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丁二酸洛沙平

丁二酸洛沙平用途

Loxapine琥珀酸盐是D2/D4多巴胺受体,5羟-色胺受体抑制剂。

丁二酸洛沙平名称

[ CAS 号 ]:
27833-64-3

[ 中文名 ]:
丁二酸洛沙平

[ 英文名 ]:
Loxapine succinate

[中文别名 ]:

洛沙平琥珀酸酯

[英文别名 ]:

Daxolin
loxapine succinate salt
MFCD00069298
Loxitane
Cloxazepin
Loxapac
EINECS 248-682-0
Lederle
Loxapine succinate
Loxapine (succinate)

丁二酸洛沙平生物活性

[ 描述 ]:

Loxapine琥珀酸盐是D2/D4多巴胺受体,5羟-色胺受体抑制剂。

[ 相关类别 ]:

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

研究领域 >> 神经疾病

[参考文献]

[1]. Singh AN, et al. A neurochemical basis for the antipsychotic activity of loxapine: interactions with dopamine D1, D2, D4 and serotonin 5-HT2 receptor subtypes. J Psychiatry Neurosci. 1996 Jan;21(1):29-35.

[2]. Labuzek K, et al. Chlorpromazine and loxapine reduce interleukin-1beta and interleukin-2 release by rat mixed glial and microglial cell cultures. Eur Neuropsychopharmacol. 2005 Jan;15(1):23-30.

[3]. Lee T, et al. Loxapine and clozapine decrease serotonin (S2) but do not elevate dopamine (D2) receptor numbers in the rat brain. Psychiatry Res. 1984 Aug;12(4):277-85.

[4]. Kalkman HO, et al. Clozapine inhibits catalepsy induced by olanzapine and loxapine, but prolongs catalepsy induced by SCH 23390 in rats. Naunyn Schmiedebergs Arch Pharmacol. 1997 Mar;355(3):361-4.

[相关活性小分子]

丁二酸洛沙平物理化学性质

[ 沸点 ]:
458.6ºC at 760mmHg

[ 熔点 ]:
150-152°C

[ 分子式 ]:
C₂₂H₂₄ClN₃O₅

[ 分子量 ]:
445.896

[ 闪点 ]:
231.1ºC

[ 精确质量 ]:
445.140442

[ PSA ]:
102.67000

[ LogP ]:
3.01860

[ 外观性状 ]:
白色固体

[ 储存条件 ]:
-20°C Freezer

[ 水溶解性 ]:
H2O: soluble

丁二酸洛沙平毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: WM5750000

CAS REGISTRY NUMBER :: 27833-64-3

LAST UPDATED :: 198910

DATA ITEMS CITED :: 3

MOLECULAR FORMULA :: C18-H18-Cl-N3-O.C4-H6-O4

MOLECULAR WEIGHT :: 445.94

WISWESSER LINE NOTATION :: T C676 BO INJ MG J- AT6N DNTJ D1 &QV2VQ

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 6 mg/kg/2D-I

TOXIC EFFECTS :: Behavioral - toxic psychosis

REFERENCE :: JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978- Volume(issue)/page/year: 44,37,1983

TYPE OF TEST :: LDLo - Lowest published lethal dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 30 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - coma Lungs, Thorax, or Respiration - chronic pulmonary edema

REFERENCE :: CTOXAO Clinical Toxicology. (New York, NY) V.1-18, 1968-81. For publisher information, see JTCTDW. Volume(issue)/page/year: 14,181,1979

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - woman

DOSE/DURATION :: 27 mg/kg/9D-I

TOXIC EFFECTS :: Endocrine - hyperglycemia

REFERENCE :: JCLPDE Journal of Clinical Psychiatry. (Physicians Postgraduate Press, Inc., POB 240008, Memphis, TN 38124) V.39- 1978- Volume(issue)/page/year: 44,347,1983

丁二酸洛沙平安全信息

[ 个人防护装备 ]:
Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter

[ 危害码 (欧洲) ]:
Xi

[ 危险品运输编码 ]:
UN 2811 6.1 / PGII

[ WGK德国 ]:
3

[ RTECS号 ]:
WM5750000

丁二酸洛沙平文献

Investigation of the disposition of loxapine, amoxapine and their hydroxylated metabolites in different brain regions, CSF and plasma of rat by LC–MS/MS

J. Pharm. Biomed. Anal. 58 , 83-93, (2012)

Loxapine represents an interesting example of old “new” drug and is recently drawing attention for its novel inhalation formulation for the treatment of both psychiatric and non-psychiatric disorders....

In vitro aerosol characterization of Staccato(®) Loxapine.

Int. J. Pharm. 403(1-2) , 101-8, (2011)

Medicinal aerosol products (metered dose and dry powder inhalers) require characterization testing over a wide range of use and pre-operating stress scenarios in order to ensure robust product perform...

Inhaled loxapine for agitation revisited: focus on effect sizes from 2 Phase III randomised controlled trials in persons with schizophrenia or bipolar disorder.

Int. J. Clin. Pract. 66(3) , 318-25, (2012)

To describe the efficacy of inhaled loxapine for the treatment of agitation associated with schizophrenia or bipolar disorder using different examples of effect size (ES).Psychopharmacologic Drug Advi...

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