colonic

Zamifenacin fumarate (UK-76654 fumarate) 是肠道选择性毒蕈碱M3受体的有效拮抗剂， 可显著降低肠易激综合症的结肠蠕动。

Lafutidine (FRG-8813) 是一种组胺受体 H2RA 拮抗剂，可抑制胃酸分泌，具有胃粘膜保护作用，可用于研究胃食管反流疾病。

Theaflavin digallate和乳酸一起可以减少单纯疱疹病毒的传播。

Dextran sulfate sodium salt (MW 36,000 - 50,000) 是一种中等分子量的聚阴离子葡聚糖衍生物，具有较强的肠上皮透过能力，是最常用的炎症性肠病（IBD）造模药物，可有效诱导急性和慢性结肠炎。Dextran sulfate sodium salt (MW 36,000 - 50,000)其机制可能涉及巨噬细胞功能失调和肠道菌群紊乱，具有结肠上皮毒性，故长期使用也可诱导结肠癌模型。

Trimebutine (Mebutin) 是阿片受体激动剂，有抗毒蕈碱活性。它是解痉剂，可调节肠道和结肠运动，并通过抗毒蕈碱和弱μ-阿片受体激动剂作用缓解腹痛。

Glycoursodeoxycholic acid (Ursodeoxycholylglycine) 是一种酰基甘氨酸和胆汁酸-甘氨酸缀合物，是熊去氧胆酸的代谢物。

Glycodeoxycholate Sodium 诱导肝细胞凋亡的机制与内切酶的DNA裂解有关。它是一种次级胆汁酸，由结肠环境中微生物菌群中存在的酶的作用产生。

A-1211212 (BCL2-IN-1) 是一种具有高效性和选择性的 Bcl-2 抑制剂，可促进淋巴细胞凋亡增加，改变小鼠的结肠粘膜并改善炎症。

Reutericyclin是一类口服活性良好的选择性抗革兰氏阳性菌物质，同时兼具抗菌与抗肥胖作用。Reutericyclin可通过特异性瓦解细菌跨膜电位，对艰难梭菌、金黄色葡萄球菌等致病菌产生非溶菌型的杀菌或抑菌效果，还可快速清除艰难梭菌繁殖体与芽孢结构。Reutericyclin 耐受酶解降解、具有铁离子螯合作用，且难以被结肠上皮吸收。除有效清除葡萄球菌生物膜、抑制耐药菌增殖外，Reutericyclin还可调节肠道菌群结构、改善机体能量代谢水平，以此改善利培酮用药引发的体重异常升高问题。现阶段，Reutericyclin已被广泛应用于艰难梭菌感染、药物诱导性体重增长及葡萄球菌浅表皮肤感染等方向的基础研究。

Balamapimod（又称 MKI-822）是一种小分子 Ras/Raf/MEK 抑制剂，可直接靶向异常激活的 MAPK 信号级联反应，用于抑制与肿瘤转化、炎症信号及病理性细胞增殖相关的异常蛋白激酶活性。通过通路水平的抑制作用，Balamapimod 在卒中、骨质疏松、类风湿性关节炎、多囊肾病、结肠息肉及其他炎症驱动型疾病中显示出明确的研究和治疗相关性。

Zamifenacin obviously decreases colonic motility in irritable bowel syndrome. Zamifenacin is an effective gut-selective muscarinic M3 receptor antagonist.

X-17 是一种强效的Vanin-1抑制剂，具有显著的抗炎和抗氧化活性。它能够抑制炎症因子的表达和髓过氧化物酶的活性，同时提高结肠中的谷胱甘肽储备，并恢复肠道屏障功能。

5-HT4R agonist-2 (Compound 4) 是一种选择性5-HT4R激动剂，EC50为0.41 nM。5-HT4R agonist-2 显著增强全肠和结肠的转运功能，增加粪便的排出量和水分，同时保持最低限度的全身吸收，具有用于慢性特发性便秘研究的潜力。

ATB-429 是一种具有释放 H2S 功能的美沙拉嗪衍生物，在肠易激综合征 (IBS) 模型中显示出显著的抗伤害和抗炎特性。通过释放硫化氢 (H2S)，该化合物能够调节健康和结肠炎后大鼠对结肠直肠扩张引发的超敏反应。ATB-429 减少了腹部戒断反应并抑制脊髓中 c-FosmRNA 的表达，可能有助于缓解胃肠道炎症相关的疼痛。此外，ATB-429 能下调结肠中环氧合酶-2 (COX-2) 和 IL-1β 的mRNA表达，而单一美沙拉嗪未表现出此效应。该作用机制与 ATP 敏感的 K+ (KATP) 通道有关，并可通过格列本脲逆转ATB-429 的作用证实。研究结果表明，ATB-429 在治疗与炎症相关的疼痛性肠道疾病时具备潜在的治疗优势。

Zinc picolinate 是一种锌补充剂，能够减轻结肠炎大鼠的结肠炎症并增强屏障功能，同时抑制子宫肌瘤的生长。

SKF38393 hydrobromide是SKF38393的盐形式。SKF38393是多巴胺D1受体激动剂，能够增加小鼠NAc中Shati/Nat8L mRNA的表达，在星形胶质细胞中增加了5-羟色胺和n -甲基- D -天冬氨酸诱导的运动相关破裂的频率；可以模拟多巴胺导致小鼠结肠运动的抑制；可促进蝗虫群居化

NSC61610是一种具有抗炎功效的分子，在体外以LANCL2和腺苷酸环化酶/cAMP依赖的方式激活过PPARγ，下调结肠炎症基因表达和促进调节性T细胞反应，改善实验性结肠炎。

Aloe emodin anthrone is a stimulant-laxative which has been shown to enhance colonic membrane permeability of water-soluble and poorly permeable compounds.

Aloe-emodin-glucoside is a stimulant-laxative which has been shown to enhance colonic membrane permeability of water-soluble and poorly permeable compounds.

Butyrylcholine is a novel colonic ion transport regulator produced by colonic epithelial cells that stimulates nicotine and muscarinic receptors.

MK-8970 is an acetal carbonate prodrug of raltegravir with enhanced colonic absorption.

STA 2 is an analogue of TXA2, a thromboxane receptor in the colonic epithelium.

(Ala13)-Apelin-13 acetate，一种 APJ 拮抗剂，可调节CRF 诱导的增强的结肠运动、内脏敏感性和肠屏障。

Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004). Urocortin II is a neuropeptide hormone and member of the corticotropin-releasing factor (CRF) family which includes mammalian CRF , urocortin , urocortin III , frog sauvagine, and piscine urotensin I.1 Mouse urocortin II shares 34 and 42% sequence homology with rat CRF and urocortin . It is expressed in mouse paraventricular, supraoptic, and arcuate nuclei of the hypothalamus, the locus coeruleus, and in motor nuclei of the brainstem and spinal ventral horn. Urocortin II selectively binds to CRF1 over CRF2 receptors (Kis = 0.66 and >100 nM, respectively) and induces cAMP production in CHO cells expressing CRF2 (EC50 = 0.14 nM). In vivo, urocortin II suppresses nighttime food intake by 35% in rats when administered intracerebroventricularly at a dose of 1 μg. Urocortin II (0.1 and 0.5 μg, i.c.v) stimulates fecal pellet output, increases distal colonic transit, and inhibits gastric emptying in mice.2 References1. Reyes, T.M., Lewis, K., Perrin, M.H., et al. Urocortin II: A member of the corticotropin-releasing factor (CRF) neuropeptide family that is selectively bound by type 2 CRF receptors. Proc. Natl. Acad. Sci. U.S.A. 98(5), 2843-2848 (2001).2. Martinez, V., Wang, L., Million, M., et al. Urocortins and the regulation of gastrointestinal motor function and visceral pain. Peptides 25(10), 1733-1744 (2004).