| Identification | Back Directory | [Name]
PCS1055 dihydrochloride | [CAS]
361979-40-0 | [Synonyms]
PCS1055 dihydrochloride
PCS1055 dihydrochloride >=98% (HPLC) | [Molecular Formula]
C27H33ClN4 | [MDL Number]
MFCD30718586 | [MOL File]
361979-40-0.mol | [Molecular Weight]
449.04 |
| Hazard Information | Back Directory | [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.
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| [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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| Company Name: |
Energy Chemical
|
| Tel: |
021-58432009 400-005-6266 |
| Website: |
http://www.energy-chemical.com |
| Company Name: |
Merck KGaA
|
| Tel: |
21-20338288 |
| Website: |
www.sigmaaldrich.cn |
|