315698-36-3
315698-36-3
Chemical Structure
MLS1547
- CAS No.: 315698-36-3
- Formula:C19H19ClN4O
- Molecular Weight:354.83
IUPAC Name: 5-chloro-7-((4-(pyridin-2-yl)piperazin-1-yl)methyl)quinolin-8-ol
InChIKey: OPEJNANYABTIGC-UHFFFAOYSA-N
SMILES: OC1=C2N=CC=CC2=C(Cl)C=C1CN3CCN(C4=NC=CC=C4)CC3
Biological Activity: MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM)[1][2].
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MLS1547 | 99.94% | MLS1547 is a highly efficacious G protein-biased dopamine D2 receptor (D2R) agonist (Ki=1.2 μM). MLS1547 stimulates D2R G protein-mediated signaling (EC50=0.37 μM in a calcium mobilization assay). MLS1547 acts as an antagonist for dopamine (DA)-stimulated β-arrestin recruitment to the D2R (IC50=9.9 μM). | ||||||||||||||||||||
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References
- [1]. Free RB, et al. Discovery and characterization of a G protein-biased agonist that inhibits β-arrestin recruitment to the D2 dopamine receptor. Mol Pharmacol. 2014;86(1):96-105. [Content Brief]
- [2]. Chun LS, et al. Structure-Activity Investigation of a G Protein-Biased Agonist Reveals Molecular Determinants for Biased Signaling of the D2 Dopamine Receptor. Front Synaptic Neurosci. 2018;10:2. Published 2018 Feb 21. [Content Brief]
Keywords
