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XB-ART-10207
J Biol Chem 2000 Dec 15;27550:39324-31. doi: 10.1074/jbc.M004385200.
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Identification and characterization of two G protein-coupled receptors for neuropeptide FF.

Bonini JA , Jones KA , Adham N , Forray C , Artymyshyn R , Durkin MM , Smith KE , Tamm JA , Boteju LW , Lakhlani PP , Raddatz R , Yao WJ , Ogozalek KL , Boyle N , Kouranova EV , Quan Y , Vaysse PJ , Wetzel JM , Branchek TA , Gerald C , Borowsky B .


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The central nervous system octapeptide, neuropeptide FF (NPFF), is believed to play a role in pain modulation and opiate tolerance. Two G protein-coupled receptors, NPFF1 and NPFF2, were isolated from human and rat central nervous system tissues. NPFF specifically bound to NPFF1 (K(d) = 1.13 nm) and NPFF2 (K(d) = 0.37 nm), and both receptors were activated by NPFF in a variety of heterologous expression systems. The localization of mRNA and binding sites of these receptors in the dorsal horn of the spinal cord, the lateral hypothalamus, the spinal trigeminal nuclei, and the thalamic nuclei supports a role for NPFF in pain modulation. Among the receptors with the highest amino acid sequence homology to NPFF1 and NPFF2 are members of the orexin, NPY, and cholecystokinin families, which have been implicated in feeding. These similarities together with the finding that BIBP3226, an anorexigenic Y1 receptor ligand, also binds to NPFF1 suggest a potential role for NPFF1 in feeding. The identification of NPFF1 and NPFF2 will help delineate their roles in these and other physiological functions.

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Species referenced: Xenopus
Genes referenced: cck hcrt npff npffr1.1 npffr2 npy