HUMAN RECOMBINANT PAC1 RECEPTOR
MULTISCREEN™ STABLE CELL LINES
1 vial (2 x 106) frozen cells
Sigma Freezing Medium (C-6164)
Full-length Human ADCYAP1R1 cDNA (GenBank Accession Number NM_001118.3) with FLAG-tag sequence at the N-terminus
Liquid nitrogen upon receiving
Propagation Medium: DMEM, 10% FBS, 1 μg/mL puromycin
Background: The pituitary adenylate cyclase-activating polypeptide (PACAP)- selective PAC1 receptor (PAC1R, ADCYAP1R1) is a member of the vasoactive intestinal peptide (VIP) family of G protein-coupled receptors (GPCRs). PAC1R has been shown to play crucial roles in the central and peripheral nervous systems. Inadequate PACAP/PAC1R signaling has been implicated in a number of disorders, including stress-related psychopathologies (i.e., depression, posttraumatic stress disorder, and related abnormalities), chronic pain and migraine, and metabolic diseases. Repealing PAC1R signaling under these pathological conditions represent opportunities for therapeutic intervention.
Application: Functional assays
Figure 1. Dose-dependent stimulation of intracellular cAMP accumulation upon treatment with ligand, measured with MultiscreenTM TR-FRET cAMP 1.0 No Wash Assay Kit (Multispan MSCM01). Figure 2. Receptor expression on cell surface measured by flow cytometry (FACS) using an anti-FLAG antibody. Thin line: parental cells; thick line: receptor-expressing cells.
Dautzenberg FM, Mevenkamp G, Wille S, Hauger RL. (1999) N-terminal splice variants of the type I PACAP receptor: isolation, characterization and ligand binding/selectivity determinants. J Neuroendocrinol, 11 (12): 941-9. [PMID:10583729]
Dickson L, Aramori I, McCulloch J, Sharkey J, Finlayson K. (2006) A systematic comparison of intracellular cyclic AMP and calcium signalling highlights complexities in human VPAC/PAC receptor pharmacology. Neuropharmacology, 51 (6): 1086-98. [PMID:16930633]
Moody TW, Jensen RT, Fridkin M, Gozes I. (2002) (N-steary l, norleucine17) VIP hy brid is a broad spectrum vasoactive intestinal peptide receptor antagonist. J Mol Neurosci, 18 (1-2): 29-35. [PMID:11931347]