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Nelotanserin

Catalog No. T7350   CAS 839713-36-9
Synonyms: APD125

Nelotanserin (APD125) 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).

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Nelotanserin Chemical Structure
Nelotanserin, CAS 839713-36-9
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 48.00
5 mg In stock $ 80.00
10 mg In stock $ 122.00
25 mg In stock $ 198.00
50 mg In stock $ 369.00
100 mg In stock $ 549.00
500 mg In stock $ 1,190.00
1 mL * 10 mM (in DMSO) In stock $ 77.00
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Purity: 98.42%
Purity: 98.01%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Nelotanserin (APD125) 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).
Targets&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[1].
Synonyms APD125
Molecular Weight 437.24
Formula C18H15BrF2N4O2
CAS No. 839713-36-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 32 mg/mL (73.19 mM)

TargetMolReferences and Literature

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 . Serotonin control of sleep-wake behavior[J]. Sleep Medicine Reviews, 2011, 15(4):0-281.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Drug Library Anti-Cancer Clinical Compound Library Anti-Alzheimer's Disease Compound Library Neuronal Signaling Compound Library Anti-Cancer Compound Library Anti-Neurodegenerative Disease Compound Library ReFRAME Related Library Serotonin Receptor-Targeted Compound Library NO PAINS Compound Library Covalent Inhibitor Library

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Keywords

Nelotanserin 839713-36-9 GPCR/G Protein Neuroscience 5-HT Receptor Inhibitor inhibit APD125 APD-125 APD 125 Serotonin Receptor 5-hydroxytryptamine Receptor inhibitor

 

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