HUHS2002 is a free fatty acid derivative that primarily targets cholinesterase (ChE) to enhance α7 nicotinic acetylcholine receptor activity. This compound significantly increases whole-cell membrane currents of α7 ACh receptors expressed in Xenopus oocytes in a concentration-dependent manner, with effects reversibly blocked by the Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93. Furthermore, HUHS2002 activates CaMKII in cultured rodent hippocampal neurons, an effect also inhibited by KN-93. Additionally, HUHS2002 exhibits partial inhibition of protein phosphatase 1 (PP1) activity in a cell-free assay, suggesting its potential use in studying cholinergic signaling pathways and neuropharmacology.
HUHS2002 is a free fatty acid derivative that primarily targets cholinesterase (ChE) to enhance α7 nicotinic acetylcholine receptor activity. This compound significantly increases whole-cell membrane currents of α7 ACh receptors expressed in Xenopus oocytes in a concentration-dependent manner, with effects reversibly blocked by the Ca2+/calmodulin-dependent protein kinase II (CaMKII) inhibitor KN-93. Furthermore, HUHS2002 activates CaMKII in cultured rodent hippocampal neurons, an effect also inhibited by KN-93. Additionally, HUHS2002 exhibits partial inhibition of protein phosphatase 1 (PP1) activity in a cell-free assay, suggesting its potential use in studying cholinergic signaling pathways and neuropharmacology.
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