Hyland Niall P, Cox Helen M
Wolfson Centre for Age-Related Diseases, King's College London.
Br J Pharmacol. 2005 Nov;146(5):712-22. doi: 10.1038/sj.bjp.0706368.
1 Neuropeptide Y (NPY) is a prominent enteric neuropeptide with prolonged antisecretory effects in mammalian intestine. Veratridine depolarises neurons consequently causing epithelial anion secretion across mouse colon mucosa. Our aim was to characterise functionally, veratridine-stimulated mucosal responses and to determine the roles for NPY, Y(1), and Y(2) receptors in modulating these neurogenic effects. 2 Colon mucosae (with intact submucous innervation) from wild-type mice (+/+) and knockouts lacking either NPY (NPY-/-), Y(1)-/- or Y(2)-/- were placed in Ussing chambers and voltage clamped at 0 mV. Veratridine-stimulated short-circuit current (I(sc)) responses in +/+, Y(1) or Y(2) antagonist pretreated +/+ colon, Y(1)-/- and NPY-/- colon were insensitive to cholinergic blockade by atropine (At; 1 microM) and hexamethonium (Hex; 10 microM). Tetrodotoxin (TTX, 100 nM) abolished veratridine responses, but had no effect upon carbachol (CCh) or vasoactive intestinal polypeptide (VIP)-induced secretory responses. 3 To establish the functional roles for Y(1) and Y(2) receptors, +/+ tissues were pretreated with either the Y(1) or Y(2) receptor antagonist (BIBO3304 (300 nM) or BIIE0246 (1 microM), respectively) and veratridine responses were compared with those from Y(1)-/- or Y(2)-/- colon. Neither BIBO3304 nor Y(1)-/- altered veratridine-induced secretion, but Y(1) agonist responses were abolished in both preparations. In contrast, the Y(2) antagonist BIIE0246 significantly amplified veratridine responses in +/+ mucosa. Unexpectedly, NPY-/- colon exhibited significantly attenuated veratridine responses (between 1 and 5 min). 4 We demonstrate that electrogenic veratridine responses in mouse colon are noncholinergic and that NPY can act directly upon epithelia, a Y(1) receptor effect. The enhanced veratridine response observed in +/+ tissue following BIIE0246, indicates that Y(2) receptors are located on submucosal neurons and that their activation by NPY will inhibit enteric noncholinergic secretory neurotransmission. 5 We also demonstrate Y(1) and Y(2) receptor-mediated antisecretory tone in +/+ colon and show selective loss of each in Y(1) and Y(2) null colon respectively. In NPY-/- tissue, only Y(1)-mediated tone was present, this presumably being mediated by endogenous endocrine peptide YY. Y(2) tone was absent from NPY-/- (and Y(2)-/-) colon and we conclude that NPY activation of neuronal Y(2) receptors attenuates secretory neurotransmission thereby providing an absorptive electrolyte tone in isolated colon.
1 神经肽Y(NPY)是一种重要的肠神经肽,在哺乳动物肠道中具有持久的抗分泌作用。藜芦碱使神经元去极化,从而导致小鼠结肠黏膜上皮阴离子分泌。我们的目的是从功能上表征藜芦碱刺激的黏膜反应,并确定NPY、Y(1)和Y(2)受体在调节这些神经源性效应中的作用。2 将来自野生型小鼠(+/+)以及缺乏NPY(NPY-/-)、Y(1)-/-或Y(2)-/-的基因敲除小鼠的结肠黏膜(具有完整的黏膜下神经支配)置于Ussing槽中,并在0 mV下进行电压钳制。在+/+、用Y(1)或Y(2)拮抗剂预处理的+/+结肠、Y(1)-/-和NPY-/-结肠中,藜芦碱刺激的短路电流(I(sc))反应对阿托品(At;1 microM)和六甲铵(Hex;10 microM)的胆碱能阻断不敏感。河豚毒素(TTX,100 nM)消除了藜芦碱反应,但对卡巴胆碱(CCh)或血管活性肠肽(VIP)诱导的分泌反应没有影响。3 为了确定Y(1)和Y(2)受体的功能作用,分别用Y(1)或Y(2)受体拮抗剂(BIBO3304(300 nM)或BIIE0246(1 microM))预处理+/+组织,并将藜芦碱反应与来自Y(1)-/-或Y(2)-/-结肠的反应进行比较。BIBO3304和Y(1)-/-均未改变藜芦碱诱导的分泌,但两种制剂中Y(1)激动剂反应均被消除。相反,Y(2)拮抗剂BIIE0246显著增强了+/+黏膜中的藜芦碱反应。出乎意料的是,NPY-/-结肠中藜芦碱反应在1至5分钟之间显著减弱。4 我们证明小鼠结肠中的电源性藜芦碱反应是非胆碱能的,并且NPY可以直接作用于上皮细胞,这是一种Y(1)受体效应。在BIIE0246处理后的+/+组织中观察到的增强的藜芦碱反应表明,Y(2)受体位于黏膜下神经元上,并且NPY对它们的激活将抑制肠非胆碱能分泌性神经传递。5 我们还证明了+/+结肠中Y(1)和Y(2)受体介导的抗分泌张力,并分别显示了Y(1)和Y(2)基因敲除结肠中各自抗分泌张力的选择性丧失。在NPY-/-组织中,仅存在Y(1)介导的张力,这可能由内源性内分泌肽YY介导。NPY-/-(和Y(2)-/-)结肠中不存在Y(2)张力,我们得出结论,神经元Y(2)受体的NPY激活减弱了分泌性神经传递,从而在离体结肠中提供了一种吸收性电解质张力。