GR 113808

structure given in first source; a 5-HT(4) receptor antagonist: GR 125487 is the HCl salt

Also Known As:

(1-(2-(methylsulfonylamino)ethyl)-4-piperidinyl)methyl 1-methyl-1H-indole-3-carboxylate; GR 125487; GR-113808; GR113808; 1H-Indole-3-carboxylic acid, 1-methyl-, (1-(2-((methylsulfonyl)amino)ethyl)-4-piperidinyl)methyl ester

Networked: 15 relevant articles (0 outcomes, 2 trials/studies)

Bio-Agent Context: Research Results

Experts

1.	Bianco, Francesca: 1 article (11/2016)
2.	Bonora, Elena: 1 article (11/2016)
3.	De Giorgio, Roberto: 1 article (11/2016)
4.	Dicay, Michael: 1 article (11/2016)
5.	Keenan, Catherine M: 1 article (11/2016)
6.	Lavoie, Brigitte: 1 article (11/2016)
7.	Linton, Alisha A: 1 article (11/2016)
8.	MacNaughton, Wallace K: 1 article (11/2016)
9.	Mawe, Gary M: 1 article (11/2016)
10.	O'Neill, Conor H: 1 article (11/2016)

Related Diseases

1.	Alzheimer Disease (Alzheimer's Disease) 07/01/2003 - "[3H]GR113808 binding to serotonin 5-HT(4) receptors in the postmortem neocortex of Alzheimer disease: a clinicopathological study." 03/01/1995 - "In these studies, the affinities of GR 113808 were not significantly different.4. The density of 5-HT4 receptors selected from regions of post mortem brains of patients with Parkinson's disease, Huntington's disease and Alzheimer's disease were compared to age-matched controls. "
2.	Parkinson Disease (Parkinson's Disease) 03/01/1995 - "In these studies, the affinities of GR 113808 were not significantly different.4. The density of 5-HT4 receptors selected from regions of post mortem brains of patients with Parkinson's disease, Huntington's disease and Alzheimer's disease were compared to age-matched controls. "
3.	Huntington Disease (Huntington's Disease) 03/01/1995 - "In these studies, the affinities of GR 113808 were not significantly different.4. The density of 5-HT4 receptors selected from regions of post mortem brains of patients with Parkinson's disease, Huntington's disease and Alzheimer's disease were compared to age-matched controls. "
4.	Hyperalgesia 03/01/2011 - "In contrast, ipsilateral peripheral pretreatment with the selective 5-HT(4) (GR-125487, 1-100nmol/paw), 5-HT(6) (SB-258585, 0.00001-0.001nmol/paw), and 5-HT(7) (SB-269970, 0.1-10nmol/paw) receptor antagonists significantly prevented formalin-induced secondary allodynia and hyperalgesia in both paws. " 05/15/2013 - "Microinjection of selective 5-HT1A, 5-HT2, 5-HT3, 5-HT4, 5-HT5A, 5-HT6 and 5-HT7 receptor antagonists, 1-(2-methoxyphenyl)-4-[4-(2-phthalimido)butyl] piperazine hydrobromide (NAN-190) (10μg), cyproheptadine (50ng), granisetron hydrochloride (granisetron) (10μg), 1-[2-[(methylsulfonyl)-amino]ethyl]-4-piperidinyl]methyl1-methyl-1H-indole-3-carboxylate (GR113808) (5μg), SB699551 dihydrochloride (SB699551) (10μg), SB258585 dihydrochloride (SB258585) (2μg) or SB269970 hydrochloride (SB269970) (10μg) into the VLO 5-min prior to 5-HT (10μg) injection, all antagonized the 5-HT-induced inhibition of allodynia. "
5.	Colitis 12/01/2023 - "GR113808 treatment diminished the protective effect of EA at sensitized acupoints in colitis rats (P<0.05). " 11/01/2016 - "Daily administration of tegaserod increased motility in inflamed colons of guinea pigs and mice, whereas administration of GR113808 disrupted motility in animals without colitis. " 11/01/2016 - "The 5-HT4R agonist tegaserod (1 mg/kg), the 5-HT4R antagonist GR113808 (1 mg/kg), or vehicle (control) were delivered by enema to wild-type or 5-HT4R knockout mice at the onset of, or during, active colitis, induced by administration of dextran sodium sulfate or trinitrobenzene sulfonic acid. "

Related Drugs and Biologics

1.	Serotonin (5 Hydroxytryptamine)
2.	Serotonin 5-HT4 Receptor Antagonists
3.	5-HT4 Serotonin Receptors
4.	SB 258585
5.	indole
6.	Serotonin Plasma Membrane Transport Proteins (Serotonin Transporter)
7.	15-Hydroxy-11 alpha,9 alpha-(epoxymethano)prosta-5,13-dienoic Acid
8.	Granisetron (Kytril)
9.	8-Hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT)
10.	Ondansetron (Zofran)

Related Therapies and Procedures

1.	Acupuncture Points (Acupuncture Point)
2.	Injections
3.	Enema (Enemas)