N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE
| 中文名称 | N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE |
|---|---|
| 中文同义词 | 化合物EMPA;EMPA,OX2拮抗剂;N-乙基-2-[(6-甲氧基-3-吡啶基)[(2-甲基苯基)磺酰基]氨基]-N-(3-吡啶基甲基)乙酰胺 |
| 英文名称 | EMPA |
| 英文同义词 | N-Ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-acetamide;N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE;EMPA, CID 9981404;Acetamide, N-ethyl-2-[(6-methoxy-3-pyridinyl)[(2-methylphenyl)sulfonyl]amino]-N-(3-pyridinylmethyl)-;Hypocretin Receptor,EMPA,Orexin Receptor (OX Receptor),HCRT Receptor,inhibit,Inhibitor |
| CAS号 | 680590-49-2 |
| 分子式 | C23H26N4O4S |
| 分子量 | 454.54 |
| EINECS号 | |
| 相关类别 | Heterocycles, Pharmaceuticals, Intermediates & Fine Chemicals, Sulfur & Selenium Compounds |
| Mol文件 | 680590-49-2.mol |
| 结构式 | ![N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE 结构式](CAS/GIF/680590-49-2.gif) |
N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE 性质
| 沸点 | 660.7±65.0 °C(Predicted) |
|---|---|
| 密度 | 1.280±0.06 g/cm3(Predicted) |
| 储存条件 | -20°C |
| 溶解度 | 在 DMSO 中溶解度为 100 mM，在乙醇中溶解度为 100 mM |
| 形态 | 粉末 |
| 酸度系数(pKa) | 4.77±0.10(Predicted) |
| 颜色 | 白色至浅棕色 |
N-ETHYL-2-[(6-METHOXYPYRIDIN-3-YL)-(2-METHYLPHENYL)SULFONYLAMINO]-N-(PYRIDIN-3-YLMETHYL)ACETAMIDE 用途与合成方法
|
OX 2 Receptor
|
EMPA competitively antagonizes orexin-A-and orexin-B-evoked accumulation of [
3
H]inositol phosphates (IP) at hOX
2
receptors with pA
2
values of 8.6 and 8.8 respectively.
EMPA displaces the [
3
H]EMPA binding from cell membranes containing human and rat OX
2
receptors, with K
i
values of 1.10±0.24 nM and 1.45±0.13 nM, respectively.
EMPA shows an IC
50
=5.75 µM, K
i
=2.63 µM, and IC
50
=12.8 µM, K
i
=5.8 µM in the binding assay at human and mouse V
1a
receptors, respectively.
In CHO(dHFr
-
) cells stably expressing hOX
2
receptors, EMPA inhibits orexin-A-or orexin-B-evoked [Ca
2+
]
i
response with IC
50
s of 8.8±1.7 nM and 7.9±1.7 nM, respectively.
EMPA (1-300 mg/kg; i.p.) dose-dependently reverses this [Ala
11
,D-Leu
15
]orexin-B-induced hyperlocomotion without itself significantly affecting locomotor activity (LMA) in male NMRI mice.
EMPA (3-30 mg/kg; i.p.) induces a significant and dose-dependent reduction in the baseline LMA in france and male Wistar rats. EMPA (3-30 mg/kg; i.p.) demonstrates a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals.
| Animal Model: | Male NMRI mice (20-30 g) |
| Dosage: | 1, 3, 10, 30, 100, 300 mg/kg |
| Administration: | Injected i.p. at a volume of 10 mL/kg |
| Result: | Dose-dependently reversed this [Ala 11 ,D-Leu 15 ]orexin-B-induced hyperlocomotion without itself significantly affecting LMA. |
| Animal Model: | France and Male Wistar rats (196-237 g) |
| Dosage: | 3, 10, 30 mg/kg |
| Administration: | Injected i.p. at a volume of 5 mL/kg |
| Result: |
Induced a significant and dose-dependent reduction in the baseline LMA.
Demonstrated a clear dose-dependent inhibition of spontaneous activity as compared with vehicle-treated animals. |