GLPBio

GR 113808

Catalog No.: GC11624Purity:>98.00%
COASDSData Sheet
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.

GR 113808
Cas No.: 144625-51-4
1mgIn Stock
$41.00
1
5mgIn Stock
$90.00
1
10mgIn Stock
$149.00
1
25mgIn Stock
$317.00
1
50mgIn Stock
$515.00
1
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Description

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.

Protocol

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:
[1]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.

Product Documents

Purity:>98.00%Appearance:A solid
COASDSData Sheet

Chemical Properties

CAS No.
144625-51-4
Chemical Name
(1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 1-methyl-1H-indole-3-carboxylate
SMILES
O=C(C1=CN(C)C2=CC=CC=C12)OCC3CCN(CCNS(=O)(C)=O)CC3
Molecular Formula
C19H27N3O4S
Molecular Weight
393.5
Solubility
DMSO: 100 mM,Ethanol: 10 mM
Storage
Store at -20°C
General tips
Select a suitable solvent according to the product solubility data. Once prepared, aliquot the stock solution to avoid repeated freeze-thaw cycles.
Use stock solutions within 6 months when stored at -80°C or within 1 month when stored at -20°C.
To improve solubility, warm the tube to 37°C and sonicate it for an appropriate period.
Shipping Condition
Evaluation samples are shipped with blue ice. Other available sizes are shipped at room temperature or with blue ice upon request.

CalculatorsMolarity / Dilution / Molecular Weight / Unit Conversion / In Vivo Formulation / Solubility

g/mol

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