Description
SB-699551 is an antagonist of the serotonin (5-HT) receptor subtype 5-HT5A (Ki = 6.31 nM).1 It is selective for 5-HT5A over a panel of 14 other receptors (Kis = >315 nM for all) but does inhibit the serotonin transporter (SERT; Ki = 25.12 nM). SB-699551 also decreases sphere formation in patient-derived xenograft (PDX) breast cancer cells (IC50 = 596 nM).2 It decreases tumor volume in combination with docetaxel (Item No. 11637) in a PDX mouse model of breast cancer. SB-699551 inhibits cued fear conditioning in mice (ED50 = 25.4 mg/kg).3WARNING This product is not for human or veterinary use.
References
[1] DAVID F. CORBETT . Discovery of a potent and selective 5-ht5A receptor antagonist by high-throughput chemistry[J]. Bioorganic & Medicinal Chemistry Letters, 2005, 15 18: Pages 4014-4018. DOI: 10.1016/j.bmcl.2005.06.024
[2] WILLIAM D GWYNNE. Antagonists of the serotonin receptor 5A target human breast tumor initiating cells.[J]. ACS Applied Electronic Materials, 2020: 724. DOI: 10.1186/s12885-020-07193-6
[3] FERENC KASSAI. Effect of 5-HT5A antagonists in animal models of schizophrenia, anxiety and depression.[J]. Behavioural Pharmacology, 2012, 23 4: 397-406. DOI: 10.1097/fbp.0b013e3283565248
