RS-127445
| CAS No. | 199864-87-4 | Cat. No. | BCP02714 |
| Name | RS-127445 | ||
| Synonyms | RS 127445;RS127445;MT-500;MT 500;MT500; | ||
| Formula | C17H16FN3 | M. Wt | 281.33 |
| Description | RS-127445 is a selective; high affinity; orally bioavailable serotonin 5-HT2B receptor antagonist. RS-127445 was found to have nanomolar affinity for the 5-HT2B receptor (pKi = 9.5+/-0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently antagonized 5-HT-evoked formation of inositol phosphates (pK(B) = 9.5+/-0.1) and 5-HT-evoked increases in intracellular calcium (pIC50 = 10.4+/-0.1). RS-127445 also blocked 5-HT-evoked contraction of rat isolated stomach fundus (pA2 = 9.5+/-1.1) and (+/-)alpha-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2 = 9.9+/-0.3). | ||
| Pathways | Neuro Signaling Pathway GPCR/G Protein | ||
| Targets | 5 HT Receptor/Serotonin Receptor | ||
Structure
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