For research use only. Not for therapeutic Use.
Nelotanserin（Cat No.:I005032） is a powerful and selective 5-HT2A inverse agonist. It exhibits high potency in the low nanomolar range specifically targeting the 5-HT2A receptor. Notably, ketanserin demonstrates a remarkable selectivity of at least 30-fold and 5000-fold when compared to the 5-HT2C and 5-HT2B receptors, respectively. By acting as an inverse agonist, ketanserin effectively reduces the activity of the 5-HT2A receptor. This property makes it a potential therapeutic candidate for conditions related to 5-HT2A receptor dysregulation, such as hallucinations, sleep disorders, and psychiatric disorders like schizophrenia and depression.
| Catalog Number | I005032 |
| CAS Number | 839713-36-9 |
| Molecular Formula | C18H15BrF2N4O2 |
| Purity | ≥95% |
| Target | target: 5-HT2A |
| Solubility | DMSO ≥ 32 mg/mL |
| Storage | Store at -20°C |
| IUPAC Name | 1-[3-(4-bromo-2-methylpyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea |
| InChI | InChI=1S/C18H15BrF2N4O2/c1-25-17(13(19)9-22-25)12-8-11(4-6-16(12)27-2)23-18(26)24-15-5-3-10(20)7-14(15)21/h3-9H,1-2H3,(H2,23,24,26) |
| InChIKey | COSPVUFTLGQDQL-UHFFFAOYSA-N |
| SMILES | CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)F)F)OC |
| Reference | </br>1:Discovery of 1-[3-(4-bromo-2-methyl-2h-pyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea (nelotanserin) and related 5-hydroxytryptamine2A inverse agonists for the treatment of insomnia. Teegarden BR, Li H, Jayakumar H, Strah-Pleynet S, Dosa PI, Selaya SD, Kato N, Elwell KH, Davidson J, Cheng K, Saldana H, Frazer JM, Whelan K, Foster J, Espitia S, Webb RR, Beeley NR, Thomsen W, Morairty SR, Kilduff TS, Al-Shamma HA.J Med Chem. 2010 Mar 11;53(5):1923-36. doi: 10.1021/jm9007328. PMID: 20143782 </br>2:Nelotanserin, a novel selective human 5-hydroxytryptamine2A inverse agonist for the treatment of insomnia. Al-Shamma HA, Anderson C, Chuang E, Luthringer R, Grottick AJ, Hauser E, Morgan M, Shanahan W, Teegarden BR, Thomsen WJ, Behan D.J Pharmacol Exp Ther. 2010 Jan;332(1):281-90. doi: 10.1124/jpet.109.160994. Epub 2009 Oct 19. PMID: 19841476 Free Article |
