Nelotanserin, 羟色胺 2a (5-HT2a) 受体反向激动剂

小分子

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 | 尼洛坦色林

Nelotanserin (USAN/INN) | Nelotanserin [USAN:INN] | UNII-4ZA73QEW2P | AKOS016313895 | SB19023 | BDBM50324541 | APD 125 | CHEBI:177438 | 1-[3-(4-bromo-2-methylpyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-diluorophenyl)urea | AKOS027255058 | APD125(Nelotanserin) |

Nelotanserin

N646312-5mg

5mg

≥98%

-20°C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 Form:Solid 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

C18H15BrF2N4O2

437.24 g/mol

11683556

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

1-[3-(4-bromo-2-methylpyrazol-3-yl)-4-methoxyphenyl]-3-(2,4-difluorophenyl)urea

1S/C18H15BrF2N4O2/c1-25-17(13(19)9-22-25)12-8-11(4-6-16(12)27-2)23-18(26)24-15-5-3-10(20)7-14(15)21/h3-9H,1-2H3,(H2,23,24,26)

COSPVUFTLGQDQL-UHFFFAOYSA-N

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

11683556

DMSO : ≥ 32 mg/mL (73.19 mM)

2

5

4

436.035 Da

436.035 Da

68.200 Ų

27

0

518

0

1

3.3

3.3

反向激动剂

羟色胺 2a (5-HT2a) 受体反向激动剂