859502-43-5
Chemical Structure
GR125487 sulfamate
- CAS No.: 859502-43-5
- Formula:C19H29FN4O8S2
- Molecular Weight:524.58
IUPAC Name: (1-(2-(methylsulfonamido)ethyl)piperidin-4-yl)methyl 5-fluoro-2-methoxy-1H-indole-3-carboxylate sulfamate
InChIKey: VQJFDBXITIOGJM-UHFFFAOYSA-N
SMILES: O=C(C1=C(NC2=C1C=C(F)C=C2)OC)OCC3CCN(CC3)CCNS(=O)(C)=O.O=S(O)(N)=O
Biological Activity: GR125487 is a highly selective 5-HT4 receptor antagonist and acts as an inverse agonist at constitutively active 5-HT4 (a) receptors. GR125487 inhibits adenylyl cyclase/cAMP signaling by blocking the Gs-coupled 5-HT4 receptor. GR125487 is used in research on 5-HT4 receptor function, neuropsychiatric disorders, and gastrointestinal motility[1][2][3][4][5][6][7][8][9][10][11][12][13].
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GR125487 sulfamate | 97% | GR125487 is a highly selective 5-HT4 receptor antagonist and acts as an inverse agonist at constitutively active 5-HT4 (a) receptors. GR125487 inhibits adenylyl cyclase/cAMP signaling by blocking the Gs-coupled 5-HT4 receptor. GR125487 is used in research on 5-HT4 receptor function, neuropsychiatric disorders, and gastrointestinal motility. | ||||||||||||||||||||
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References
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- [2]. Claeysen S, et al. Pharmacological properties of 5-hydroxytryptamine4 receptor antagonists on constitutively active wild-type and mutated receptors. Mol Pharmacol. 2000;58(1):136-144.
- [3]. Kozono N, et al. Roles of the serotonin 5-HT4 receptor in dendrite formation of the rat hippocampal neurons in vitro. Brain Res. 2017;1655:114-121.
- [4]. Nirogi R, et al. Synthesis of GR 125487, a selective 5-HT4 receptor antagonist. Synthetic Communications. 2016;46(12):1036-1043.
- [5]. Letty S, et al. 5-HT4 receptors improve social olfactory memory in the rat. Neuropharmacology. 1997;36(4-5):681-7. [Content Brief]
- [6]. Marchetti-Gauthier E, et al. BIMU1 increases associative memory in rats by activating 5-HT4 receptors. Neuropharmacology. 1997;36(4-5):697-706.
- [7]. Crema F, et al. Intestinal prokinesia by two esters of 4-amino-5-chloro-2-methoxybenzoic acid: involvement of 5-hydroxytryptamine-4 receptors and dissociation from cardiac effects in vivo. J Pharmacol Exp Ther. 1999;288(3):1045-1052.
- [8]. Horikoshi K, et al. Possible involvement of 5-HT4 receptors, in addition to 5-HT3 receptors, in the emesis induced by high-dose cisplatin in Suncus murinus. Japanese journal of pharmacology. 2001 Jan;85(1):70-4.
- [9]. Kamei J, et al. Effect of chronic pain on morphine-induced respiratory depression in mice. Neuroscience. 2011;174:224-233.
- [10]. Mendez-David I, et al. Rapid anxiolytic effects of a 5-HT₄ receptor agonist are mediated by a neurogenesis-independent mechanism. Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology. 2014 May;39(6):1366-78.
- [11]. Hasebe S, et al. Pharmacological profile of encounter-induced hyperactivity in isolation-reared mice. Behavioural pharmacology. 2015 Oct;26(7 Spec No):681-90.
- [12]. Cui C, et al. 5-HT4 Receptor is Protective for MPTP-induced Parkinson's Disease Mice Via Altering Gastrointestinal Motility or Gut Microbiota. Journal of neuroimmune pharmacology : the official journal of the Society on NeuroImmune Pharmacology. 2023 Dec;18(4):610-627.
- [13]. Farrell EK, et al. Vanillin suppresses seizure-induced mortality in the DBA/1 mouse model of SUDEP. Neuroscience letters. 2026 Apr 26;877:138575.
