1、NelotanserinCat. No.: HY-10559CAS No.: 839713-36-9Molecular Formula: CHBrFNOMolecular Weight: 437.24Target: 5-HT ReceptorPathway: GPCR/G Protein; Neuronal SignalingStorage: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 monthSolvent 5-HT2C Receptor, IC50: 79 nM; 5-HT2B Receptor, IC50: 7
2、91 nMIn Vitro Results from IP accumulation assays suggest that Nelotanserin is a potent 5-HT2A full inverse agonist (IC50=1.7 nM), a moderately potent 5-HT2C partial inverse agonist (IC50=79 nM) (maximal response was 62% of the response obtained for the reference inverse agonist clozapine), and a we
3、ak 5-HT2B inverse agonist (IC50=791 nM). Nelotanserin displays high affinity for recombinant human 5-HT2A receptors (Ki=0.35 nM), moderate affinity for human 5-HT2C receptors (Ki=100 nM), and low affinity for human 5-HT2B receptors (2000 nM) stably expressed in HEK293 cells. The results suggest that
4、 Nelotanserin has a 262-fold higher affinity for human 5-HT2A than 5-HT2C receptors and a 6610-fold higher affinity for human 5-HT2A than 5-HT2B receptors1.Product Data Sheet InhibitorsAgonistsScreening Librarieswww.MedChemE1In Vivo Each compound is tested in a minimum of five rats by oral gavage wi
5、th administration occurring in the middle of the inactive period, 6 h after light onset. The delta power during non-REM sleep (NREMS) is significantly different between all the analogues tested and the vehicle control. Nelotanserin (Compound 39) produces significant increases in delta power that per
6、sist for the first 4 h following dosing. Significant differences are found, however, in NREMS bout length. Nelotanserin significantly increases NREMS bout length during the first hour following dosing, and 3 does so during the second hour. In conjunction with this increased NREM bout duration, the n
7、umber of NREM bouts decrease during the first hour for Nelotanserin (p0.01) as well as for compound 15 (p0.05)2.REFERENCES1. Al-Shamma HA et al. Nelotanserin, a novel selective human 5-hydroxytryptamine2A inverse agonist for the treatment of insomnia. J Pharmacol Exp Ther. 2010 Jan;332(1):281-90.2.
8、Teegarden BR et al. 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. J Med Chem. 2010 Mar 11;53(5):1923-36.Caution: Product has not been fully validated for medical applications. For research use only.Tel: 609-228-6898 Fax: 609-228-5909 E-mail: techMedChemEAddress: 1 Deer Park Dr, Suite Q, Monmouth Junction, NJ 08852, USAwww.MedChemE2
