Datasheet Inhibitors / Agonists / Screening Libraries A SCREENING EXPERT

Product Name : Nelotanserin Catalog Number : T7350 CAS Number : 839713-36-9 Molecular Formula : C18H15BrF2N4O2 Molecular Weight : 437.24

Description: Nelotanserin is a potent 5-HT2A inverse agonist(IC50 : 1.7 nM), a moderately potent 5-HT2C partial inverse agonist t(IC50 :79 nM )and a weak 5-HT2B inverse agonistt(IC50 : 791 nM).

Storage: 2 years -80°C in solvent; 3 years -20°C powder;

DMSO 32 mg/mL (73.19 mM) Solubility ( < 1 mg/ml refers to the product slightly soluble or insoluble )

5-HT2A Receptor 1.7 nM Receptor (IC50) 5-HT2C Receptor 79 nM 5-HT2B Receptor 791 nM

In vivo Activity In healthy human volunteers, nelotanserin was rapidly absorbed after oral administration and achieved maximum concentrations 1 h later. EEG effects occurred within 2 to 4 h after dosing, and were consistent with vigilance-lowering. A dose response of nelotanserin was assessed in a postnap model in healthy subjects. All doses (up to 40 mg) of nelotanserin significantly improved measures of sleep consolidation, including decreases in the number of stage shifts, number of awakenings after sleep onset, microarousal index, and number of sleep bouts, concomitant with increases in sleep bout duration. Nelotanserin did not affect total sleep time, or sleep onset latency. Furthermore, subjective pharmacodynamic effects observed the morning after dosing were minimal and had no functional consequences on psychomotor skills or memory[1].

Reference 1. Al-Shamma H A , Anderson C , Chuang E , et al. Nelotanserin, a Novel Selective Human 5-Hydroxytryptamine2A Inverse Agonist for the Treatment of Insomnia[J]. Journal of Pharmacology and Experimental Therapeutics, 2010, 332(1):281-290. 2. Monti J M . control of sleep-wake behavior[J]. Sleep Medicine Reviews, 2011, 15(4):0-281.

FOR RESEARCH PURPOSES ONLY. NOT FOR DIAGNOSTIC OR THERAPEUTIC USE. Information for product storage and handling is indicated on the product datasheet. Targetmol products are stable for long term under the recommended storage conditions. Our products may be shipped under different conditions as many of them are stable in the short-term at higher or even room temperatures. We ensure that the product is shipped under conditions that will maintain the quality of the reagents. Upon receipt of the product, please follow the storage recommendations on the product data sheet.

[email protected] | Tel: +1-781-999-4286 | www.targetmol.com