Results 1 to 10 of about 1,634 (125)

Therapeutic potential of small molecules that block receptor-induced Kv7/M-current suppression in neuroprotection, seizures, and pain. [PDF]

Br J Pharmacol
Receptor‐induced Kv7/M‐current suppression increases neuronal activity and contributes to pathology of several conditions. A new class of Kv7 modulators identified in this study attenuates M‐current suppression and shows therapeutic effects. Abstract Background and Purpose Neuronal Kv7 channels generate low voltage–gated potassium currents known as the
Kim YW, Behara PK, Alhassen L, Wong C, Civelli O, Hoshi N.   +5 more
europepmc   +2 more sources

Could NAPQI Contribute to Paracetamol Analgesia? Redox Modulation of Kv7 Ion Channels. [PDF]

Pharmacol Res Perspect
ABSTRACT Paracetamol (acetaminophen, APAP) is one of the most widely used analgesic and antipyretic drugs worldwide, yet its mechanism of action remains incompletely understood. While several pathways have been proposed, including cyclooxygenase inhibition and endocannabinoid modulation via AM404, none fully account for its pharmacological profile. The
M-Alicante S, Urrutia J, Muguruza-Montero A, Revuelta M, Arrizabalaga-Iriondo A, Villarroel A, Nuñez E.   +6 more
europepmc   +2 more sources

From Retigabine to Azetukalner: Reviving Voltage-Gated Potassium Channels for Epilepsy Therapy. [PDF]

Arch Pharm (Weinheim)
From the withdrawal of retigabine to the breakthrough of azetukalner, this review explores how rational redesign of KV7.2/3 potentiators overcame toxicity hurdles. We detail the synthesis, improved metabolic stability, and robust clinical outcomes in epilepsy, highlighting a new era of targeted potassium channel therapy. ABSTRACT Heterotetrameric KV7.2/
Rosendahl P, Schulig L, Link A.
europepmc   +2 more sources

K_v7 and K_2P Potassium Channels in Thalamocortical Function and Their Therapeutic Potential in Childhood Absence Epilepsy. [PDF]

Arch Pharm (Weinheim)
Modulation of K2P and Kv7 channels has the potential to reduce hyperexcitability and hypersynchronicity within the thalamocortical system. This offers a new avenue to suppress spike and wave discharges, the electrophysiological hallmark of absence epilepsy.
Takhi A, Seebohm G, Budde T, Lüttjohann A.   +3 more
europepmc   +2 more sources

Ganoderic Acid A Ameliorates Pentylenetetrazol-Induced Epilepsy in Mice via Activating KCNQ2. [PDF]

CNS Neurosci Ther
GA‐A binds and activates KCNQ2, thereby reducing epileptic‐like EEG discharges, the loss and apoptosis of hippocampal neurons, and improving anxiety and depression‐like behavioral changes. In addition, GA‐A inhibits neuroinflammation and alleviates oxidative stress independent of activating KCNQ2.
Yao Y, Liu Z, Wang X, Bian C, Wang R, Zhang Y.   +5 more
europepmc   +2 more sources

Identification of Sodium/Myo-Inositol Transporter 1 as a Major Determinant of Arterial Contractility. [PDF]

FASEB J
The tonicity‐responsive enhancer binding‐protein (TonEBP) and serum glucocorticoid kinase (SGK) sense a rise in extracellular hypertonicity resulting in an increase SMIT1 membrane abundance in vascular smooth muscle cells. SMIT1 associates with Kv7.4/5, Gβγ, and KCNE4, promoting hyperpolarization, reduced voltage‐gated calcium channel (VGCC) opening ...
Forrester EA, Lau S, Benitez-Angeles M, Garland CJ, Barrese V, Albert AP, Greenwood IA.   +6 more
europepmc   +2 more sources

Discovery of a potent, Kv7.3-selective potassium channel opener from a Polynesian traditional botanical anticonvulsant [PDF]

Communications Chemistry
Plants remain an important source of biologically active small molecules with high therapeutic potential. The voltage-gated potassium (Kv) channel formed by Kv7.2/3 (KCNQ2/3) heteromers is a major target for anticonvulsant drug development.
Geoffrey W. Abbott, Rían W. Manville
doaj   +2 more sources

Channel Dysfunction as the Basis for Comorbidities in Multiple Sclerosis and Depression. [PDF]

Arch Pharm (Weinheim)
Ion channel remodelling induced by neuroinflammation in multiple sclerosis alters neuronal excitability and immune signalling, creating shared molecular pathways that link multiple sclerosis pathology to depression and reveal novel pharmacological targets.
Rychlik N, Jüngling K, Meuth SG, Budde T, Méndez-Couz M.   +4 more
europepmc   +2 more sources

Pharmacological approaches in drug-resistant pediatric epilepsies caused by pathogenic variants in potassium channel genes [PDF]

Frontiers in Cellular Neuroscience
Variants in genes encoding for voltage-gated K+ (Kv) channels are frequent cause of drug-resistant pediatric epilepsies. Obtaining a molecular diagnosis gives the opportunity to assess the efficacy of pharmacological strategies based on in vitro features
Ilaria Filareto, Ilaria Mosca, Elena Freri, Francesca Ragona, Laura Canafoglia, Roberta Solazzi, Barbara Castellotti, Giuliana Messina, Cinzia Gellera, Maria Virginia Soldovieri, Paolo Ambrosino, Maurizio Taglialatela, Jacopo C. DiFrancesco, Tiziana Granata   +13 more
doaj   +2 more sources

System-wide targeted analysis of oxylipins and lipoproteins in chronic peripheral neuropathic pain—an explorative study [PDF]

PAIN Reports
. Introduction:. Neuroinflammation and oxidative dysfunction, and their reciprocal interplay, are critically involved in the pathophysiology of chronic neuropathic pain (NeuP).
Mika Jönsson, Emmanuel Bäckryd, Stefan Ljunggren, Nina Ottosson, Amaia Jauregi-Miguel, Sara I. Liin, Antonio Checa, Craig E. Wheelock, Bijar Ghafouri   +8 more
doaj   +2 more sources