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Description

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, VPAC2 is expressed on stimulated CD4 T cells, and binding of T cell-derived VIP to VPAC2 induces a shift toward the Th2 pathway (Delgado et al., 2004, Voice et al., 2004). In addition, VPAC2 is an essential regulator of the circadian pacemaker of the hypothalamic suprachiasmatic nuclei (Hughes et al., 2004). Chemicon's VPAC2 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 VPAC2 interactions with PACAP. The membrane preparations exhibit a Kd of 0.9 nM for [125I]-PACAP27. With 5 µ,g/well VPAC2 Membrane Prep and 0.5 nM [125I]-PACAP27, a greater than 15-fold signal-to-background ratio was obtained., Human VPAC2