SB-699551

SB-699551 is a potent and selective 5-HT5A antagonist with a Ki value of 5.1 μM. SB-699551 increases the phosphorylation levels of CREB and ATF1, and decreases the phosphorylation levels of AKT, PRAS40, P70S6K, FOXO1, and S6RP. SB-699551 improves drug-induced cognitive deficits. SB-699551 improves social withdrawal and forgetfulness. SB-699551 inhibits breast cancer.

Product Specifications

CAS Number

[864741-95-7]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

5-HT Receptor; Akt; Epigenetic Reader Domain; FOXO; Ribosomal S6 Kinase (RSK)

Type

Reference compound

Related Pathways

Epigenetics; GPCR/G Protein; MAPK/ERK Pathway; Metabolic Enzyme/Protease; Neuronal Signaling; PI3K/Akt/mTOR

Applications

Cancer-Kinase/protease

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/sb-699551.html

Concentration

10mM

Purity

99.53

Solubility

DMSO : 100 mg/mL (ultrasonic) |H2O : 1 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(N(CCN(C)C)CC1=CC=C(C2=CC=C(CNCCC3=CC=CC=C3)C=C2)C=C1)CCC4CCCC4.[H]Cl.[H]Cl

Molecular Formula

C34H47Cl2N3O

Molecular Weight

584.66

Precautions

H302, H315, H319, H335

References & Citations

[1]David R Thomas, et al. SB-699551-A (3-cyclopentyl-N-[2- (dimethylamino) ethyl]-N-[ (4'-{[ (2-phenylethyl) amino]methyl}-4-biphenylyl) methyl]propanamide dihydrochloride), a novel 5-ht5A receptor-selective antagonist, enhances 5-HT neuronal function: Evidence for an autoreceptor role for the 5-ht5A receptor in guinea pig brain. Neuropharmacology. 2006 Sep;51 (3) :566-77.|[2]Curtin PC, et al. The 5-HT5A receptor regulates excitability in the auditory startle circuit: functional implications for sensorimotor gating. J Neurosci. 2013 Jun 12;33 (24) :10011-20.|[3]Gwynne WD, et al. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells. BMC Cancer. 2020 Aug 5;20 (1) :724.|[4]Gwynne WD, et al. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells. BMC Cancer. 2020 Aug 5;20 (1) :724.|[5]Kalinina N I, et al. Involvement of 5-HT 1 and 5-HT 5A Receptors in Modulation of Synaptic Transmission and Intrinsic Membrane Properties of Spinal Motoneurons of the Frog (Rana ridibunda) . Journal of Evolutionary Biochemistry and Physiology, 2022, 58 (1) : 138-148. |[6]Sánchez-Maldonado C, et al. GR-127935-sensitive mechanism mediating hypotension in anesthetized rats: are 5-HT5B receptors involved? J Cardiovasc Pharmacol. 2015 Apr;65 (4) :335-41.|[7]Nikiforuk A, et al. The effects of a 5-HT5A receptor antagonist in a ketamine-based rat model of cognitive dysfunction and the negative symptoms of schizophrenia. Neuropharmacology. 2016 Jun;105:351-360.|[8]Aparicio-Nava L, et al. Effects of 5-HT5A receptor blockade on amnesia or forgetting. Behav Brain Res. 2019 Jan 14;357-358:98-103.|[9]Quiñonez-Bastidas GN, et al. Antinociceptive effect of (-) -epicatechin in inflammatory and neuropathic pain in rats. Behav Pharmacol. 2018 Apr;29 (2 and 3-Spec Issue) :270-279.|[10]Fernández-González JF, et al. Chronic sarpogrelate treatment improves renal sympathetic hyperactivity in experimental diabetes. Biomed Pharmacother. 2024 Jul;176:116814.|[11]Gonzalez R, et al. Role of 5-HT5A receptors in the consolidation of memory. Behav Brain Res. 2013 Sep 1;252:246-51.