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Description

Human VIPR1 cDNA, encoding VPAC1, Vasoactive intestinal peptide (VIP), a 28 amino acid peptide originally isolated by its vasodilation activity, binds to two class B GPCRs, VPAC1 and VPAC2, to exert its functions in the CNS, vasculature, immune system and adrenal medulla (Harmar et al., 1998). In the immune system, VIP is synthesized by mast cells and lymphocytes, and appears to inhibit inflammation and to shift the immune response toward a Th2 pathway (Delgado et al., 2004). In the heart, VIP is expressed by nerve fibers, where it modulates heart rate, and coronary blood flow (Henning and Sawmiller, 2001). Chemicon's VPAC1 membrane preparations are crude membrane preparations made from our proprietary stable recombinant cell lines to ensure high-level of GPCR surface expression, thus, they are ideal HTS tools for screening of antagonists of VPAC1 interactions with VIP. The membrane preparations exhibit a Kd of 1.2 nM for [125I]-VIP. With 2.5 mug/well VPAC1 Membrane Prep and 0.4 nM [125I]-VIP, a greater than 5-fold signal-to-background ratio is obtained.