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癸氟奋乃静

癸氟奋乃静用途

Fluphenazine decanoate 是一种长效的吩噻嗪抗精神病药,用于治疗精神分裂症。Fluphenazine decanoate 也是一种高度且连续的多巴胺 D2 受体阻滞剂。

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癸氟奋乃静名称

[ CAS 号 ]:
5002-47-1

[ 中文名 ]:
癸氟奋乃静

[ 英文名 ]:
Fluphenazine decanoate

[中文别名 ]:

保利坤

[英文别名 ]:

Fluphenazine depot
Modecate
Fluphenaline decanoate
Fluphenazindecanoat
Moditen-depo
Fluorophenazine decanoate
Dapotum D
Fluphenazine decanoate
fluphenazine O-decanoate
Flufenazine decanoate

癸氟奋乃静生物活性

[ 描述 ]:

Fluphenazine decanoate 是一种长效的吩噻嗪抗精神病药,用于治疗精神分裂症。Fluphenazine decanoate 也是一种高度且连续的多巴胺 D2 受体阻滞剂。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 多巴胺受体

信号通路 >> 神经信号通路 >> 多巴胺受体

研究领域 >> 神经疾病

[ 靶点 ]

Dopamine D2 receptor[2]

[体内研究]

六只雌性波斯水牛(Equaus hemionus onager)用癸酸氟苯那津(0.1 mg/kg IM)或生理盐水对照。监测尿皮质醇、孕酮、雌激素代谢产物和行为,用超声检查卵泡动力学直到排卵。与生理盐水(9.73 ng/mg肌酐)相比,服用癸酸氟苯那津(6.61 ng/mg肌酐)的运动员皮质醇浓度显著降低。两组间雌激素或孕酮峰值浓度没有差异,所有动物在癸酸氟奋乃静治疗后的预期时间内排卵。然而,一些吸食者的皮质醇分泌只有轻微的减少,一个接受治疗的女性显示黄体孕酮峰值被抑制,这表明使用癸酸氟奋乃嗪可能会造成生殖成本[1]。

[参考文献]

[1]. Wagman JD, et al. The effect of fluphenazine decanoate on glucocorticoid production, reproductive cyclicity, and the behavioral stress response in the Persian onager (Equus hemionus onager). Zoo Biol. 2015 Nov;34(6):525-34.

[2]. Uchida H, et al. Dose and dosing frequency of long-acting injectable antipsychotics: a systematic review of PET and SPECT data and clinical implications. J Clin Psychopharmacol. 2014 Dec;34(6):728-35.

[3]. Weiss RB, et al. Long-acting neuroleptic use for reproductive management of non-domestic ungulates using the domestic goat (Capra hircus) as a model. Zoo Biol. 2014 May-Jun;33(3):204-11.

癸氟奋乃静物理化学性质

[ 密度 ]:
1.149 g/cm3

[ 沸点 ]:
658.1ºCat 760 mmHg

[ 熔点 ]:
30-32°

[ 分子式 ]:
C₃₂H₄₄F₃N₃O₂S

[ 分子量 ]:
591.77100

[ 闪点 ]:
351.8ºC

[ 精确质量 ]:
591.31100

[ PSA ]:
61.32000

[ LogP ]:
7.94050

[ 折射率 ]:
1.537

[ 储存条件 ]:
2-8℃

[ 水溶解性 ]:
Practically insoluble in water, very soluble in ethanol and in methylene chloride, freely soluble in methanol.

癸氟奋乃静毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: HE0525000

CHEMICAL NAME :: Decanoic acid, 2-(4-(3-(2-(trifluoromethyl)phenothiazin-10-yl)propyl )- 1-piperazinyl)ethyl ester

CAS REGISTRY NUMBER :: 5002-47-1

LAST UPDATED :: 199612

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C32-H44-F3-N3-O2-S

MOLECULAR WEIGHT :: 591.85

WISWESSER LINE NOTATION :: T C666 BN ISJ EXFFF B3- AT6N DNTJ D2OV9

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 46 mg/kg/5Y-I

TOXIC EFFECTS :: Behavioral - muscle contraction or spasticity

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human

DOSE/DURATION :: 179 ug/kg

TOXIC EFFECTS :: Behavioral - antipsychotic

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 21 mg/kg/6D-I

TOXIC EFFECTS :: Cardiac - pulse rate Gastrointestinal - changes in structure or function of salivary glands Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Human - man

DOSE/DURATION :: 1071 ug/kg/12D-I

TOXIC EFFECTS :: Behavioral - ataxia Lungs, Thorax, or Respiration - dyspnea Skin and Appendages - sweating

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 19 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Lungs, Thorax, or Respiration - respiratory depression Nutritional and Gross Metabolic - body temperature decrease

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 576 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Skin and Appendages - hair

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - effect, not otherwise specified Behavioral - altered sleep time (including change in righting reflex) Skin and Appendages - hair

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 46 mg/kg/52W-I

TOXIC EFFECTS :: Liver - changes in liver weight Kidney, Ureter, Bladder - other changes in urine composition Nutritional and Gross Metabolic - weight loss or decreased weight gain

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 82 mg/kg/52W-I

TOXIC EFFECTS :: Blood - normocytic anemia Blood - changes in bone marrow (not otherwise specified) Related to Chronic Data - changes in prostate weight

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 230 mg/kg

SEX/DURATION :: male 4 week(s) pre-mating female 2 week(s) pre-mating female 1-7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - menstrual cycle changes or disorders

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 5 mg/kg

SEX/DURATION :: female 17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - stillbirth Reproductive - Effects on Newborn - viability index (e.g., # alive at day 4 per # born alive) Reproductive - Effects on Newborn - weaning or lactation index (e.g., # alive at weaning per # alive at day 4)

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 25 mg/kg

SEX/DURATION :: female 17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - delayed effects

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Intramuscular

DOSE :: 5 mg/kg

SEX/DURATION :: female 7 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Newborn - sex ratio

MUTATION DATA

TEST SYSTEM :: Rodent - rat

DOSE/DURATION :: 20 mg/kg/12W (Intermittent)

REFERENCE :: MUREAV Mutation Research. (Elsevier Science Pub. B.V., POB 211, 1000 AE Amsterdam, Netherlands) V.1- 1964- Volume(issue)/page/year: 244,331,1990 *** REVIEWS *** TOXICOLOGY REVIEW ABPYBL Advances in Biochemical Psychopharmacology. (Raven Press, 1185 Ave. of the Americas, New York, NY 10036) V.1- 1969- Volume(issue)/page/year: 9,301,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - X5576 No. of Facilities: 16 (estimated) No. of Industries: 1 No. of Occupations: 2 No. of Employees: 794 (estimated) No. of Female Employees: 419 (estimated)

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癸氟奋乃静安全信息

[ 危害码 (欧洲) ]:
Xn

[ 危险品运输编码 ]:
UN 3249

[ RTECS号 ]:
HE0525000

[ 包装等级 ]:
II

[ 危险类别 ]:
6.1(a)

[ 海关编码 ]:
3003909090

癸氟奋乃静海关

[ 海关编码 ]: 3003909090

癸氟奋乃静文献

Adherence challenges and long-acting injectable antipsychotic treatment in patients with schizophrenia.

J. Psychosoc. Nurs. Ment. Health Serv. 51(3) , 13-8, (2013)

Medication nonadherence has been associated with persistence of psychotic symptoms, relapse, and hospitalization in patients with schizophrenia. Patients with untreated psychosis are significantly les...

Ten year outcomes of outpatients with schizophrenia on conventional depot antipsychotics: a systematic chart review.

Int. Clin. Psychopharmacol. 28(5) , 261-6, (2013)

Long-term follow-up data of patients with schizophrenia on depot antipsychotics have been few and the longest follow-up period has been up to 7 years. We carried out a systematic chart review to exami...

Differing effects of antipsychotic medications on substance abuse treatment patients with co-occurring psychotic and substance abuse disorders.

Am. J. Addict. 15(2) , 166-73, (2006)

This retrospective study of patients treated in a ninety-day, inpatient, dual-diagnosis treatment program examined antipsychotic effectiveness in this population using length of stay in treatment and ...

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