HUMAN RECOMBINANT D4 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Full-length Human DRD4 cDNA (GenBank Accession NM_000797) with FLAG-tag sequence at the N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin
Stable in culture for minimum of two months
Background: The human dopamine receptor D4 is a D2-like receptor that inhibits adenylyl cyclase activity and activates K+ channels. D4 receptor antagonists show great potential in the treatment of human personality and psychiatric disorders, such as ADHD (Attention deficit hyperactivity disorder), schizophrenia, alcoholism, and drug addiction.
Application: Functional assays
Figure 1. Dose-dependent stimulation of calcium flux upon treatment with ligand, measured with MultiscreenTM Calcium 1.0 No Wash Assay Kit (Multispan MSCA01). Figure 2. Dose-dependent inhibition of forskolin-stimulated intracellular cAMP level upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 3. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Kulkarni SK, et al. (2000) Dopamine D4 receptors and development of newer antipsychotic drugs. Fundam Clin Pharmacol 14(6):529-39.
Missale C, et al. (1998) Dopamine receptors: from structure to function. Physiol Rev 78(1):189-225.
Van Tol HH, et al. (1991) Cloning of the gene for a human dopamine D4 receptor with high affinity for the antipsychotic clozapine. Nature 350(6319):610-4