GR 113808 | 5-HT Receptors | Potent, Selective 5-HT4 Antagonist | GR113808

Category:

Cat.No.	Product Name
1322	GR 113808

Price and Availability

Click here for full price details of
GR 113808

Other Information:

Sold with the permission of GlaxoSmithKline

Chemical Name: 1-methyl-1H-indole-3-carboxylic acid, [1-[2-[(methylsulfonyl)amino]ethyl]-4-piperidinyl]methy l ester

Biological Activity:

Potent, selective 5-HT₄ receptor antagonist (pK_B = 9.43 in human colonic muscle, and K_d = 0.15 nM for binding to cloned human 5-HT₄ receptors). Displays > 300-fold selectivity over 5-HT_1A, 5-HT_1B, 5-HT_2A, 5-HT_2C and 5-HT₃ receptors.

Technical Data:

M.Wt:	393.5
Formula:	C₁₉H₂₇N₃O₄S
Storage:	Store at RT
Solubility:	Soluble to 12 mM in DMSO and to 25 mM in 1eq. HCl
Purity:	>98%
CAS No:	[144625-51-4]

Resources:

Certificate of Analysis / MSDS:

Certificate of Analysis: View current batch

For specific/earlier batch please select:

Product/Material Safety Data Sheet: View current batch

For specific/earlier batch please select:

References:

Gale et al (1994) GR113808: a novel, selective antagonist with high affinity at the 5-HT₄ receptor. Br.J.Pharmacol. 111 332. Eglen et al (1995) Central 5-HT₄ receptors. TiPS 16 391. Van den Wyngaert et al (1997) Cloning and expression of a human serotonin 5-HT₄ receptor cDNA. J.Neurochem. 69 1810. Prins et al (2000) An improved in vitro bioassay for the study of 5-HT₄ receptors in the human isolated large intestinal circular muscle. Br.J.Pharmacol. 129 1601.

View related products by Pharmacological Action or by Research Area

Keywords: GR 113808, 5-HT Receptors, Potent, Selective 5-HT4 Antagonist, GR113808, Tocris Bioscience

Literature in this Area

Scientific Reviews

5-HT Receptors & their Ligands
Download PDF

Featured New Product

Dual 5-HT/noradrenalin reuptake inhibitor

2917 Venlafaxine

Dual serotonin / noradrenaline reuptake inhibitor that displays ~ 30-fold higher affinity for SERT than NET (K_i values are 82 and 2480 nM respectively). Anti-depressant; increases swimming and climbing behaviour in the forced-swim test in rats.

View all Featured New Products

New Products in this Area

	2643	DOI hydrochloride
	Mixed 5-HT_2A/2C agonist
	2901	SB 242084
	Selective 5-HT_2C antagonist; brain penetrant
	2925	LP 12 hydrochloride
	5-HT₇ agonist
	2726	SB 258719 hydrochloride
	Selective 5-HT₇ antagonist
	2739	U 92016A
	Selective 5-HT_1A agonist
	2865	Risperidone
	5-HT_2A antagonist
	2746	Amperozide hydrochloride
	Atypical antipsychotic; high affinity 5-HT₂ ligand
	2844	Mosapride citrate
	5-HT₄ agonist and 5-HT₃ antagonist
	2777	Nefazodone hydrochloride
	5-HT_2A antagonist and 5-HT uptake inhibitor. Antidepressant
	2645	Fananserin
	5-HT_2A antagonist. Also D₄ antagonist
	2592	TCB-2
	Potent, high affinity 5-HT_2A agonist
	2495	Melperone hydrochloride
	5-HT_2A/D₂ receptor antagonist; neuroleptic
	2451	LY 344864 hydrochloride
	Potent, selective 5-HT_1F agonist
	2534	LP 44
	High affinity 5-HT₇ agonist

for new product e-alerts

User ID
Password