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SB 742457 hydrochloride
- GSK 742457 HCl - Intepirdine HCl
- Parent CAS: 607742-69-8
- Soluble in DMSO
- MF: C19H19N3O2S.HCl
- MW: 389.9
Description
SB 742457 hydrochloride is a potent and selective serotonin 5-HT6 receptor antagonist that blocks Gs-coupled 5-HT6 signaling.
5-HT6 receptors are enriched in the central nervous system and influence cholinergic, glutamatergic and monoaminergic neurotransmission involved in cognition. SB 742457, also known as intepirdine, is a reference ligand for cognitive and serotonergic pathway studies. Research indicates that combining SB74247 with Donepezil (Axon 1438) can provide cognitive and functional benefits.
Key Features
- Selective 5-HT6 receptor antagonist
- Blocks 5-HT6-mediated cAMP signaling
- Modulates neurotransmitter systems linked to cognition
- Orally active CNS pharmacology tool
Applications
- 5-HT6 receptor binding and functional assays
- Cognition and memory pathway research
- Cholinergic–serotonergic interaction studies
- Neurodegeneration-related pharmacology models
More Information
| Parent CAS No. | 607742-69-8 |
|---|---|
| Chemical Name | 3-Benzenesulfonyl-8-piperazin-1-yl-quinoline hydrochloride |
| SMILES | C1(S(C2C=CC=CC=2)(=O)=O)C=C2C=CC=C(N3CCNCC3)C2=NC=1.Cl |
| MFCD | MFCD12546132 |
| InChi | InChI=1S/C19H19N3O2S.ClH/c23-25(24,16-6-2-1-3-7-16)17-13-15-5-4-8-18(19(15)21-14-17)22-11-9-20-10-12-22;/h1-8,13-14,20H,9-12H2;1H |
| InChiKey | BWLWNUQEZNYKAU-UHFFFAOYSA-N |
| CID | 56972141 |
| Short Description | 5-HT6 antagonist |
References
- N Idris et al. Sertindole improves sub-chronic PCP-induced reversal learning and episodic memory deficits in rodents: involvement of 5-HT(6) and 5-HT (2A) receptor mechanisms. Psychopharmacology 2010, 208 (1), 23–36.
- G Maher-Edwards et al. Double-Blind, Controlled Phase II Study of a 5-HT6 Receptor Antagonist, SB-742457, in Alzheimer's Disease. Curr. Alzheimer Res. 2009, 7(5), 374-385.
- G Rossé G and H Schaffhauser. 5-HT(6) Receptor Antagonists as Potential Therapeutics for Cognitive Impairment. Curr. Top. Med. Chem. 2010, 10(2), 207-221.
- N Upton et al. 5-HT6 receptor antagonists as novel cognitive enhancing agents for Alzheimer's disease. Neurotherapeutics 2008, 5(3), 458–469.
- Mitchell E.S. et al. 5-HT6 receptors: a novel target for cognitive enhancement. Pharmacol Ther. 2005, 108(3), 320-333.
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