[HTML][HTML] Structural insights into the mechanisms and pharmacology of K2P potassium channels

AM Natale, PE Deal, DL Minor Jr - Journal of molecular biology, 2021 - Elsevier
Leak currents, defined as voltage and time independent flows of ions across cell
membranes, are central to cellular electrical excitability control. The K 2P (KCNK) potassium …

The Background K+ Channel TRESK in Sensory Physiology and Pain

A Andres-Bilbe, A Castellanos, A Pujol-Coma… - International Journal of …, 2020 - mdpi.com
TRESK belongs to the K2P family of potassium channels, also known as background or leak
potassium channels due to their biophysical properties and their role regulating membrane …

Biologically active compounds and drugs in the tetrazole series

LV Myznikov, SV Vorona, YE Zevatskii - Chemistry of Heterocyclic …, 2021 - Springer
The review summarizes the advances in medicinal chemistry of tetrazole biologically active
compounds and drugs over the past 15 years. Most of the considered compounds are at …

Protein and Chemical Determinants of BL-1249 Action and Selectivity for K2P Channels

L Pope, C Arrigoni, H Lou, C Bryant… - ACS chemical …, 2018 - ACS Publications
K2P potassium channels generate leak currents that stabilize the resting membrane
potential of excitable cells. Various K2P channels are implicated in pain, ischemia …

Investigation of the Spatial Structure of Flufenamic Acid in Supercritical Carbon Dioxide Media via 2D NOESY

IA Khodov, KV Belov, MA Krestyaninov, AA Dyshin… - Materials, 2023 - mdpi.com
The search for new forms of already known drug compounds is an urgent problem of high
relevance as more potent drugs with fewer side effects are needed. The trifluoromethyl …

Synthesis and Medicinal Applications of Fenamic Acid Derivatives

M Sharma, P Prasher - Current Organic Chemistry, 2023 - ingentaconnect.com
Fenamic acid-derived NSAIDs contain N-phenyl anthranilic acid as a pharmacophore with
pKa∼ 4, which is completely ionized at the physiological pH and is mainly excreted in the …

Selective and state‐dependent activation of TRESK (K2P18.1) background potassium channel by cloxyquin

M Lengyel, A Dobolyi, G Czirják… - British Journal of …, 2017 - Wiley Online Library
Background and Purpose Cloxyquin (5‐cloroquinolin‐8‐ol) has been described as an
activator of TRESK (K2P18. 1, TWIK‐related spinal cord K+ channel) background potassium …

A “target class” screen to identify activators of two-pore domain potassium (K2P) channels

D McCoull, E Ococks, JM Large… - … the Science of Drug …, 2021 - journals.sagepub.com
Two-pore domain potassium (K2P) channels carry background (or leak) potassium current
and play a key role in regulating resting membrane potential and cellular excitability …

Synthesis of flufenamic acid: an organic chemistry lab sequence using boronic acids and nitrosoarenes under transition-metal-free conditions

S Roscales, AG Csákÿ - Journal of Chemical Education, 2019 - ACS Publications
A method for the synthesis of flufenamic acid, a nonstereoidal anti-inflammatory drug
(NSAID) of the anthranilate family (fenams), is described as an experiment for the upper …

Conformational Analysis of Flufenamic Acid in SC-CO2 by 2D NOESY

KV Belov, AA Dyshin, MA Krestyaninov… - Russian Journal of …, 2023 - Springer
The possibilities of nuclear Overhauser effect spectroscopy (NOESY) for conformational
analysis of fenamate (eg, flufenamic acid) molecules were shown. It was established that the …