GR 113808
目录号 : GC11624GR 113808是一种有效和选择性的5-HT4受体拮抗剂，pKb=8.8。
Cas No.:144625-51-4
Sample solution is provided at 25 µL, 10mM.
;)
,-1-7$$$37316672.jpg');)
;)
;)
$$$36806353.jpg');)
;33(7)%EF%BC%9A546-561$$$37156877.jpg');)
;)
;)
;)
%201124-1138.$$$35908550.jpg');)
%20766-780.$$$37100057.jpg');)
%20418-432.$$$36893736.jpg');)
%EF%BC%9A-240-255.$$$35108512.jpg');)
533-545$$$36543525.jpg');)
%201-13.$$$36600053.jpg');)
;)
GR 113808 is a potent and selective 5-HT4 receptor antagonist with a pKb of 8.8[1]. GR 113808 can be used in the study of gastrointestinal motility disorders, neurological diseases and tumors[2, 3]. GR 113808 can attenuate morphine-stimulated dopamine release in the striatum of rats[4].
In vivo, GR 113808 (1mg/kg) treated with colitis mice by enema for 5-7 days reversed the significant improvement of Tegaserod on clinical and histological damage to the colon[5]. GR 113808 (16μg) treated with dorsal hippocampal (dHIP) injection in rats with medial forebrain bundle (MFB) lesions increased dopamine levels in the striatum, medial prefrontal cortex (mPFC), lateral habenula (LHb) and ventral hippocampus (vHIP), and increased serotonin (5-HT) levels in the LHb[6].
References:
[1] Kaumann A J. Blockade of human atrial 5-HT4 receptors by GR 113808[J]. British journal of pharmacology, 1993, 110(3): 1172.
[2] Kato S, Fujiwara I, Yoshida N. Nitrogen‐containing heteroalicycles with serotonin receptor binding affinity: Development of gastroprokinetic and antiemetic agents[J]. Medicinal research reviews, 1999, 19(1): 25-73.
[3] Guillemot J, Compagnon P, Cartier D, et al. Metoclopramide stimulates catecholamine-and granin-derived peptide secretion from pheochromocytoma cells through activation of serotonin type 4 (5-HT4) receptors[J]. Endocrine-Related Cancer, 2009, 16(1): 281.
[4] Pozzi L, Trabace L, Invernizzi R, et al. Intranigral GR-113808, a selective 5-HT4 receptor antagonist, attenuates morphine-stimulated dopamine release in the rat striatum[J]. Brain research, 1995, 692(1-2): 265-268.
[5] Spohn S N, Bianco F, Scott R B, et al. Protective actions of epithelial 5-hydroxytryptamine 4 receptors in normal and inflamed colon[J]. Gastroenterology, 2016, 151(5): 933-944. e3.
[6] Wang J W, Gao F, Wang Z L, et al. Activation and blockade of dorsal hippocampal serotonin4 receptors produce antidepressant effects in the hemiparkinsonian rats[J]. Brain Research, 2021, 1761: 147426.
GR 113808是一种有效和选择性的5-HT4受体拮抗剂，pKb=8.8[1]。GR 113808能够用于胃肠动力障碍、神经系统疾病及肿瘤研究[2, 3]。GR 113808能够减弱吗啡刺激的大鼠纹状体中多巴胺的释放[4]。
在体内，GR 113808（1mg/kg）通过灌肠治疗结肠炎小鼠5-7天，逆转了Tegaserod对结肠临床和组织学损伤的显著改善效果[5]。GR 113808（16μg）通过背侧海马体（dHIP）注射治疗内侧前脑束（MFB）病变大鼠，增加了纹状体、内侧前额皮质（mPFC）、外侧缰核（LHb）和腹侧海马（vHIP）中的多巴胺水平，并增加了LHb中的5-羟色胺（5-HT）水平[6]。
| Animal experiment [1]: | |
Animal models | Male CD-1 IGS mice、male and female 5-HT4-receptor knockout mice and their littermates on an SV129 background、male Hartley guinea pigs |
Preparation Method | Enemas with either vehicle (1% dimethyl sulfoxide in 0.9% saline, 0.2mL/mouse) or drug (tegaserod; GR 113808; both delivered at 1mg/kg) were administered daily for 5-7 days starting 24h after induction of colitis. Inflammation was measured using the colitis disease activity index and by histologic analysis of intestinal tissues. Epithelial proliferation, wound healing, and resistance to oxidative stress-induced apoptosis were assessed, as was colonic motility. |
Dosage form | 1mg/kg; 5-7 days; enema |
Applications | In DSS-inflamed mice, treatment with tegaserod (1mg/kg), beginning 24h after DSS was introduced, significantly reduced the clinical and the histologic damage of the colon compared with vehicle-treated DSS inflamed animals. The protective effects of tegaserod were blocked by the 5-HT4 antagonist GR 113808. |
References: | |
| Cas No. | 144625-51-4 | SDF | |
| 化学名 | (1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate | ||
| Canonical SMILES | O=C(C1=CN(C)C2=CC=CC=C12)OCC3CCN(CCNS(=O)(C)=O)CC3 | ||
| 分子式 | C19H27N3O4S | 分子量 | 393.5 |
| 溶解度 | DMSO: 100 mM,Ethanol: 10 mM | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
||
| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
 |
1 mg | 5 mg | 10 mg |
| 1 mM | 2.5413 mL | 12.7065 mL | 25.413 mL |
| 5 mM | 0.5083 mL | 2.5413 mL | 5.0826 mL |
| 10 mM | 0.2541 mL | 1.2706 mL | 2.5413 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet