GR 113808 |
Catalog No.GC11624
One-Click Copy Product Info
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GR 113808 es un antagonista potente y selectivo del receptor 5-HT4 con un pKb de 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 es un antagonista potente y selectivo del receptor 5-HT4 con un pKb de 8.8[1]. GR 113808 se puede utilizar en el estudio de trastornos de la motilidad gastrointestinal, enfermedades neurológicas y tumores [2, 3]. GR 113808 puede atenuar la liberación de dopamina estimulada por morfina en el cuerpo estriado de las ratas [4].
In vivo, GR 113808 (1mg/kg) tratado con ratones de colitis por enema durante 5-7 días revirtió la mejora significativa de Tegaserod en el daño clínico e histológico al colon [5]. GR 113808 (16μg) tratado con inyección del hipocampo dorsal (dHIP) en ratas con lesiones del haz del prosencéfalo medial (MFB) aumentó los niveles de dopamina en el cuerpo estriado, la corteza prefronatal medial (mPFC), la habenula lateral (LHb) y el hipocampo ventral (vHIP), y aumentó los niveles de serotonin (5-HT) en el 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.
| Experimentos con animales [1]: | |
Modelos animales | Ratones CD-1 IGSmacho, ratones macho y hembra knockout del receptor 5-HT4 y sus compañeros de camada sobre un fondo SV129, conejillos de indias Hartley machos |
Método de preparación | Los enemas con cualquier vehículo (1% de dimethyl sulfoxide en solución 0.9% salina, 0.2mL/ratón) o medicamento (tegaserod; GR 113808; ambos entregados a 1mg/kg) se administraron diariamente durante 5-7 días a partir de 24h después de la inducción de la colitis. La ioinflamación se midió utilizando el índice de actividad de la enfermedad de la colitis y mediante el análisis histológico de los tejidos intestinales. Se evaluó la proliferación epitelial, la curación de heridas y la resistencia a la apoptosis inducida por el estrés oxidativo, al ilo que la motilidad colónica. |
Forma de dosificación | 1mg/kg; 5-7 días; enema |
Áreas de aplicación | En ratones inflamados con DSS, el tratamiento con tegaserod (1mg/kg), que comenzó 24h después de que se introdujera el DSS, redujo significativamente el daño clínico e histológico del colon en comparación con los animales inflamados con DSS tratados con vehículos. Los efectos protectores del tegaserod fueron bloqueados por el antagonista 5-HT4 GR 113808. |
References: | |
| 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)
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μL
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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.)