Bonini J A, Jones K A, Adham N, Forray C, Artymyshyn R, Durkin M M, Smith K E, Tamm J A, Boteju L W, Lakhlani P P, Raddatz R, Yao W J, Ogozalek K L, Boyle N, Kouranova E V, Quan Y, Vaysse P J, Wetzel J M, Branchek T A, Gerald C, Borowsky B
Synaptic Pharmaceutical Corporation, Paramus, New Jersey 07652, USA.
J Biol Chem. 2000 Dec 15;275(50):39324-31. doi: 10.1074/jbc.M004385200.
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.
中枢神经系统八肽神经肽FF（NPFF）被认为在疼痛调节和阿片耐受中发挥作用。从人和大鼠中枢神经系统组织中分离出两种G蛋白偶联受体，NPFF1和NPFF2。NPFF特异性结合NPFF1（解离常数K(d)=1.13纳米）和NPFF2（解离常数K(d)=0.37纳米），并且在多种异源表达系统中，两种受体均被NPFF激活。这些受体的mRNA和结合位点在脊髓背角、下丘脑外侧、三叉神经脊束核和丘脑核中的定位支持了NPFF在疼痛调节中的作用。与NPFF1和NPFF2氨基酸序列同源性最高的受体中，有食欲素、神经肽Y和胆囊收缩素家族的成员，这些家族与进食有关。这些相似性以及厌食性Y1受体配体BIBP3226也与NPFF1结合这一发现表明NPFF1在进食中可能发挥作用。NPFF1和NPFF2的鉴定将有助于阐明它们在这些及其他生理功能中的作用。
