Orignially characterized as an mGluR5 negative allosteric modulator (IC50 = 1.35 μM, Emax = 3.82% of Glu Emax; rat mGluR5 HEK293A cells), ML365 is now better known as selective two-pore potassium (K2P) channel TASK1 (K2P3.1; KCNK3) inhibitor with 100- and 62-fold selectivity over TASK3 (K2p9.1; KCNK9), respectively, by thellium flux (rat TASK1/TASK3 CHO cell IC50 = 4/390 nM) and QPatch assay (rat TASK1/TASK3 CHO cell IC50 = 16/990 nM). ML365 is employed in the range from 40 nM to 20 μM. Selective TASK1 blockage is achieved at the lower end of the concentration range, while TASK3 activity can also be inhibited at the high end of the range.
Selective two-pore potassium (K2P) channel TASK1 (K2P3.1; KCNK3) inhibitor with 62- to 100-fold selectivity over TASK3 (K2p9.1; KCNK9).
Código de clase de almacenamiento
13 - Non Combustible Solids
Clase de riesgo para el agua (WGK)
WGK 3
Punto de inflamabilidad (°F)
Not applicable
Punto de inflamabilidad (°C)
Not applicable
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The noradrenergic neurons of the locus coeruleus (LC) are associated with various brain functions and psychiatric disorders, such as addiction and depression. It has been shown that neuropeptide galanin (GAL) inhibits neuronal excitability in LC, but the mechanisms remain unclear.
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