Cox H M, Pollock E L, Tough I R, Herzog H
Centre for Neuroscience, King's College London, GKT School of Biomedical Sciences, Guy's Campus, SE1 9RT, London, United Kingdom.
Peptides. 2001 Mar;22(3):445-52. doi: 10.1016/s0196-9781(01)00355-2.
A functional study has been performed to characterise the Y receptors responsible for NPY, PYY and PP-stimulated responses in mouse colonic mucosal preparations. Electrogenic ion secretion was stimulated with VIP following which NPY, PYY and PP analogues were, to varying degrees, inhibitory. PYY(3-36), hPP, Gln(23)hPP and rPP were effective but less potent than full length PYY, NPY or their Pro(34)-substituted analogues, while the Y(5) agonist Ala(31), Aib(32)hNPY was the least active peptide tested. The Y(1) antagonists, BIBP3226 and BIBO3304 virtually abolished Pro(34)PYY and PYY responses while PYY(3-36) responses were selectively inhibited by the Y(2) antagonist, BIIE0246. A combination of BIBO3304 and BIIE0246 also partially attenuated hPP responses, leaving residual effects that were most probably Y(4)-mediated. Thus we conclude that Y(1), Y(2) and Y(4) receptors attenuate ion secretion in mouse colon.
已进行了一项功能研究，以表征负责小鼠结肠黏膜制剂中NPY、PYY和PP刺激反应的Y受体。用VIP刺激电生性离子分泌，随后NPY、PYY和PP类似物在不同程度上具有抑制作用。PYY(3 - 36)、hPP、Gln(23)hPP和rPP有效，但效力低于全长PYY、NPY或其Pro(34)取代的类似物，而Y(5)激动剂Ala(31)、Aib(32)hNPY是所测试的活性最低的肽。Y(1)拮抗剂BIBP3226和BIBO3304几乎消除了Pro(34)PYY和PYY反应，而PYY(3 - 36)反应被Y(2)拮抗剂BIIE0246选择性抑制。BIBO3304和BIIE0246的组合也部分减弱了hPP反应，留下的残余效应很可能是由Y(4)介导的。因此，我们得出结论，Y(1)、Y(2)和Y(4)受体减弱小鼠结肠中的离子分泌。
