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。

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。

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).

Succinic acid sodium 是一种口服具有活力的抗焦虑剂。Succinic acid sodium 能够下调 KCNMB1 (钾通道亚基 β1) 和TET1(10-11 易位 1) 的表达。Succinic acid sodium 可抑制体内的结肠上皮细胞的增殖。Succinic acid sodium 能够用于研究妊娠期高血压。

Wnt signaling is required for direct multiple biological processes and also plays key roles in the pathogenesis of various diseases. Cyclic AMP response element-binding protein (CREB) is a transcription factor that is a member of the leucine zipper family of DNA binding proteins. This protein binds as a homodimer to the cAMP-responsive element, an octameric palindrome. The protein is phosphorylated by several protein kinases, and induces transcription of genes in response to hormonal stimulation of the cAMP pathway. Via generating a transcriptionally active complex with β-catenin, CREB acts as a mediator of Wnt signaling.ICG-001 is an inhibitor of β-catenin/CREB mediated transcription. The direct cellular target of ICG-001 is CREB. the inhibitory IC50of ICG-001 against β-catenin/CREB mediated transcription was 3 μM. ICG-001 treatment at the concentration of 25 μM for 24h significantly increased caspase activity in both colon cancer cell lines SW480 and HCT116 cell lines but not in normal colonic epithelial cells CCD-841Co. In a cell growth inhibition assay, the IC50s of ICG-001 against SW480 and HCT116 cells were 4.43 μM and 5.95 μM, respectively.In a SW620 nude mouse xenograft model, an water-soluble analog of ICG-001 given at the dose of 150 mg/kg i.v. once in every 2 days dramatically suppressed tumor growth. In a bleomycin-induced pulmonary fibrosis mice model, ICG-001 given at the dose of 5 mg/kg per day reversed pulmonary fibrosis. In a rat myocardial infarction model, ICG-001 was administrated subcutaneously at the dose of 50 mg/kg/day for 10 days which significantly improved cardiac contractile function after myocardial infarction in the rats.

Ciclotropium (free base) is quaternary ammonium compound with anticholinergic and parasympatholytic activity. Oral Cyclotropium bromide inhibited fasting and meal-stimulated colonic motility significantly without causing adverse side effects. After cyclotropium bromide, there was a significant correlation between antral contraction amplitude and gastric emptying.