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Showing 1-30 of 108 results for "A1289" within Papers
Kumiko Nakamura et al.
European journal of pharmacology, 694(1-3), 98-103 (2012-09-12)
We previously reported that two types of K(+) channels, the BK type Ca(2+)-activated K(+) channel coupled with phospholipase C (PLC) and the voltage-dependent K(+) channel (Kv channel), are, respectively, involved in the prostanoid TP receptor- and muscarinic M(2) receptor-mediated inhibition
SĆ©bastien Dilly et al.
Biochemical pharmacology, 85(4), 560-569 (2012-12-29)
Valine residues in the pore region of SK2 (V366) and SK3 (V520) were replaced by either an alanine or a phenylalanine to evaluate the impact on the interactions with the allosteric blocker apamin. Unlike TEA which showed high sensitivity to
Audrey E Padula et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 40(8), 1928-1939 (2015-02-11)
Small-conductance Ca(2+)-activated K(+) (KCa2) channels control neuronal excitability and synaptic plasticity, and have been implicated in substance abuse. However, it is unknown if genes that encode KCa2 channels (KCNN1-3) influence alcohol and drug addiction. In the present study, an integrative
Paul F Kramer et al.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology, 40(10), 2418-2424 (2015-04-02)
Midbrain dopamine neurons are important mediators of reward and movement and are sensitive to cocaine-induced plasticity. After even a single injection of cocaine, there is an increase in AMPA-dependent synaptic transmission. The present study examines cocaine-induced plasticity of mGluR-dependent currents
P S Wong et al.
Pharmacological research, 90, 25-35 (2014-09-27)
Hydrogen peroxide (H2O2) has been proposed to act as a factor for endothelium-derived hyperpolarization (EDH) and EDH may act as a 'back up' system to compensate the loss of the NO pathway. Here, the mechanism of action of H2O2 in
Serge A Y Afeli et al.
American journal of physiology. Renal physiology, 303(4), F559-F568 (2012-05-18)
Animal studies suggest that the small (SK) and intermediate (IK) conductance Ca(2+)-activated K(+) channels may contribute to detrusor smooth muscle (DSM) excitability and contractility. However, the ability of SK and IK channels to control DSM spontaneous phasic and nerve-evoked contractions
Morgana Moretti et al.
European journal of pharmacology, 687(1-3), 21-27 (2012-05-12)
Considering that the administration of ascorbic acid elicits an antidepressant-effect in mice by a mechanism which involves an interaction with N-methyl-D-aspartate receptors and the l-arginine-nitric oxide-cGMP pathway and taking into account that the stimulation of this pathway is associated with
Kazuhiro Nishiyama et al.
Pharmacology, 94(5-6), 230-238 (2014-11-28)
Na(+)/Ca(2+) exchanger 1 (NCX1) is a plasma membrane transporter involved in regulating intracellular Ca(2+) concentrations. NCX1 is critical for Ca(2+) regulation in cardiac muscle, vascular smooth muscle and nerve fibers. However, little is known about the physiological role of NCX1
Arij Daou et al.
Nature communications, 11(1), 952-952 (2020-02-23)
Neurons regulate their intrinsic physiological properties, which could influence network properties and contribute to behavioral plasticity. Recording from adult zebra finch brain slices we show that within each bird basal gangliaĀ Area X-projecting (HVCX) neurons share similar spike waveform morphology and
Gen Ohtsuki et al.
Neuron, 75(1), 108-120 (2012-07-17)
Small-conductance Ca(2+)-activated K(+) channels (SK channels) modulate excitability and curtail excitatory postsynaptic potentials (EPSPs) in neuronal dendrites. Here, we demonstrate long-lasting plasticity of intrinsic excitability (IE) in dendrites that results from changes in the gain of this regulatory mechanism. Using
Apamin, a centrally acting neurotoxic peptide: binding and actions.
E Habermann et al.
Advances in cytopharmacology, 3, 387-394 (1979-01-01)
Clint Gray et al.
PloS one, 8(1), e53505-e53505 (2013-01-12)
Maternal undernutrition results in elevated blood pressure (BP) and endothelial dysfunction in adult offspring. However, few studies have investigated interventions during early life to ameliorate the programming of hypertension and vascular disorders. We have utilised a model of maternal undernutrition
Apamin modulates electrophysiological characteristics of the pulmonary vein and the Sinoatrial Node.
Wei-Ta Chen et al.
European journal of clinical investigation, 43(9), 957-963 (2013-07-10)
Small-conductance calcium-activated potassium (SK) channels play an important role in atrial electrophysiology. Blocking SK channels prolongs action potential (AP) duration and attenuate electrical remodelling. The effects of SK blocking on the pulmonary vein (PV) and the sinoatrial node (SAN) remain
David H F Vandael et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 32(46), 16345-16359 (2012-11-16)
Mouse chromaffin cells (MCCs) fire spontaneous action potentials (APs) at rest. Ca(v)1.3 L-type calcium channels sustain the pacemaker current, and their loss results in depolarized resting potentials (V(rest)), spike broadening, and remarkable switches into depolarization block after BayK 8644 application.
Kathryn L Turner et al.
Cerebral cortex (New York, N.Y. : 1991), 24(9), 2388-2400 (2013-04-16)
From the subventricular zone (SVZ), neuronal precursor cells (NPCs), called neuroblasts, migrate through the rostral migratory stream (RMS) to become interneurons in the olfactory bulb (OB). Ion channels regulate neuronal migration during development, yet their role in migration through the
Rupal P Soder et al.
American journal of physiology. Regulatory, integrative and comparative physiology, 304(2), R155-R163 (2012-11-24)
Overactive bladder (OAB) is often associated with increased involuntary detrusor smooth muscle (DSM) contractions during the bladder-filling phase. To develop novel therapies for OAB, it is critical to better understand the mechanisms that control DSM excitability and contractility. Recent studies
Serge Simonet et al.
British journal of pharmacology, 167(4), 854-867 (2012-06-01)
The purpose of the study was to investigate renal endothelium-dependent vasodilatation in a model of severe hypertension associated with kidney injury. Changes in perfusion pressure were measured in isolated, perfused kidneys taken from 18-week-old Wistar-Kyoto rat (WKY), spontaneously hypertensive rats
JosƩ M La Fuente et al.
European journal of pharmacology, 735, 68-76 (2014-04-22)
We have analysed the effects of large-conductance calcium-activated potassium channel (BK) stimulation on neurogenic and myogenic contraction of human bladder from healthy subjects and patients with urinary symptoms and evaluated the efficacy of activating BK to relief bladder hyperactivity in
Ramesh C Mishra et al.
Cardiovascular research, 97(2), 339-348 (2012-11-03)
Endothelial SK(Ca) and IK(Ca) channels play an important role in the regulation of vascular function and systemic blood pressure. Based on our previous findings that small molecule activators of SK(Ca) and IK(Ca) channels (i.e. NS309 and SKA-31) can inhibit myogenic
Viola Mazzoleni et al.
FASEB journal : official publication of the Federation of American Societies for Experimental Biology, 35(2), e21167-e21167 (2020-11-27)
Panton-Valentine Leukocidin (PVL) is a bicomponent leukotoxin produced by 3%-10% of clinical Staphylococcus aureus (SA) strains involved in the severity of hospital and community-acquired infections. Although PVL was long known as a pore-forming toxin, recent studies have challenged the formation
Amaury Graulich et al.
Journal of medicinal chemistry, 48(15), 4972-4982 (2005-07-22)
The synthesis and the (125)I-apamin binding studies of original C-5- and C-8-substituted 1-(3,4-dimethoxy-benzyl)-2,2-dimethyl-1,2,3,4-tetrahydroisoquinoliniums and 1-(3,4-dimethoxy-benzyl)-6,6-dimethyl-4,5,6,7-tetrahydrothieno[2,3-c]pyridiniums were performed in order to find a reversible and selective SK channel blocker structurally related to N-methyl-laudanosine and N-methyl-noscapine. A bulky alkyl substituent in the
Y M Al Suleimani et al.
European journal of pharmacology, 765, 107-114 (2015-08-25)
Atypical cannabinoid O-1602 (5-Methyl-4-[(1R,6R)-3-methyl-6-(1-cyclohexen-1-yl]-1,3-benzenediol) induces vasorelaxation and activates the orphan G protein-coupled receptor GPR55 in human endothelial cells. This study investigates the underlying mechanisms of vasorelaxation induced by this compound. The vasodilator activity was assessed in the rat third order
Haeyeong Lee et al.
The Journal of physiology, 591(2), 503-513 (2012-11-14)
We sought to characterize molecular expression and ionic conductances in a novel population of interstitial cells (PDGFRĪ±(+) cells) in murine bladder to determine how these cells might participate in regulation of detrusor excitability. PDGFRĪ±(+) cells and smooth muscle cells (SMCs)
M Lazdunski et al.
Biochemical Society symposium, 50, 31-42 (1985-01-01)
Apamin is a bee venom neurotoxin of 10 amino acids containing two disulphide bridges. Current-clamp and voltage-clamp experiments have shown that apamin externally applied blocks specifically at low concentration (0.1 microM) the Ca2+-dependent slow K+ conductance which mediates the long-lasting
Apamin from bee venom. Effects of the neurotoxin on subcellular particles of neural cultures
Spoerri E, et al.
Febs Letters, 53(2), 143-147 (1975)
Angy J Kallarackal et al.
Behavioural brain research, 237, 71-75 (2012-09-18)
Neurofibromatosis 1 (NF1) is a common genetic disorder known to cause a variety of physiological symptoms such as the formation of both benign and malignant tumors, and is also known to cause visuospatial learning deficits. Mouse models of NF1 show
Christian Schach et al.
American journal of physiology. Heart and circulatory physiology, 307(8), H1093-H1102 (2014-08-17)
Impaired endothelial function, which is dysregulated in diabetes, also precedes hypertension. We hypothesized that in Type 2 diabetes, the impaired endothelium-dependent relaxation is due to a loss of endothelium-derived hyperpolarization (EDH) that is regulated by impaired ion channel function. Zucker
Bart Pauwels et al.
The journal of sexual medicine, 11(7), 1664-1674 (2014-05-21)
Erectile dysfunction (ED), as well as many cardiovascular diseases, is associated with impaired nitric oxide (NO) bioavailability. Recently, oxime derivatives have emerged as vasodilators due to their NO-donating capacities. However, whether these oximes offer therapeutic perspectives as an alternative NO
Miguel Diaz et al.
Nitric oxide : biology and chemistry, 92, 1-10 (2019-08-02)
Resveratrol is a plant-derived phytoalexin with antioxidant, anti-inflammatory and cardio-protective properties and may be a promising therapeutic intervention strategy in cardiovascular disease. Here, we investigated the acute direct effects of trans-resveratrol (RV), on acetylcholine (ACh)-induced and flow-mediated dilation (FMD) of
Courtney L Williams et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 34(31), 10402-10414 (2014-08-01)
Stress can reinstate cocaine seeking through an interaction between the stress hormone corticotropin releasing factor (CRF) and glutamate release onto dopamine neurons in the ventral tegmental area (VTA). To better understand the underlying causes, synaptic mechanisms were investigated in brain
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