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氧托溴铵

氧托溴铵用途

Oxitropium bromide是毒蕈碱受体拮抗剂。它是一种用于治疗哮喘和慢性阻塞性肺疾病的抗胆碱能支气管扩张剂药物。

氧托溴铵名称

[ CAS 号 ]:
30286-75-0

[ 中文名 ]:
氧托溴铵

[ 英文名 ]:
Oxitropium Bromide

[英文别名 ]:

Oxivent
Oxitropium
Oxitropium bromide
Ba-253-BR-L
Ventilat
oxytropium bromide
Bromure d'oxitropium

氧托溴铵生物活性

[ 描述 ]:

Oxitropium bromide是毒蕈碱受体拮抗剂。它是一种用于治疗哮喘和慢性阻塞性肺疾病的抗胆碱能支气管扩张剂药物。

[ 相关类别 ]:

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

信号通路 >> 神经信号通路 >> mAChR

研究领域 >> 炎症/免疫

[ 靶点 ]

mAChR[1]

[体外研究]

Oxitropium bromide是一种毒蕈碱拮抗剂,可阻断musucarinic乙酰胆碱受体(mAChR)。未经处理的膈肌的氧托溴铵和注射内毒素的膈肌孵育不会增加体外剂量依赖性的力-频率曲线;然而,它会导致两种类型的肌肉都抗疲劳[1]。

[体内研究]

吸入氧化溴化物在吸入后2小时将力-频率曲线向上移动,并抑制体内注射内毒素引起的力-频率曲线的减少[1]。 Oxitropium bromide强烈且持续地抑制乙酰胆碱(ACh)诱导的抗性。溴化氧噻嗪溴化物可以防止组胺,5-羟色胺,白三烯D4或抗原诱导的耐药性增加[2]。以1.5μg或更高的剂量吸入抗胆碱能药物氧托溴铵可大大减少静脉注射组胺产生的粘液评分的降低,但吸入的组胺不会减少[3]。

[动物实验]

小鼠：在氧托溴铵吸入组中，动物通过75-mL间隔物从氧托溴铵MDI（计量吸入器）吸入2次，然后解剖膈肌并立即测量收缩性，1小时，2小时和4小时后（每组n = 5只动物）。将动物置于离心管（内径= 30mm）中，在底部具有圆孔（直径= 10mm），其鼻和嘴通过孔暴露以进行呼吸。氧托溴铵MDI（定量吸入器）将2次喷射释放到与管连接的间隔物中。吸入氧托溴铵气雾约10秒钟，而动物则通过管孔自发呼吸[1]。

[参考文献]

[1]. Shindoh C, et al. Effects of inhalation or incubation of oxitropium bromide on diaphragm muscle contractility in mice. Allergol Int. 2011 Sep;60(3):365-72.

[2]. Kohno SW, et al. Effect of oxitropium bromide (Ba253) on increased airway resistance induced by various agonists and antigen in the guinea pig. Jpn J Pharmacol. 1989 Aug;50(4):455-66.

[3]. Takeyama K, et al. Effect of oxitropium bromide on histamine-induced airway goblet cell secretion. Am J Respir Crit Care Med. 1996 Jul;154(1):231-6.

[相关活性小分子]

氧托溴铵物理化学性质

[ 熔点 ]:
203-204° (dec)

[ 分子式 ]:
C₁₉H₂₆BrNO₄

[ 分子量 ]:
412.31800

[ 精确质量 ]:
411.10500

[ PSA ]:
59.06000

[ 储存条件 ]:
-20°C，密闭，干燥

氧托溴铵毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: RN7090000

CHEMICAL NAME :: 3-Oxa-9-azoniatricyclo(3.3.1.0(sup 2,4))nonane, 9-ethyl-7-(3-hydroxy-1-oxo-2-phenylpropoxy)- 9-methyl-, bromide, (7(S)-(1-alpha,2-beta,4-beta,5-alpha,7-beta))-

CAS REGISTRY NUMBER :: 30286-75-0

LAST UPDATED :: 199512

DATA ITEMS CITED :: 16

MOLECULAR FORMULA :: C19-H26-N-O4.Br

MOLECULAR WEIGHT :: 412.37

WISWESSER LINE NOTATION :: T C356 A AK DOTJ A2 A1 HOVYR&1Q &E

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 :: 2250 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,117,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 19 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,353,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1600 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,117,1979

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1150 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,117,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 25700 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,117,1979

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 3 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,117,1979

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 40 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - changes in motor activity (specific assay) Lungs, Thorax, or Respiration - other changes

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,353,1988

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: >8 gm/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 35,435,1985

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 34 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: DRFUD4 Drugs of the Future. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1975/76- Volume(issue)/page/year: 4,117,1979 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 55 gm/kg/13W-C

TOXIC EFFECTS :: Nutritional and Gross Metabolic - weight loss or decreased weight gain

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,353,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 17 gm/kg/78W-C

TOXIC EFFECTS :: Gastrointestinal - decreased motility or constipation Related to Chronic Data - death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,353,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 2730 mg/kg/13W-C

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - conjunctive irritation Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol)

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 36,353,1988 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 55 gm/kg

SEX/DURATION :: male 10 week(s) pre-mating female 2 week(s) pre-mating female 1-7 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 - Fertility - post-implantation mortality (e.g. dead and/or resorbed implants per total number of implants) Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 37,413,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 6600 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 37,413,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 7800 mg/kg

SEX/DURATION :: female 17-21 day(s) after conception lactating female 21 day(s) post-birth

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

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 37,413,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 2600 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: OYYAA2 Oyo Yakuri. Pharmacometrics. (Oyo Yakuri Kenkyukai, CPO Box 180, Sendai 980-91, Japan) V.1- 1967- Volume(issue)/page/year: 37,413,1989

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