Nelotanserin 是5-HT2A强完全逆向激动剂，5-HT2C中等强度的部分反向激动剂和5-HT2B的弱反向激动剂，IC50s值分别为 1.7、79 和 791 nM。

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).

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].

839713-36-9

C18H15BrF2N4O2

437.245

APD125;1-[3-(4-溴-1-甲基-1H-吡唑-5-基)-4-甲氧基苯基]-3-(2,4-二氟苯基)脲;Nelotanserin

DMSO:32 mg/mL (73.19 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years