791789-61-2
Chemical Structure
SB-699551 free base
- CAS No.: 791789-61-2
- Formula:C34H45N3O
- Molecular Weight:511.74
IUPAC Name: 3-cyclopentyl-N-(2-(dimethylamino)ethyl)-N-((4'-((phenethylamino)methyl)-[1,1'-biphenyl]-4-yl)methyl)propanamide
InChIKey: SEQAMPXQRKYYQF-UHFFFAOYSA-N
SMILES: O=C(N(CCN(C)C)CC1=CC=C(C2=CC=C(CNCCC3=CC=CC=C3)C=C2)C=C1)CCC4CCCC4
Biological Activity: SB-699551 free base is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 free base shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 free base disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 free base can be used for the research of anxiety, breast cancer, and Alzheimer's disease[1][2][3][4][5].
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SB-699551 free base | SB-699551 free base is a selective and brain penetrant 5-HT5A receptor antagonist with a pKi of 8.2 nM. SB-699551 free base shows high selectivity over most other 5-HT receptor subtypes, dopamine receptors, and α1B adrenoceptor. SB-699551 free base disrupts Gαi/o-coupled and PI3K/AKT/mTOR signaling pathways, alters CREB, ATF1, AKT, PRAS40, S6K, and FOXO1 phosphorylation in breast tumor cells. SB-699551 free base can be used for the research of anxiety, breast cancer, and Alzheimer's disease. | |||||||||||||||||||||
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- [1]. Corbett DF, et al. Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry. Bioorg Med Chem Lett. 2005;15(18):4014-4018. [Content Brief]
- [2]. Kassai F, et al. Effect of 5-HT5A antagonists in animal models of schizophrenia, anxiety and depression. Behav Pharmacol. 2012;23(4):397-406. [Content Brief]
- [3]. Gwynne WD, et al. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells. BMC Cancer. 2020;20(1):724. Published 2020 Aug 5. [Content Brief]
- [4]. Gonzalez R, et al. Role of 5-HT5A receptors in the consolidation of memory. Behav Brain Res. 2013 Sep 1;252:246-51. [Content Brief]
- [5]. Aparicio-Nava L, et al. Effects of 5-HT5A receptor blockade on amnesia or forgetting. Behav Brain Res. 2019;357-358:98-103. [Content Brief]
Keywords
