PCS1055 dihydrochloride is a selective and competitive antagonist of the muscarinic M4 receptor, with an IC50 value of 18.1 nM and a Kd of 5.72 nM. This compound effectively inhibits the binding of the radioligand [3H]-NMS to the M4 receptor, displaying a Ki of 6.5 nM. PCS1055 dihydrochloride demonstrates over 100-fold selectivity against M1, M3, and M5 receptors, and 30-fold selectivity at the M2 receptor. Additionally, it serves as a potent acetylcholinesterase inhibitor, with IC50 values of 22 nM and 120 nM for electric eel and human AChE, respectively, highlighting its potential for various neurological research applications.
PCS1055 dihydrochloride is a selective and competitive antagonist of the muscarinic M4 receptor, with an IC50 value of 18.1 nM and a Kd of 5.72 nM. This compound effectively inhibits the binding of the radioligand [3H]-NMS to the M4 receptor, displaying a Ki of 6.5 nM. PCS1055 dihydrochloride demonstrates over 100-fold selectivity against M1, M3, and M5 receptors, and 30-fold selectivity at the M2 receptor. Additionally, it serves as a potent acetylcholinesterase inhibitor, with IC50 values of 22 nM and 120 nM for electric eel and human AChE, respectively, highlighting its potential for various neurological research applications.
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