A 5-HT4 antagonist
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GR113808

Item No. 28733

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methyl ester
CAS Number
144625-51-4
Molecular Formula
C19H27N3O4S
Formula Weight
393.5
Purity
≥98%
Formulation (Request formulation change)
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMSO: 100 mMEthanol: 10 mM
λmax
216, 290 nm
SMILES
CN1C=C(C(OCC2CCN(CCNS(C)(=O)=O)CC2)=O)C3=CC=CC=C31
InChi Code
InChI=1S/C19H27N3O4S/c1-21-13-17(16-5-3-4-6-18(16)21)19(23)26-14-15-7-10-22(11-8-15)12-9-20-27(2,24)25/h3-6,13,15,20H,7-12,14H2,1-2H3
InChi Key
MOZPSIXKYJUTKI-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    5 mg

    $103

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    10 mg

    $161

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    25 mg

    $378

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    50 mg

    $702

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    Product Description

    GR113808 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT4.1 It binds to 5-HT4 receptors with an IC50 value of 0.4 nM in COS-7 cells expressing the human recombinant receptor and in guinea pig striatal membranes (IC50 = 0.5 nM).2 GR113808 is selective for 5-HT4 receptors over 5-HT1 receptors (Kis = >10 µM in dog saphenous vein and porcine vena cava), as well as 5-HT2 and 5-HT3 receptors (Kis = >10 and 1 μM in rabbit thoracic aorta and rat cerebral cortex, respectively).1 It is also selective for 5-HT4 over adenosine, adrenergic, dopamine, GABA, muscarinic, nicotinic, histamine, and NMDA receptors (Kis = >10 μM for all). GR113808 inhibits relaxation induced by 5-HT (Item No. 14332) in rat thoracic esophagus precontracted by carbachol (carbamoylcholine; Item No. 14486; pA2 = 9.3). In vivo, GR113808 inhibits 5-methoxytryptamine-induced tachycardia in anaesthetized piglets.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Gale, J.D., Grossman, C.J., Whitehead, J.W., et al. GR113808: A novel, selective antagonist with high affinity at the 5-HT4 receptor. Br. J. Pharmacol. 111(1), 332-338 (1994).

    2. Van den Wyngaert, I., Gommeren, W., Verhasselt, P., et al. Cloning and expression of a human serotonin 5-HT4 receptor cDNA. J. Neurochem. 69(5), 1810-1819 (1997).