57754-86-6
57754-86-6 結(jié)構(gòu)式
基本信息
3-(2-甲氧基苯氧基)-N-甲基-3-苯基丙-1-胺鹽酸鹽
Nsc298819
NisoxetineHCl
NISOXETINE HYDROCHLORIDE
LY-94939
NSC298819
NISOXETINE HCL
4-((2-Nitrophenyl)thio)-2H-oxete hydrochloride
NISOXETINE HYDROCHLORIDE (LY-94,939) NOR PINEPHRINE UPTAKE
(±)-γ-(2-methoxyphenoxy)-n-methyl-benzenepropanamine hydrochloride
(+/-)-g-(2-Methoxyphenoxy)-N-methylbenzenepropanaminehydrochloride
3-(2-methoxyphenoxy)-N-methyl-3-phenylpropan-1-amine hydrochloride
物理化學(xué)性質(zhì)
常見問題列表
Kd: 0.76 nM (NET)
Nisoxetine inhibits [
3
H]Nisoxetine binding to rat frontal cortical membranes with a K
i
of 1.4±0.1 nM.
Nisoxetine inhibits [
3
H]Noradrenaline uptake into rat frontal cortical synaptosomes with a K
i
of 2.1±0.3 nM.
Nisoxetine inhibits Na
+
currents with IC
50
s of 1.6 and 28.6 μM at the membrane potential of -70 and -100 mV, respectively.
Nisoxetine (0.6-2.2 μM; a single intrathecal injection) displays dose-dependent effects on spinal anesthesia in rats.
Nisoxetine (2.2 μM; a single intrathecal injection) shows 100, 100, and 100% of blockades in motor function, proprioception, and with duration of action of about 61, 96, and 236 min, respectively.
| Animal Model: | Sprague-Dawley rats(290-340 g) |
| Dosage: | 0.6, 1.2, 1.8, 2.2 μM |
| Administration: | A single intrathecal injection |
| Result: | With ED 50 s of 0.82 , 0.75 and 0.70 μM in motor function, proprioception, and nociception respectively. |