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v5754
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Thomas S Dash et al.
Structure (London, England : 1993), 27(2), 315-326 (2018-12-18)
Disulfide-rich peptides (DRPs) play diverse physiological roles and have emerged as attractive sources of pharmacological tools and drug leads. Here we describe the 3D structure of a centipede venom peptide, U-SLPTX15-Sm2a, whose family defines a unique class of one of
X Zheng et al.
Toxicon : official journal of the International Society on Toxinology, 101, 41-47 (2015-05-06)
Saxitoxin (STX), a member of the family of paralytic shellfish poisoning toxins, poses toxicological and ecotoxicological risks. To develop an analytical recognition element for STX, a DNA aptamer (APT(STX1)) was previously discovered via an iterative process known as Systematic Evolution
Carsten Stoetzer et al.
Naunyn-Schmiedeberg's archives of pharmacology, 389(3), 315-325 (2015-12-17)
Propofol and dexmedetomidine are very commonly used sedative agents. However, several case reports demonstrated cardiovascular adverse effects of these two sedatives. Both substances were previously demonstrated to quite potently inhibit neuronal voltage-gated Na(+) channels. Thus, a possible molecular mechanism for
M Kammerer et al.
Naunyn-Schmiedeberg's archives of pharmacology, 384(1), 47-57 (2011-05-03)
In epilepsy, allegedly, a neurotransmitter imbalance between the inhibitory GABA and the excitatory glutamate prevails. Therefore, some antiepileptic drugs (AEDs) are thought to increase GABA release. Because little is known about corresponding presynaptic effects of AEDs in the human brain
Xiaojia Li et al.
Naunyn-Schmiedeberg's archives of pharmacology, 388(12), 1259-1269 (2015-08-11)
Ikarisoside A is a natural flavonol glycoside derived from plants of the genus Epimedium, which have been used in Traditional Chinese Medicine as tonics, antirheumatics, and aphrodisiacs. Here, we report the effects of ikarisoside A and three other flavonol glycosides
Shan Zou et al.
PloS one, 8(8), e73499-e73499 (2013-09-12)
In ischemic and traumatic brain injury, hyperactivated glutamate (N-methyl-D-aspartic acid, NMDA) and sodium (Nav) channels trigger excitotoxic neuron death. Na(+), Ca(++) and H2O influx into affected neurons elicits swelling (increased cell volume) and pathological blebbing (disassociation of the plasma membrane's
Maria M Buckley et al.
Frontiers in cellular neuroscience, 14, 95-95 (2020-05-20)
An intact gut epithelium preserves the immunological exclusion of "non-self" entities in the external environment of the gut lumen. Nonetheless, information flows continuously across this interface, with the host immune, endocrine, and neural systems all involved in monitoring the luminal
Chunlei Zhang et al.
Fitoterapia, 122, 20-25 (2017-08-16)
Iritectol G, a novel iridal-type triterpenoid containing an uncommon tetrahydrofuran moiety, was isolated from the rhizomes of Iris tectorum. The structure was elucidated by comprehensive spectroscopic analysis. Iritectol G inhibited spontaneous and 4-aminopyridine-evoked calcium oscillations in primary cultured neocortical neurons
Jose Manuel Leão et al.
Marine drugs, 16(3) (2018-03-07)
Tetrodotoxins (TTX) are a potent group of natural neurotoxins putatively produced by symbiotic microorganisms and affecting the aquatic environment. These neurotoxins have been recently found in some species of bivalves and gastropods along the European Coasts (Greece, UK, and The
Jiali Nie et al.
Journal of cellular physiology, 234(7), 11587-11601 (2018-11-30)
Cardiac hypertrophy and heart failure are characterized by increased late sodium current and abnormal Ca2+ handling. Ranolazine, a selective inhibitor of the late sodium current, can reduce sodium accumulation and Ca 2+ overload. In this study, we investigated the effects
Pablo Estevez et al.
Toxins, 11(4) (2019-04-25)
Ciguatera Fish Poisoning is a worldwide concern caused by the consumption of fish contaminated with ciguatoxins not only in endemic regions in the Pacific Ocean or the Caribbean Sea but also in emerging areas of Macaronesia on the eastern Atlantic.
Ai Yoshinaka-Niitsu et al.
Bioorganic & medicinal chemistry, 20(9), 2796-2802 (2012-04-10)
Voltage-gated sodium channels (VGSCs) are responsible for generating action potentials in nervous systems. Veratridine (VTD), a lipid soluble alkaloid isolated from sabadilla lily seed, is believed to bind to segment 6 of VGSCs and act as a partial agonist. However
Huayue Li et al.
Biochimica et biophysica acta, 1830(3), 2591-2599 (2012-12-04)
Herein we report the discovery of a cystine-crosslinked peptide from Porifera along with high-quality spatial details accompanied by the description of its unique effect on neuronal calcium influx. Asteropsin A (ASPA) was isolated from the marine sponge Asteropus sp., and
Sameer Otoom et al.
Neuro endocrinology letters, 32(4), 487-490 (2011-08-31)
Veratridine was characterized previously as an experimental model of epilepsy in vitro. The aim of this preliminary investigation is to identify the pattern of seizure induced by this model in vivo. Veratridine (200 μg/kg) was administered intraperitoneally to male Sprague-Dawley rats
Giuseppe Tringali et al.
The journal of headache and pain, 19(1), 107-107 (2018-11-14)
Perampanel is a novel antiepileptic drug acting via non-competitive antagonism on glutamatergic AMPA receptors, and the subsequent inhibition of ion calcium influx. Since it was recently postulated that the antagonists of glutamate receptors might play a role in the treatment
Pierre Morissette et al.
Toxicology and applied pharmacology, 390, 114883-114883 (2020-01-26)
Human-based in silico models are emerging as important tools to study the effects of integrating inward and outward ion channel currents to predict clinical proarrhythmic risk. The aims of this study were 2-fold: 1) Evaluate the capacity of an in
Peter Milberg et al.
Heart rhythm, 9(4), 570-578 (2011-11-15)
Molecular remodeling in heart failure includes slowing of repolarization, leading to proarrhythmia. To evaluate the effects of Na(+)/Ca(2+) exchanger (NCX) inhibition on repolarization as a novel antiarrhythmic concept in chronic heart failure (CHF). CHF was induced by rapid ventricular pacing
Chelsea R White et al.
Immunobiology, 224(1), 80-93 (2018-11-06)
Prior work demonstrated that a splice variant of SCN5A, a voltage-gated sodium channel gene, acts as a cytoplasmic sensor for viral dsRNA in human macrophages. Expression of this channel also polarizes macrophages to an anti-inflammatory phenotype in vitro and in
Takayuki Nemoto et al.
FEBS letters, 587(7), 898-905 (2013-02-26)
Endothelin-1 and voltage-dependent sodium channels are involved in control and suppression of neuropathological factors, which contribute to sculpting the neuronal network. We previously demonstrated that veratridine-induced NaV1.7 sodium channel activation caused intracellular calcium elevation, catecholamine secretion and tau dephosphorylation in
Ming Yang et al.
Journal of cellular physiology, 235(4), 3950-3972 (2019-10-16)
Ion channels can regulate the plasma membrane potential (Vm ) and cell migration as a result of altered ion flux. However, the mechanism by which Vm regulates motility remains unclear. Here, we show that the Nav 1.5 sodium channel carries
Michael P Rassner et al.
Epilepsia, 54(3), e41-e44 (2013-01-31)
To learn whether epileptic seizures in Rasmussen encephalitis (RE) may be promoted by insufficient γ-aminobutyric acid (GABA) release. (3) H-GABA was released from neocortical synaptosomes through transporter reversal following intrasynaptosomal Na(+) accumulation by veratridine that prevents inactivation of Na(+) channels.
Irina Vetter et al.
Biochemical pharmacology, 83(11), 1562-1571 (2012-03-14)
The human neuroblastoma cell line SH-SY5Y is a potentially useful model for the identification and characterisation of Na(v) modulators, but little is known about the pharmacology of their endogenously expressed Na(v)s. The aim of this study was to determine the
Michael Didriksen et al.
Journal of psychiatry & neuroscience : JPN, 42(1), 48-58 (2016-07-09)
The hemizygous 22q11.2 microdeletion is a common copy number variant in humans. The deletion confers high risk for neurodevelopmental disorders, including autism and schizophrenia. Up to 41% of deletion carriers experience psychotic symptoms. We present a new mouse model (Df(h22q11)/+)
Elisa Mura et al.
PloS one, 7(1), e29661-e29661 (2012-01-19)
We previously showed that beta-amyloid (Aβ), a peptide considered as relevant to Alzheimer's Disease, is able to act as a neuromodulator affecting neurotransmitter release in absence of evident sign of neurotoxicity in two different rat brain areas. In this paper
Pedro Reis Costa et al.
Toxins, 13(4) (2021-04-04)
Tetrodotoxin (TTX) is a potent neurotoxin, considered an emerging toxin in Europe where recently a safety limit of 44 µg TTX kg-1 was recommended by authorities. In this study, three specimens of the large gastropod trumpet shell Charonia lampas bought
Travis A Hage et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 32(8), 2714-2721 (2012-02-24)
We report a novel coupled system of sodium-activated potassium currents (I(KNa)) and persistent sodium currents (I(NaP)), the components of which are widely distributed throughout the brain. Its existence and importance has not been previously recognized. Although I(KNa) was known to
Michele Morari et al.
The Journal of pharmacology and experimental therapeutics, 364(2), 198-206 (2017-11-24)
Safinamide has been recently approved as an add-on to levodopa therapy for Parkinson disease. In addition to inhibiting monoamine oxidase type B, it blocks sodium channels and modulates glutamate (Glu) release in vitro. Since this property might contribute to the
J E Medland et al.
Neurogastroenterology and motility : the official journal of the European Gastrointestinal Motility Society, 28(9), 1317-1329 (2016-05-03)
Early life adversity (ELA) is a risk factor for the later-life onset of gastrointestinal (GI) diseases such as irritable bowel syndrome (IBS); however, the mechanisms are poorly understood. Here, we utilized a porcine model of ELA, early weaning stress (EWS)
Maarten E A Reith et al.
The Journal of pharmacology and experimental therapeutics, 343(2), 413-425 (2012-08-17)
Despite a wealth of information on cocaine-like compounds, there is no information on cocaine analogs with substitutions at C-1. Here, we report on (R)-(-)-cocaine analogs with various C-1 substituents: methyl (2), ethyl (3), n-propyl (4), n-pentyl (5), and phenyl (6).
Wesley L McKeithan et al.
Frontiers in physiology, 8, 766-766 (2017-10-28)
The ability to produce unlimited numbers of human induced pluripotent stem cell derived cardiomyocytes (hiPSC-CMs) harboring disease and patient-specific gene variants creates a new paradigm for modeling congenital heart diseases (CHDs) and predicting proarrhythmic liabilities of drug candidates. However, a
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