齐美定

齐美定用途

齐美利定是5-羟色胺摄取和SERT的有效和选择性抑制剂。齐美利定是一种抗抑郁药[1][2][3][4]。
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齐美定名称

[ CAS 号 ]:
56775-88-3

[ 中文名 ]:
泽麦定

[ 英文名 ]:
Zimeldine

[中文别名 ]:

[英文别名 ]:

齐美定生物活性

[ 描述 ]:

齐美利定是5-羟色胺摄取和SERT的有效和选择性抑制剂。齐美利定是一种抗抑郁药[1][2][3][4]。

[ 相关类别 ]:

研究领域 >> 神经疾病
信号通路 >> 神经信号通路 >> 5-羟色胺转运蛋白
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

[体内研究]

齐美利定(15 mg/kg,IP,一次)可降低大鼠对吗啡诱导的镇痛耐受的发展[3]。齐美利定(5 mg/kg,IP,每日14天)不会改变CA3海马锥体神经元对应用5-HT的微离子电渗疗法的反应性[2]。内侧杏仁核(MeA)中的齐美利定(0.2、2和20 nmol/100 nL)在禁食大鼠中引起剂量依赖性的吞咽减退作用[4]。动物模型：雄性Wistar白化大鼠(160-180 g,n=72)[3]剂量：15 mg/kg给药：IP,一次结果：显著减弱吗啡耐受的发展和表达。通过甩尾和热板试验,齐美利定组在60分钟测量时和吗啡耐受组在30分钟测量时获得了齐美利丁的最大抗伤害作用。齐美利定与吗啡联用显示出附加镇痛作用。动物模型：Sprague Dawley大鼠(150至250 g,10只,雄性)[2]剂量：5 mg/kg给药：IP,每日14天结果：未改变CA3海马锥体神经元对应用5-HT的微离子电渗疗法的反应性。

[参考文献]

[1]. Heel RC, et al. Zimelidine: a review of its pharmacological properties and therapeutic efficacy in depressive illness. Drugs. 1982 Sep;24(3):169-206.

[2]. Blier P, et al. Electrophysiological investigations on the effect of repeated zimelidine administration on serotonergic neurotransmission in the rat. J Neurosci. 1983 Jun;3(6):1270-8.

[3]. Ozdemir E, et al. Zimelidine attenuates the development of tolerance to morphine-induced antinociception. Indian J Pharmacol. 2012 Mar;44(2):215-8.

[4]. Scopinho AA, et al. Medial amygdaloid nucleus 5-HT₂c receptors are involved in the hypophagic effect caused by zimelidine in rats. Neuropharmacology. 2012 Aug;63(2):301-9.

齐美定物理化学性质

[ 密度 ]:
1.3±0.1 g/cm3

[ 沸点 ]:
412.8±45.0 °C at 760 mmHg

[ 分子式 ]:
C16H19BrCl2N2

[ 分子量 ]:
317.224

[ 闪点 ]:
203.4±28.7 °C

[ 精确质量 ]:
316.057495

[ PSA ]:
16.13000

[ LogP ]:
4.63

[ 蒸汽压 ]:
0.0±1.0 mmHg at 25°C

[ 折射率 ]:
1.597

齐美定毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :
UC6555000
CHEMICAL NAME :
2-Propen-1-amine, 3-(4-bromophenyl)-N,N-dimethyl-3-(3-pyridinyl)-, (Z)-
CAS REGISTRY NUMBER :
56775-88-3
BEILSTEIN REFERENCE NO. :
0479680
LAST UPDATED :
199612
DATA ITEMS CITED :
6
MOLECULAR FORMULA :
C16-H17-Br-N2
MOLECULAR WEIGHT :
317.26
WISWESSER LINE NOTATION :
T6NJ CYR DE&U2N1&1

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Human - woman
DOSE/DURATION :
56 mg/kg/14D
TOXIC EFFECTS :
Behavioral - muscle weakness Behavioral - headache Gastrointestinal - nausea or vomiting
REFERENCE :
BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 285,1009,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
900 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic
REFERENCE :
DRUGAY Drugs. International Journal of Current Therapeutics and Applied Pharmacology Reviews. (ADIS Press International Inc., Suite B-30, Oxford Ct. Business Center, 582 Middletown Blvd., Langhorne, PA 19047) V.1- 1971- Volume(issue)/page/year: 24,169,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
50 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic
REFERENCE :
DRUGAY Drugs. International Journal of Current Therapeutics and Applied Pharmacology Reviews. (ADIS Press International Inc., Suite B-30, Oxford Ct. Business Center, 582 Middletown Blvd., Langhorne, PA 19047) V.1- 1971- Volume(issue)/page/year: 24,169,1982
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Oral
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
800 mg/kg
TOXIC EFFECTS :
Behavioral - convulsions or effect on seizure threshold Behavioral - antipsychotic
REFERENCE :
DRUGAY Drugs. International Journal of Current Therapeutics and Applied Pharmacology Reviews. (ADIS Press International Inc., Suite B-30, Oxford Ct. Business Center, 582 Middletown Blvd., Langhorne, PA 19047) V.1- 1971- Volume(issue)/page/year: 24,169,1982
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 - convulsions or effect on seizure threshold Behavioral - antipsychotic
REFERENCE :
DRUGAY Drugs. International Journal of Current Therapeutics and Applied Pharmacology Reviews. (ADIS Press International Inc., Suite B-30, Oxford Ct. Business Center, 582 Middletown Blvd., Langhorne, PA 19047) V.1- 1971- Volume(issue)/page/year: 24,169,1982 ** REPRODUCTIVE DATA **
TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Subcutaneous
DOSE :
280 mg/kg
SEX/DURATION :
female 14 day(s) pre-mating
TOXIC EFFECTS :
Reproductive - Maternal Effects - menstrual cycle changes or disorders
REFERENCE :
NEAGDO Neurobiology of Aging. (ANKHO International Inc., POB 426, Fayetteville, NY 13066) V.1- 1980- Volume(issue)/page/year: 7,9,1986
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齐美定安全信息

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22

[ 安全声明 (欧洲) ]:
S36

齐美定合成路线

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