(-)-Viloxazine HCl

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Chemical Structure| 56287-61-7 同义名 : -
CAS号 : 56287-61-7
货号 : A1167355
分子式 : C13H20ClNO3
纯度 : 99%+
分子量 : 273.756
MDL号 : N/A
存储条件:

Pure form Inert atmosphere,Room Temperature

In solvent -20°C:3-6个月-80°C:12个月

溶解度 : -
动物实验配方:
生物活性
描述 (S)-Viloxazine Hydrochloride is S(+)-isomers of the atypical antidepressant viloxazin (Viloxazine) can as a norepinephrine reuptake inhibitor (NRI). n vitro, viloxazine demonstrated antagonistic activity at 5-HT2B and agonistic activity at 5-HT2C receptors, along with predicted high receptor occupancy at clinical doses. In vivo, viloxazine increased extracellular 5-HT levels in the prefrontal cortex (PFC), a brain area implicated in ADHD (attention deficit/hyperactivity disorder). Viloxazine also exhibited moderate inhibitory effects on the norepinephrine transporter (NET) in vitro and in vivo, and elicited moderate activity at noradrenergic and dopaminergic systems[2]. The AMDP-evaluation suggests that viloxazin has a somewhat more marked and more rapid effect on symptoms of retardation, whereas amitriptyline acts predominantly on depressive mood, disturbances of sleep and vital feelings. The viloxazine blood levels showed a remarkably low inter- and intraindividual variance[3]. Fourteen consecutive daily injections of either the racemate or the S-isomer (2, 5 and 10 mg kg-1 i.p.) significantly improved the acquisition of avoidance behaviour. Racemic viloxazine caused a concentration-dependent (10(-5)-10(-3 M) release of 5-MT without affecting any significant change in the release of either catecholamine[4].
实验方案
1mg 5mg 10mg

1 mM

5 mM

10 mM

3.65mL

0.73mL

0.37mL

18.26mL

3.65mL

1.83mL

36.53mL

7.31mL

3.65mL

参考文献

[1]Matthews PRL, Horder J, Pearce M. Selective noradrenaline reuptake inhibitors for schizophrenia. Cochrane Database Syst Rev. 2018;1(1):CD010219.

[2]Yu C, Garcia-Olivares J, Candler S, Schwabe S, Maletic V. New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300

[3]Müller-Oerlinghausen B, Rüther E. Clinical profile and serum concentration of viloxazine as compared to amitriptyline. Pharmakopsychiatr Neuropsychopharmakol. 1979 Jul;12(4):321-37

[4]Greenwood DT, Kemp JD, Middlemiss DN. Stereospecificity of behavioural effects of viloxazine in bulbectomized rats does not correlate with its 5-HT-releasing action in vitro. J Pharm Pharmacol. 1982 Jan;34(1):38-41