SML1848
PCS1055 二盐酸盐
≥98% (HPLC)
别名:
6,7-二氢-N- [2- [1-（苯甲基）-4-哌啶基]乙基] -5H-苯并[6,7]环庚[1,2-c]哒嗪-3-胺二盐酸盐
InChI
1S/C27H32N4.2ClH/c1-2-7-22(8-3-1)20-31-17-14-21(15-18-31)13-16-28-26-19-24-11-6-10-23-9-4-5-12-25(23)27(24)30-29-26;;/h1-5,7-9,12,19,21H,6,10-11,13-18,20H2,(H,28,29);2*1H
InChI key
VSCSFYDNGYAWKG-UHFFFAOYSA-N
SMILES string
[H]Cl.[H]Cl.C12=C(N=NC(NCCC3CCN(CC4=CC=CC=C4)CC3)=C2)C5=C(C=CC=C5)CCC1
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 5 mg/mL, clear (warmed)
storage temp.
2-8°C
Quality Level
Biochem/physiol Actions
PCS1055 是高效的、选择性毒蕈碱型 M4 乙酰胆碱受体竞争性拮抗剂，比对 M1、M3 和 M5 受体的选择性 > 100 倍，比对 M2 受体的选择性高 30 倍。PCS1055 最初被描述为高效电鳗 AChE 抑制剂（IC50 = 22 nM），而对人 AChE 的效力较弱（IC50 = 120 nM）。
高效选择性毒蕈碱 M4 受体拮抗剂
hcodes
pcodes
Hazard Classifications
Aquatic Chronic 4
存储类别
11 - Combustible Solids
wgk
WGK 3
Carrie H Croy et al.
European journal of pharmacology, 782, 70-76 (2016-04-18)
Identification of synthetic ligands selective for muscarinic receptor subtypes has been challenging due to the high sequence identity and structural homology among the five muscarinic acetylcholine receptors. Here, we report the pharmacological characterization of PCS1055, a novel muscarinic M4 receptor
J M Contreras et al.
Journal of medicinal chemistry, 44(17), 2707-2718 (2001-08-10)
Starting from the 3-[2-(1-benzylpiperidin-4-yl)ethylamino]-6-phenylpyridazine 1, we performed the design, the synthesis, and the structure-activity relationships of a series of pyridazine analogues acting as AChE inhibitors. Structural modifications were achieved on four different parts of compound 1 and led to the
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