维洛沙秦

维洛沙秦用途

维洛嗪(维洛嗪)是一种去甲肾上腺素再摄取抑制剂,也是一种有效的5-HT2C激动剂和5-HT2B拮抗剂,其EC50分别为32μM和27μM。维洛嗪的作用机制主要涉及5-羟色胺能和去甲肾上腺素能途径。维洛嗪可用于研究抑郁症[1][2]。
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维洛沙秦名称

[ CAS 号 ]:
46817-91-8

[ 中文名 ]:
维洛沙秦

[ 英文名 ]:
2-[(2-ethoxyphenoxy)methyl]morpholine

[中文别名 ]:

[英文别名 ]:

维洛沙秦生物活性

[ 描述 ]:

维洛嗪(维洛嗪)是一种去甲肾上腺素再摄取抑制剂,也是一种有效的5-HT2C激动剂和5-HT2B拮抗剂,其EC50分别为32μM和27μM。维洛嗪的作用机制主要涉及5-羟色胺能和去甲肾上腺素能途径。维洛嗪可用于研究抑郁症[1][2]。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 肾上腺素能受体
研究领域 >> 神经疾病
信号通路 >> G 蛋白偶联受体/G 蛋白 >> 5-HT受体
信号通路 >> 神经信号通路 >> 5-HT受体

[ 靶点 ]

Human 5-HT2C Receptor:32 μM (EC50)

human 5-HT2B Receptor:27 μM (IC50)


[参考文献]

[1]. Yu C, et al. New Insights into the Mechanism of Action of Viloxazine: Serotonin and Norepinephrine Modulating Properties. J Exp Pharmacol. 2020 Aug 25;12:285-300.

[2]. Pinder RM, et al. Viloxazine: a review of its pharmacological properties and therapeutic efficacy in depressive illness. Drugs. 1977 Jun;13(6):401-21.

维洛沙秦物理化学性质

[ 密度 ]:
1.061 g/cm3

[ 沸点 ]:
350.5ºC at 760 mmHg

[ 熔点 ]:
185-186ºC

[ 分子式 ]:
C13H19NO3

[ 分子量 ]:
237.29500

[ 闪点 ]:
144.3ºC

[ 精确质量 ]:
237.13600

[ PSA ]:
39.72000

[ LogP ]:
1.78130

[ 折射率 ]:
1.499

维洛沙秦毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
QE3940000
CHEMICAL NAME :
Morpholine, 2-((2-ethoxyphenoxy)methyl)-
CAS REGISTRY NUMBER :
46817-91-8
LAST UPDATED :
199403
DATA ITEMS CITED :
5
MOLECULAR FORMULA :
C13-H19-N-O3
MOLECULAR WEIGHT :
237.33
WISWESSER LINE NOTATION :
T6M DOTJ C1OR BO2

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
2 gm/kg
TOXIC EFFECTS :
Behavioral - muscle weakness Behavioral - ataxia Behavioral - muscle contraction or spasticity
REFERENCE :
HEPHD2 Handbook of Experimental Pharmacology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.50- 1978- Volume(issue)/page/year: 55,527,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
60 mg/kg
TOXIC EFFECTS :
Behavioral - muscle weakness Behavioral - ataxia Behavioral - muscle contraction or spasticity
REFERENCE :
HEPHD2 Handbook of Experimental Pharmacology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.50- 1978- Volume(issue)/page/year: 55,527,1980
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
552 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
EJMCA5 European Journal of Medicinal Chemistry--Chimie Therapeutique. (Editions Scientifiques Elsevier, 29 rue Buffon, F-75005, Paris, France) V.9- 1974- Volume(issue)/page/year: 27,437,1992
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
60 mg/kg
TOXIC EFFECTS :
Behavioral - muscle weakness Behavioral - ataxia Behavioral - muscle contraction or spasticity
REFERENCE :
HEPHD2 Handbook of Experimental Pharmacology. (Springer-Verlag, Heidelberger Pl. 3, D-1000 Berlin 33, Fed. Rep. Ger.) V.50- 1978- Volume(issue)/page/year: 55,527,1980 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
130 mg/kg
SEX/DURATION :
female 8-20 day(s) after conception
TOXIC EFFECTS :
Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral
REFERENCE :
ATSUDG Archives of Toxicology, Supplement. (Springer-Verlag New York, Inc., Service Center, 44 Hartz Way, Secaucus, NJ 07094) No.1- 1978- Volume(issue)/page/year: 7,504,1984
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