Nelotanserin

SKU: orb1299895

Description

Nelotanserin (APD125) is a potent and selective inverse agonist of the 5-HT2A receptor (IC50 = 1.7 nM), with moderate activity at 5-HT2C and weak activity at 5-HT2B. It is a valuable research tool for investigating serotonin receptor function in neuropharmacology, sleep disorders, and related in vitro and in vivo studies.

Research Area

Neuroscience, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 839713-36-9
• MW: 437.24
• Purity: 99.88% (May vary between batches)
• Formula: C₁₈H₁₅BrF₂N₄O₂
• SMILES: COc1ccc(NC(=O)Nc2ccc(F)cc2F)cc1-c1c(Br)cnn1C
• Target: 5-HT Receptor
• Solubility: DMSO:250 mg/mL (571.77 mM)

Bioactivity

• Target IC50:
  5-HT2A receptor:1.7 nM|5-HT2C receptor:79 nM|5-HT2B receptor:791 nM
• In Vivo:
  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 insomnia 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.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

5HTReceptor, 5HT Receptor, 5-HT, 5-hydroxytryptamine Receptor, 5-HT Receptor, APD125, APD-125, APD 125, Nelotanserin, inhibit, Inhibitor, Serotonin Receptor

Compound Identifiers

PubChem CID

11683556