ChemicalBook CAS DataBase List 361979-40-0

361979-40-0

Name	PCS1055 dihydrochloride
CAS	361979-40-0
Molecular Formula	C27H33ClN4
MDL Number	MFCD30718586
Molecular Weight	449.04
MOL File	361979-40-0.mol

Chemical Properties

storage temp.	2-8°C
form	Solid
color	White to off-white
Water Solubility	H2O: 5mg/mL, clear (warmed)

Hazard Information

Description

PCS1055 is a muscarinic M4 receptor antagonist. PCS1055 represents a new M4-preferring antagonist that may be useful in elucidating the roles of M4 receptor signaling.

Uses

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].

in vivo

PCS1055 (30 mg/kg; intraperitoneal injection; male mice) treatment shows the maximal plasma levels at the 30 min time-point with 45100 nM total and 631nM unbound plasma concentrations. The maximal compound exposure observed in the brain is 11.8 nM at 1 h^[1].

Animal Model:	Male mice^[1]
Dosage:	30 mg/kg
Administration:	Intraperitoneal injection (Pharmacokinetic Analysis)
Result:	The maximal plasma levels were observed at the 30 min time-point with 45100 nM total and 631nM unbound plasma concentrations. The maximal compound exposure observed in the brain was 11.8 nM at 1 h.

IC 50

AChE; mAChR4

References

[1] Croy CH, et al. Characterization of PCS1055, a novel muscarinic M4 receptor antagonist. Eur J Pharmacol. 2016 Jul 5;782:70-6. DOI:10.1016/j.ejphar.2016.04.022
[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. DOI:10.1021/jm001088u

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