1346233-68-8
1346233-68-8 結(jié)構(gòu)式
基本信息
VU0413807
VU0424199-1
CID 45115620
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
物理化學(xué)性質(zhì)
常見問題列表
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).
| Animal Model: | Male Sprague-Dawley rats (275-299 g) induced by haloperidol |
| Dosage: | 0.03 mg/kg, 0.1 mg/kg, 0.3 mg/kg, 1 mg/kg, 3 mg/kg, 10 mg/kg, 30 mg/kg |
| Administration: | Oral administration; once |
| Result: | Reversed cataleptic behavior in rats induced by a 0.75 mg/kg dose of haloperidol. |