gastric emptying

Acotiamide monohydrochloride trihydrate (Z-338 HCl) 是一种首创的、具有口服活性的胃肠动力药。它通过促毒蕈碱受体拮抗作用和乙酰胆碱酯酶(AChE)抑制作用增强肠神经元释放的乙酰胆碱，从而增强胃排空和胃部适应性，有潜力用于功能性消化不良的研究。

Ecabapide (DQ-2511) 是一种新型促胃肠蠕动剂，能显著增强SHRSP的胃排空能力。Ecabapide 可激活的兔胃壁细胞中的环状 GMP 依赖性管家 Cl- 通道。

Relamorelin(BIM28131, RM131) 是一种具有选择性和有效性的生长素释放肽 生长激素促分泌素受体 (GHSR) 激动剂，对 GHS-1a 受体具有很高的亲和力（Ki值为0.42 ± 0.063 nM）。Relamorelin(BIM28131, RM131) 也是一种具有中枢渗透性的五肽类似物，可增加生长激素水平，加速胃排空，具有研究恶病质的潜力。

Mifentidine (DA 4577) 是一种可口服的 H2 受体拮抗剂，可用于研究胃排空和实验性胃和十二指肠溃疡。

Cisapride (R 51619) 是一种5-HT4受体激动剂，还是 hERG 抑制剂。它可作用于肠道中的血清素受体，促进肠道蠕动，增加胃排空并减少食管反流。

Methyl syringate (Syringic Acid Methyl Ester) 是水仙花蜜的化学标记物，是有效的细菌和真菌漆酶酚介质。它也是TRPA1激动剂。

AZD7687 is a potent and selective DGAT1 inhibitor with an IC50 value of 80 nM (hDGAT1). IC50 value: 80 nM [1] Target: DGAT1 in vitro: Plasma AZD7687 exposure was measured repeatedly. AZD7687 markedly reduced postprandial TAG excursion with a steep concent

Semaglutide是一种类glucagon-like peptide-1 (GLP-1)受体激动剂。该化合物通过模仿胰高血糖素样肽-1降低血糖水平。它还能促进胰岛β细胞的生长，这些细胞负责胰岛素的生产和释放。此外，Semaglutide抑制胰高血糖素的产生，该激素增加糖原分解（肝脏储存的碳水化合物的释放）和糖异生（新葡萄糖的合成）。通过降低食欲和减缓胃部消化过程，它还能减少食物摄入，从而帮助减少体内脂肪。

Cinitapride (Blaston) 是一种促胃药。它减缓肌肉的活动，以减轻诸如胃酸反流、胃排空延迟和溃疡性消化不良等病症的症状。 Cinitapride 作为 5-HT2 受体的拮抗剂和 5-HT1 和 5-HT4 受体的激动剂。

Acotiamide 是一种具有口服活性、选择性和可逆性的乙酰胆酶碱酯 (AChE) 抑制剂，IC50值为1.79 μM。Acotiamide 是一种胃促动力剂，可增强胃收缩性并加速胃排空延迟。Acotiamide 可用于胃动力障碍的功能性消化不良及肠道炎症的研究。

HMR-1426 is gastric emptying inhibitor. HMR1426 shows an anorectic potential in rats and decreased body weight and fat mass. This was achieved solely by reducing food intake without influencing overall energy expenditure or behavior.

Dazopride fumarate is a peristaltic used to enhance gastric emptying and block emesis.

Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)

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).

Relamorelin (RM-131) acetate is a pentapeptide ghrelin analog that acts as a selective agonist for the ghrelin growth hormone secretagogue receptor (GHSR). It exhibits a high affinity for the GHS-1a receptor, with a Ki value of 0.42 nM. Notably, Relamorelin acetate can cross the blood-brain barrier and target the central nervous system. This compound effectively increases growth hormone levels and promotes faster gastric emptying. Due to these properties, Relamorelin acetate holds promise for its potential applications in research related to cachexia, gastroparesis, and gastric intestinal dysmobility disorders [4] [5].

Escin IB 是一种皂苷，分离自马栗子种子的皮和胚乳中，能够抑制 pancreatic lipase 的活性。

Corydaline (Corydalin) 是从 Corydalis yanhusuo 提取的一种异喹啉生物碱，是一种新型促动力植物药的主要活性成分之一。它促进胃排空和小肠转运，促进胃的调节，具有抗乙酰胆碱酯酶、抗过敏和镇痛活性。

Acotiamide hydrochloride 是选择性的、口服具有活力的、可逆的乙酰胆酶碱酯 (AChE) 抑制剂 (IC50: 1.79 μM)，能够提高胃收缩性，加速胃排空延迟，能够用于研究胃动力障碍的功能性消化不良及肠道炎症。

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.

ADL 08-0011 is an active metabolite of the μ-opioid receptor antagonist alvimopan. It is produced from alvimopan via amide hydrolysis by gut microbiota. ADL 08-0011 is a μ-opioid receptor antagonist (Ki = 0.25 nM). It is selective for μ-opioid receptors over κ- and δ-opioid receptors (Kis = 15.8 and 31.6 nM, respectively). ADL 08-0011 inhibits endomorphin 1-induced inhibition of electrically induced contraction of isolated guinea pig ileum (pA2 = 9.4). In vivo, ADL 08-0011 (0.03-1 mg kg) reverses loperamide-induced delayed gastric emptying in a rat model of castor oil-induced diarrhea.

Relamorelin (RM-131) TFA，一种生长素类似物，是一种选择性的生长素释放肽 生长激素促分泌素受体 (GHSR) 激动剂，对GHS-1a 受体的Ki 值为 0.42 nM。Relamorelin TFA 是一种五肽，具有中枢渗透性。Relamorelin TFA 增加生长激素水平，加速胃排空，具有用于恶病质、胃轻瘫和胃 肠运动障碍研究的潜力。

Amylin, amide, human TFA 是一种含有37个氨基酸的胰腺多肽，与胰岛素共同分泌，对代谢和维持葡萄糖稳态具有重要作用。该化合物能够抑制胰高血糖素的分泌，延缓胃排空速度，同时作为增加饱腹感的因子。

Stresscopin-related peptide (human) 是 2 型 CRH 受体的特异性配体。Stresscopin-related peptide (human) 抑制食物摄入，延迟胃排空，并减少热引起的水肿。Stresscopin-related peptide (human) 在应激后维持体内平衡，可用于应激相关疾病的研究。

Beinaglutide 是一种重组人 GLP-1(rhGLP-1) 多肽，与人 GLP-1(7-36) 具有几乎 100% 的同源性。Beinaglutide 在血糖控制、抑制食物摄入和胃排空和促进体重减轻方面表现出依赖于剂量的作用。Beinaglutide 具有研究超重 肥胖和非酒精性脂肪性肝炎 (NASH) 的潜力。