393129-91-4

393129-91-4 structure

Name: WAY-388264-A
Chemical Name: 5-HT2B antagonist-1
CAS Number: 393129-91-4
Molecular Formula: C₁₁H₁₄BrN₅
Molecular Weight: 296.17
Catalog: Signaling Pathways GPCR/G Protein 5-HT Receptor
Create Date: 2022-08-17 11:49:41
Modify Date: 2024-02-04 17:41:23
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].

Name	5-HT2B antagonist-1

Description	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].
Related Catalog	Research Areas >> Cancer Research Areas >> Cardiovascular Disease Research Areas >> Endocrinology Research Areas >> Metabolic Disease Signaling Pathways >> GPCR/G Protein >> 5-HT Receptor Signaling Pathways >> Neuronal Signaling >> 5-HT Receptor
Target	5-HT2B Receptor:33.4 nM (IC50)
In Vitro	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].
In Vivo	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