315698-36-3

315698-36-3 structure

Name: MLS 1547
Chemical Name: MLS1547
CAS Number: 315698-36-3
Molecular Formula: C₁₉H₁₉ClN₄O
Molecular Weight: 354.833
Catalog: Signaling Pathways GPCR/G Protein Dopamine Receptor
Create Date: 2018-07-04 02:03:41
Modify Date: 2024-01-02 11:35:04
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].

Name	MLS1547
Synonyms	MLS1547 5-chloro-7-{[4-(pyridin-2-yl)piperazin-1-yl]methyl}quinolin-8-ol 5-Chloro-7-(4-pyridin-2-yl-piperazin-1-ylmethyl)-quinolin-8-ol 5-Chloro-7-{[4-(2-pyridinyl)-1-piperazinyl]methyl}-8-quinolinol 8-Quinolinol, 5-chloro-7-[[4-(2-pyridinyl)-1-piperazinyl]methyl]- MFCD02330713

Description	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].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Dopamine Receptor Signaling Pathways >> Neuronal Signaling >> Dopamine Receptor Research Areas >> Neurological Disease
In Vitro	MLS1547 fully antagonizes dopamine-mediated β-arrestin recruitment to the D2R in the DiscoveRx assay, with an IC50 of 9.9 μM. Similar results were obtained when MLS1547 was examined for antagonist activity in the D2R β-arrestin BRET assay, demonstrating an IC50 of 3.8 μM. MLS1547 is found to completely displace [3H]methylspiperone binding to the D2R, with a calculated Ki of 1.2 μM[1].
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. [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.