GR 113808 |
Catalog No.GC11624
One-Click Copy Product Info
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GR 113808 is a potent and selective 5-HT4 receptor antagonist with a pKb of 8.8.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 144625-51-4
Sample solution is provided at 25 µL, 10mM.
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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.
| Animal experiment [1]: | |
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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 |
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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. |
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Dosage form |
1mg/kg; 5-7 days; enema |
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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. |
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References: |
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| Cas No. | 144625-51-4 | SDF | |
| Chemical Name | (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 | ||
| Formula | C19H27N3O4S | M.Wt | 393.5 |
| Solubility | DMSO: 100 mM,Ethanol: 10 mM | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.5413 mL | 12.7065 mL | 25.413 mL |
| 5 mM | 508.3 μL | 2.5413 mL | 5.0826 mL |
| 10 mM | 254.1 μL | 1.2706 mL | 2.5413 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 12 reference(s) in Google Scholar.)