SML1848
PCS1055 dihydrochloride
≥98% (HPLC)
Synonym(s):
6,7-Dihydro-N-[2-[1-(phenylmethyl)-4-piperidinyl]ethyl]-5H-benzo[6,7]cyclohepta[1,2-c]pyridazin-3-amine dihydrochloride
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About This Item
Empirical Formula (Hill Notation):
C27H32N4 · 2HCl
CAS Number:
Molecular Weight:
485.49
UNSPSC Code:
12352200
NACRES:
NA.77
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Quality Level
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
H2O: 5 mg/mL, clear (warmed)
storage temp.
2-8°C
SMILES string
[H]Cl.[H]Cl.C12=C(N=NC(NCCC3CCN(CC4=CC=CC=C4)CC3)=C2)C5=C(C=CC=C5)CCC1
Biochem/physiol Actions
PCS1055 is a potent and selective muscarinic M4 acetylcholine receptor competitive antagonist that exhibits >100-fold selectivity over M1-, M3-, and M5-receptors and 30-fold selectivity at the M2 receptor. PCS1055 was originally described as a potent electric eel AChE inhibitor (IC50 = 22 nM) and less potent at human AChE (IC50 = 120 nM).
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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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