Nelotanserin, 羟色胺 2a (5-HT2a) 受体反向激动剂

小分子

尼洛坦色林

Nelotanserin

N654534-1ml

1ml

10mM in DMSO

-80℃储存

超低温冰袋运输

Nelotanserin is a potent 5-HT 2A inverse agonist, a moderately potent 5-HT 2C partial inverse agonist and a weak 5-HT 2B inverse agonist, with IC 50 s of 1.7, 79, 791 nM in IP accumulation assays, respectively. In Vitro Results from IP accumulation assays suggest that Nelotanserin is a potent 5-HT 2A full inverse agonist (IC 50 =1.7 nM), a moderately potent 5-HT 2C partial inverse agonist (IC 50 =79 nM) (maximal response was 62% of the response obtained for the reference inverse agonist clozapine), and a weak 5-HT 2B inverse agonist (IC 50 =791 nM). Nelotanserin displays high affinity for recombinant human 5-HT 2A receptors (K i =0.35 nM), moderate affinity for human 5-HT 2C receptors (K i =100 nM), and low affinity for human 5-HT 2B receptors (2000 nM) stably expressed in HEK293 cells. The results suggest that Nelotanserin has a 262-fold higher affinity for human 5-HT 2A than 5-HT 2C receptors and a 6610-fold higher affinity for human 5-HT 2A than 5-HT 2B receptors. MCE has not independently confirmed the accuracy of these methods. They are for reference only. In Vivo 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 IC50& Target:5-HT 2A Receptor 1.7 nM (IC 50 ) 5-HT 2C Receptor 79 nM (IC 50 ) 5-HT 2B Receptor 791 nM (IC 50 )

奈洛坦色林是一种强效的 5-HT 2A 反向激动剂，也是一种中效的 5-HT 2C 部分反向激动剂和弱效的 5-HT 2B 反向激动剂，在 IP 累积试验中的 IC 50 s 分别为 1.7、79 和 791 nM。

839713-36-9(DMSO)

C18H15BrF2N4O2

437.24 g/mol

CN1C(=C(C=N1)Br)C2=C(C=CC(=C2)NC(=O)NC3=C(C=C(C=C3)F)F)OC

反向激动剂

羟色胺 2a (5-HT2a) 受体反向激动剂