pharmacology Authors: A Grubman, A R White, J R Liddell Tags: Review Article – Mitochondrial Pharmacology: Energy, Injury & Beyond Themed Issue Source Type: research

Therapeutic Potential of Midkine in Cardiovascular Diseases
Abstract Ischemic heart disease, stroke and their pathological consequences are life‐threatening diseases that account for about half of deaths in developed countries. Pathology of these diseases includes cell death due to ischemia/reperfusion injury, vascular stenosis, and cardiac remodeling. The growth factor midkine plays a pivotal role in these events. Midkine shows an acute cytoprotective effect in ischemia/reperfusion injury at least in part via its anti‐apoptotic effect. Moreover, while midkine promotes endothelial cell proliferation, it also recruits inflammatory cells to lesions. These activities eventually en...
Source: British Journal of Pharmacology - November 28, 2013 Category: Drugs & Pharmacology Authors: Kenji Kadomatsu, Péter Bencsik, Anikó Görbe, Csaba Csonka, Kazuma Sakamoto, Satoshi Kishida, Péter Ferdinandy Tags: Review Article – Midkine Themed Issue Source Type: research

Characterization of a novel multifunctional resveratrol derivative for the treatment of atrial fibrillation
Conclusion and ImplicationsC1 behaved as a promising multifunctional small molecule targeting a number of key pathways involved in AF.
Source: British Journal of Pharmacology - December 10, 2013 Category: Drugs & Pharmacology Authors: Istvan Baczko, David Liknes, Wei Yang, Kevin C Hamming, Gavin Searle, Kristian Jaeger, Zoltan Husti, Viktor Juhasz, Gergely Klausz, Robert Pap, Laszlo Saghy, Andras Varro, Vernon Dolinsky, Shaohua Wang, Vivek Rauniyar, Dennis Hall, Jason RB Dyck, Peter E Tags: RESEARCH PAPER Source Type: research

The TRPM4 channel inhibitor 9‐phenanthrol
Abstract The phenanthrene‐derivative 9‐phenanthrol is a recently identified inhibitor of the TRPM4 Ca2+‐activated non‐selective cation channel whose mechanism of action remains to be determined. Subsequent studies performed on other ion channels confirm the specificity of the drug for TRPM4. In addition, 9‐phenanthrol modulates a variety of physiological processes through TRPM4 current inhibition and thus exerts beneficial effects in several pathological conditions. 9‐phenanthrol modulates smooth muscle contraction in bladder and cerebral arteries, impacts spontaneous activity in neurons and heart, and reduces ...
Source: British Journal of Pharmacology - January 16, 2014 Category: Drugs & Pharmacology Authors: R Guinamard, T Hof, C A Del Negro Tags: Review Article Source Type: research