932373-86-9
Chemical Structure
GSK1034702 hydrochloride
- CAS No.: 932373-86-9
- Formula:C18H25ClFN3O2
- Molecular Weight:369.86
InChIKey: FDACQSJDRGVKFF-UHFFFAOYSA-N
SMILES: O=C1NC2=C(C=C(C)C=C2N1C3CCN(C4CCOCC4)CC3)F.Cl
Biological Activity: GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions)[1][2].
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GSK1034702 hydrochloride | GSK1034702 hydrochloride is an orally active and allosteric agonist of M1 mAChR (pEC50=8.1) that can cross the blood-brain barrier. GSK1034702 hydrochloride activates the Gq/11 protein-mediated signaling pathway, enhancing neuronal firing and long-term potentiation (LTP) in the CA1 region of the hippocampus. GSK1034702 hydrochloride can modulate hippocampal function, improve memory encoding in the nicotine withdrawal cognitive dysfunction model, and show pro-cognitive effects in rodents. GSK1034702 hydrochloride can be used for the study of the mechanisms of cognitive impairment diseases such as Alzheimer's disease, and has certain peripheral M receptor activation-related side effects (such as gastrointestinal reactions). | |||||||||||||||||||||
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- [1]. Bradley SJ, et al. Bitopic Binding Mode of an M1 Muscarinic Acetylcholine Receptor Agonist Associated with Adverse Clinical Trial Outcomes. Mol Pharmacol. 2018 Jun;93(6):645-656. [Content Brief]
- [2]. Nathan PJ, et al. The potent M1 receptor allosteric agonist GSK1034702 improves episodic memory in humans in the nicotine abstinence model of cognitive dysfunction. Int J Neuropsychopharmacol. 2013 May;16(4):721-31. [Content Brief]
Keywords
