| Name | Nelotanserin |
| 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). |
| 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]. |
| Storage | store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| Solubility Information | DMSO : 50 mg/mL (114.35 mM), Sonication is recommended.
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| Keywords | 5-HT Receptor | Inhibitor | inhibit | Nelotanserin | APD-125 | APD 125 | Serotonin Receptor | 5-hydroxytryptamine Receptor |
| Inhibitors Related | Serotonin hydrochloride | Alverine citrate | Olanzapine | Dapoxetine hydrochloride | CLOZAPINE N-OXIDE | Mirtazapine | Amitriptyline hydrochloride | Cloperastine hydrochloride | Trazodone hydrochloride | Mianserin hydrochloride | Fluoxetine hydrochloride | Cinchonidine |
| Related Compound Libraries | Bioactive Compound Library | Pain-Related Compound Library | Anti-Neurodegenerative Disease Compound Library | Membrane Protein-targeted Compound Library | Anti-Cancer Clinical Compound Library | Drug Repurposing Compound Library | Clinical Compound Library | Bioactive Compounds Library Max | GPCR Compound Library | Anti-Cancer Drug Library |
United States
