RAT RECOMBINANT GPR88 RECEPTOR
MULTISCREENTM STABLE CELL LINE
1 vial (2 x 106) frozen cells
Expression vector containing full-length rat GPR88 cDNA (GenBank Accession Number: NM_031696.2) with FLAG tag sequence at N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM/F12, 10% FBS, 10 μg/mL puromycin
Stability: In progress
Background: GPR88 is an orphan G protein-coupled receptor (GPCR) considered as a promising therapeutic target for neuropsychiatric disorders including schizophrenia, Parkinson’s disease, anxiety, and addiction. The biological effects of GPR88 activation and signal transduction pathway are still unknown due to the lack of a selective agonist appropriate for in vivo investigation.
Application: Functional assays
Figure 1. Dose-dependent inhibition of forskolin-stimulated intracellular cAMP accumulation upon treatment with ligand, measured with MULTISCREENTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01).
Chunyang Jin, Ann M. Decker, Viren H. Makhijani, et al (2018). Discovery of a Potent, Selective, and Brain-Penetrant Small Molecule that Activates the Orphan Receptor GPR88 and Reduces Alcohol Intake. Med Chem. 2018 August 09; 61(15): 6748–6758
Jin, C., Decker, A. M., Huang, X. P., Gilmour, B. P., Blough, B. E., Roth, B. L., Hu, Y., Gill, J. B., & Zhang, X. P. (2014). Synthesis, pharmacological characterization, and structure-activity relationship studies of small molecular agonists for the orphan GPR88 receptor. ACS chemical neuroscience, 5(7), 576–587.