1346233-68-8
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- CAS号:
- 1346233-68-8
- 英文名:
- 3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-diMethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]Methyl]-benzaMide
- 英文别名:
- ML218;VU0413807;VU0424199-1;CID 45115620;ML218,ML-218;ML 218 hydrochloride;Benzamide, 3,5-dichloro-N-[[(1α,5α,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]-;3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-diMethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]Methyl]-benzaMide;3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]-benzamide hydrochloride
- 中文名:
- 1346233-68-8
- 中文别名:
- 化合物 T12076L
- CBNumber:
- CB52695162
- 分子式:
- C19H26Cl2N2O
- 分子量:
- 369.33
- MOL File:
- 1346233-68-8.mol
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1346233-68-8化学性质
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沸点:
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455.5±35.0 °C(Predicted)
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密度:
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1.184±0.06 g/cm3(Predicted)
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储存条件:
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2-8°C
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溶解度:
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DMSO: soluble10mg/mL (clear solution)
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酸度系数(pKa):
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13.65±0.46(Predicted)
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形态:
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powder
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颜色:
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white to beige
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1346233-68-8性质、用途与生产工艺
ML218 是一种有效的，选择性的和口服活性的 T 型 Ca2+ 通道 (Cav3.1，Cav3.2，Cav3.3) 抑制剂，对 Cav3.2 和 Cav3.3 的 IC50 分别为 310 nM 和 270 nM。ML218 抑制丘脑底核 (STN) 神经元的爆发活动。ML218 对 L 或 N 型钙通道，KATP 或 hERG 钾通道无明显抑制作用。ML218 可以穿透血脑屏障。
IC50: 310 nM (Cav3.2), 270 nM (Cav3.3), and 150 nM (Ca
2+
flux)
In plasma protein binding studies (equilibrium dialysis), ML218 possesses good free fraction in both rat and human. Intrinsic clearance experiments in liver microsomes indicated that ML218 is highly cleared in rat (CL
int
= 115 mL/min/kg), but low to moderately cleared in human liver microsomes (CL
int
= 12.7 mL/min/kg).
ML218 (0.03-30 mg/kg; oral administration; once; male Sprague-Dawley rats) treatment reverses cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol.
Free brain and plasma concentrations of ML218 increases in a dose proportional manner across the dose range (3 mg/kg: [plasma] = 98 nM, [brain] = 1.66 μM; 10 mg/kg: [plasma] = 282 nM, [brain] = 5.03 μM; 30 mg/kg: 1.2 μM, [brain] = 17.7 μM).
Noncompartmental pharmacokinetic analysis indicates ML218 (1 mg/kg, IV) has a mean residence time (MRT) of nearly 7 h, a value which is consistent with its terminal half-life (t
1/2
= 7 h).
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Animal Model:
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Male Sprague-Dawley rats (275-299 g) induced by haloperidol
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Dosage:
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0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg
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Administration:
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Oral administration; once
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Result:
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Reversed cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol.
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1346233-68-8
上下游产品信息
上游原料
下游产品
| 更新日期 | 产品编号 | 产品名称 | CAS编号 | 包装 | 价格 |
|---|
| 2024/01/25 | HY-103309 | ML218 | | 1 mg | 818元 |
| 2024/01/25 | HY-103309 | 1346233-68-8
ML218 | 1346233-68-8 | 5mg | 1800元 |
1346233-68-8, 1346233-68-8 相关搜索:
- Aromatics, Inhibitors, Pharmaceuticals, Intermediates & Fine Chemicals
- 化合物 T12076L
- 1346233-68-8
- ML218,ML-218
- 3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]-benzamide hydrochloride
- Benzamide, 3,5-dichloro-N-[[(1α,5α,6α)-3-(3,3-dimethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]methyl]-
- ML 218 hydrochloride
- VU0424199-1
- VU0413807
- ML218
- CID 45115620
- 3,5-Dichloro-N-[[(1α,5α,6-exo,6α)-3-(3,3-diMethylbutyl)-3-azabicyclo[3.1.0]hex-6-yl]Methyl]-benzaMide