colonic

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。

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。

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

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。

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

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.

DRAinh-A250 is a SLC26A3 inhibitor which blocks colonic fluid absorption and reduces constipation.

Urolithin D 是具有竞争性和选择性的 EphA 受体 的可逆性拮抗剂，是一种鞣花单宁结肠代谢物，抑制前列腺癌细胞中的 EphA2 磷酸化，可减弱脂肪细胞和肝细胞培养物中甘油三酯的积累，可用于研究代谢疾病。

Urocortin III (mouse) (free acid) 是一种选择性的 CRF2受体激动剂 (对 CRF2受体具有高亲和力)。Urocortin III (mouse) (free acid) 可显著抑制胃排空而不改变结肠运输。

α-CGRP (mouse, rat) TFA 是神经系统中的一种活性神经肽，位于神经肌肉接合部，具有显著的血管舒张功能。适用于心血管疾病、炎症、偏头痛及代谢研究领域。