Nelotanserin is a potent5-HT_2Ainverse agonist, a moderately potent5-HT_2Cpartial inverse agonist and a weak5-HT_2Binverse agonist, withIC₅₀sof 1.7, 79, 791 nM inIPaccumulation assays, respectively.

Results from IP accumulation assays suggest that Nelotanserin is a potent 5-HT_2Afull inverse agonist (IC₅₀=1.7 nM), a moderately potent 5-HT_2Cpartial inverse agonist (IC₅₀=79 nM) (maximal response was 62% of the response obtained for the reference inverse agonist clozapine), and a weak 5-HT_2Binverse agonist (IC₅₀=791 nM). Nelotanserin displays high affinity for recombinant human 5-HT_2Areceptors (K_i=0.35 nM), moderate affinity for human 5-HT_2Creceptors (K_i=100 nM), and low affinity for human 5-HT_2Breceptors (2000 nM) stably expressed in HEK293 cells. The results suggest that Nelotanserin has a 262-fold higher affinity for human 5-HT_2Athan 5-HT_2Creceptors and a 6610-fold higher affinity for human 5-HT_2Athan 5-HT_2Breceptors^[1].

Each compound is tested in a minimum of five rats by oral gavage with administration occurring in the middle of the inactive period, 6 h after light onset. The delta power during non-REM sleep (NREMS) is significantly different between all the analogues tested and the vehicle control. Nelotanserin (Compound 39) produces significant increases in delta power that persist for the first 4 h following dosing. Significant differences are found, however, in NREMS bout length. Nelotanserin significantly increases NREMS bout length during the first hour following dosing, and 3 does so during the second hour. In conjunction with this increased NREM bout duration, the number of NREM bouts decrease during the first hour for Nelotanserin (p<0.01) as well as for compound 15 (p<0.05)^[2].

437.24

Solid

C₁₈H₁₅BrF₂N₄O₂

839713-36-9

Room temperature in continental US; may vary elsewhere.

DMSO : ≥ 32 mg/mL(73.19 mM)

*"≥" means soluble, but saturation unknown.

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