Biological Activity
5-HT2B antagonist-1 is an orally active 5-HT2B receptor antagonist with an IC50 value of 33.4 nM. 5-HT2B antagonist-1 can be used in studies of diseases characterized by 5-HT2B receptor signaling, such as hepatocellular carcinoma, cardiovascular disease or gastrointestinal disease[1][2].
5-HT2B antagonist-1 (compound 5g) has some sodium channel binding activity with IC50 values in the range of 12.6 to 57.5 μM[1].5-HT2B antagonist-1 (coumpound 1-e) inhibits 5-HT2B receptor activity by less than 50% at 1 μM in CHO-K1 cell lines[3].
5-HT2B antagonist-1 (compound 15) (oral gavage, 30 mg/kg) can reduce visceral hypersensitivity significantly in irritable bowel syndrome (IBS) rats[2].
References
[1]. Xiang Ma, et al. Synthesis and in vitro evaluation of 2,4-diamino-1,3,5-triazine derivatives as neuronal voltage-gated sodium channel blockers. Bioorg Med Chem Lett. 2009 Oct 1;19(19):5644[2]. Yu Zhou, et al. Structure-Based Discovery of Novel and Selective 5-Hydroxytryptamine 2B Receptor Antagonists for the Treatment of Irritable Bowel Syndrome. J Med Chem. 2016 Jan 28;59(2):707-20.[3]. Huang Niu, et al. 5-HT2B Antagonists. WO2015158214
