361979-40-0
Chemical Structure
PCS1055 dihydrochloride
- CAS No.: 361979-40-0
- Formula:C27H34Cl2N4
- Molecular Weight:485.49
IUPAC Name: N-(2-(1-benzylpiperidin-4-yl)ethyl)-6,7-dihydro-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-amine dihydrochloride
InChIKey: VSCSFYDNGYAWKG-UHFFFAOYSA-N
SMILES: [H]Cl.[H]Cl.C12=NN=C(NCCC3CCN(CC4=CC=CC=C4)CC3)C=C1CCCC5=CC=CC=C52
Biological Activity: PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively[1][2].
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PCS1055 dihydrochloride | 98.88% | PCS1055 dihydrochloride is a potent, selective and competitive muscarinic M4 receptor antagonist with an IC50 of 18.1 nM and a Kd of 5.72 nM. PCS1055 dihydrochloride inhibits radioligand [3H]-NMS binding to the M4 receptor with a Ki of 6.5 nM. PCS1055 dihydrochloride exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 dihydrochloride is also a potent AChE inhibitor with IC50 s of 22 nM and 120 nM for electric eel and human AChE, respectively. | ||||||||||||||||||||
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References
- [1]. Croy CH, et al. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol. 2016 Jul 5;782:70-6. [Content Brief]
- [2]. Contreras JM, et al. Design, synthesis, and structure-activity relationships of a series of 3-[2-(1-benzylpiperidin-4-yl)ethylamino]pyridazine derivatives as acetylcholinesterase inhibitors. J Med Chem. 2001 Aug 16;44(17):2707-18. [Content Brief]
