Nelotanserin

Nelotanserin is a potent 5-HT2A inverse agonist, a moderately potent 5-HT2C partial inverse agonist and a weak 5-HT2B inverse agonist, with IC50s of 1.7, 79, 791 nM in IP accumulation assays, respectively.

Product Specifications

CAS Number

[839713-36-9]

Product Name Alternative

APD125

UNSPSC

12352005

Hazard Statement

H302-H315-H319-H335

Target

5-HT Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Cancer-programmed cell death

Field of Research

Cancer; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/Nelotanserin.html

Purity

99.66

Solubility

DMSO : ≥ 32 mg/mL

Smiles

COC1=C(C2=C(Br)C=NN2C)C=C(NC(NC3=C(F)C=C(F)C=C3)=O)C=C1

Molecular Formula

C18H15BrF2N4O2

Molecular Weight

437.24

Precautions

P261-P264-P270-P271-P280-P302+P352-P304+P340-P305+P351+P338-P330-P362+P364-P403+P233-P405-P501

References & Citations

[1]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]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.