sephin1 and 2-guanidine-4-methylquinazoline

sephin1 has been researched along with 2-guanidine-4-methylquinazoline* in 1 studies

Other Studies

1 other study(ies) available for sephin1 and 2-guanidine-4-methylquinazoline

Article	Year
In silico screening of GMQ-like compounds reveals guanabenz and sephin1 as new allosteric modulators of acid-sensing ion channel 3. Biochemical pharmacology, 2020, Volume: 174 Acid-sensing ion channels (ASICs) are voltage-independent cation channels that detect decreases in extracellular pH. Dysregulation of ASICs underpins a number of pathologies. Of particular interest is ASIC3, which is recognised as a key sensor of acid-induced pain and is important in the establishment of pain arising from inflammatory conditions, such as rheumatoid arthritis. Thus, the identification of new ASIC3 modulators and the mechanistic understanding of how these compounds modulate ASIC3 could be important for the development of new strategies to counteract the detrimental effects of dysregulated ASIC3 activity in inflammation. Here, we report the identification of novel ASIC3 modulators based on the ASIC3 agonist, 2-guanidine-4-methylquinazoline (GMQ). Through a GMQ-guided in silico screening of Food and Drug administration (FDA)-approved drugs, 5 compounds were selected and tested for their modulation of rat ASIC3 (rASIC3) using whole-cell patch-clamp electrophysiology. Of the chosen drugs, guanabenz (GBZ), an α Topics: Acid Sensing Ion Channels; Allosteric Regulation; Animals; CHO Cells; Computer Simulation; Cricetinae; Cricetulus; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Guanabenz; Guanidines; Protein Structure, Secondary; Quinazolines	2020

Article

Year

In silico screening of GMQ-like compounds reveals guanabenz and sephin1 as new allosteric modulators of acid-sensing ion channel 3.

Biochemical pharmacology, 2020, Volume: 174

Acid-sensing ion channels (ASICs) are voltage-independent cation channels that detect decreases in extracellular pH. Dysregulation of ASICs underpins a number of pathologies. Of particular interest is ASIC3, which is recognised as a key sensor of acid-induced pain and is important in the establishment of pain arising from inflammatory conditions, such as rheumatoid arthritis. Thus, the identification of new ASIC3 modulators and the mechanistic understanding of how these compounds modulate ASIC3 could be important for the development of new strategies to counteract the detrimental effects of dysregulated ASIC3 activity in inflammation. Here, we report the identification of novel ASIC3 modulators based on the ASIC3 agonist, 2-guanidine-4-methylquinazoline (GMQ). Through a GMQ-guided in silico screening of Food and Drug administration (FDA)-approved drugs, 5 compounds were selected and tested for their modulation of rat ASIC3 (rASIC3) using whole-cell patch-clamp electrophysiology. Of the chosen drugs, guanabenz (GBZ), an α

Topics: Acid Sensing Ion Channels; Allosteric Regulation; Animals; CHO Cells; Computer Simulation; Cricetinae; Cricetulus; Dose-Response Relationship, Drug; Drug Evaluation, Preclinical; Guanabenz; Guanidines; Protein Structure, Secondary; Quinazolines

2020