盐酸双环维林

盐酸双环维林用途

Dicyclomine hydrochloride 是一种有效的口服活性毒蕈碱胆碱能受体 (muscarinic cholinergic receptors) 拮抗剂。Dicyclomine hydrochloride 对 M1 受体亚型 (Ki=5.1 nM) 和 M2 受体亚型 (Ki=54.6 nM) 在刷缘膜和基底质膜中均表现出较高的亲和力。Dicyclomine hydrochloride是一种抗痉挛试剂,在体内可缓解胃肠道平滑肌痉挛。

点击显示

盐酸双环维林名称

[ CAS 号 ]:
67-92-5

[ 中文名 ]:
盐酸双环维林

[ 英文名 ]:
Dicyclomine hydrochloride

[中文别名 ]:

盐酸双环胺

[英文别名 ]:

Dicyclomine, Hydrochloride

盐酸双环维林生物活性

[ 描述 ]:

[ 相关类别 ]:

信号通路 >> 神经信号通路 >> mAChR

信号通路 >> G 蛋白偶联受体/G 蛋白 >> 由mAChR

研究领域 >> 神经疾病

[ 靶点 ]

Ki: 5.1 nM (muscarinic M1 receptor subtype in brush-border membrane) Ki: 54.6 nM (muscarinic M2 receptor subtype in basal plasma membrane[1]

[体内研究]

盐酸双环胺(腹腔注射；8mg/kg；每日)在所有测量中均加重认知损害。此外,双环胺治疗的3xTg AD小鼠的记忆障碍比双环胺治疗的非转基因小鼠更严重[2]。盐酸双环胺(腹腔注射；2.0、4.0和8.0 mg/kg；7天)对配对伙伴学习(PAL)任务的表现有非常显著的影响老鼠。还有低剂量全身治疗显示小鼠在空间任务中的行为障碍[3]。动物模型：C57Bl/6小鼠[1]剂量：2.0、4.0和8.0 mg/kg给药：腹腔注射；每日；7天结果：由于药物在海马体外的作用而产生损伤。

[参考文献]

[1]. J Pavía,et al. Pharmacological Characterization and Distribution of Muscarinic Receptors in Human Placental Syncytiotrophoblast Brush-Border and Basal Plasma Membranes. Eur J Pharmacol. . 1997 Feb 12;320(2-3):209-14.

[2]. Antonella Caccamo, et al. M1 Receptors Play a Central Role in Modulating AD-like Pathology in Transgenic Mice. 2006 Mar 2;49(5):671-82.doi: 10.1016/j.neuron.2006.01.020.

[3]. Susan J Bartko,et al. A Computer-Automated Touchscreen Paired-Associates Learning (PAL) Task for Mice: Impairments Following Administration of Scopolamine or Dicyclomine and Improvements Following Donepezil.Psychopharmacology (Berl). 2011 Mar;214(2):537-48.

盐酸双环维林物理化学性质

[ 沸点 ]:
399.8ºC at 760 mmHg

[ 熔点 ]:
164-166ºC

[ 分子式 ]:
C₁₉H₃₆ClNO₂

[ 分子量 ]:
345.94800

[ 闪点 ]:
116.5ºC

[ 精确质量 ]:
345.24300

[ PSA ]:
29.54000

[ LogP ]:
5.20420

[ 外观性状 ]:
powder | off-white

[ 储存条件 ]:
通风低温干燥

[ 水溶解性 ]:
H2O: 50 mg/mL

盐酸双环维林MSDS

详细MSDS(安全技术说明书)

盐酸双环维林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: DT7350000

CHEMICAL NAME :: (Bicyclohexyl)-1-carboxylic acid, 2-(diethylamino)ethyl ester, hydrochloride

CAS REGISTRY NUMBER :: 67-92-5

LAST UPDATED :: 199701

DATA ITEMS CITED :: 12

MOLECULAR FORMULA :: C19-H35-N-O2.Cl-H

MOLECULAR WEIGHT :: 346.01

WISWESSER LINE NOTATION :: L6TJ A- AL6TJ AVO2N2&2 &GH

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Human - infant

DOSE/DURATION :: 1 gm/kg

TOXIC EFFECTS :: Behavioral - rigidity (including catalepsy) Lungs, Thorax, or Respiration - dyspnea Lungs, Thorax, or Respiration - cyanosis

REFERENCE :: BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 288,901,1984

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1290 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Behavioral - muscle weakness Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,1954,1974

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

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 625 mg/kg

TOXIC EFFECTS :: Behavioral - somnolence (general depressed activity) Behavioral - convulsions or effect on seizure threshold

REFERENCE :: JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 39,305,1950

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

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1900 ug/kg

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

REFERENCE :: FSTEAI Farmaco. Scienza e Tecnica. (Pavia, Italy) V.1-7, 1946-52. For publisher information, see FRPSAX. Volume(issue)/page/year: 7,448,1952

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 31500 ug/kg

TOXIC EFFECTS :: Autonomic Nervous System - smooth muscle relaxant (mechanism undefined, spasmolytic)

REFERENCE :: ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 11,1119,1961

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 35 mg/kg

TOXIC EFFECTS :: Behavioral - convulsions or effect on seizure threshold Kidney, Ureter, Bladder - hematuria

REFERENCE :: JAPMA8 Journal of the American Pharmaceutical Association, Scientific Edition. (Washington, DC) V.29-49, 1940-60. For publisher information, see JPMSAE. Volume(issue)/page/year: 39,305,1950 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 26 gm/kg/30D-I

TOXIC EFFECTS :: Liver - hepatitis (hepatocellular necrosis), zonal Blood - normocytic anemia Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,1954,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 39 gm/kg/13W-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Blood - changes in other cell count (unspecified) Related to Chronic Data - death

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,1954,1974

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 31200 mg/kg/26W-I

TOXIC EFFECTS :: Blood - changes in serum composition (e.g. TP, bilirubin, cholesterol) Biochemical - Enzyme inhibition, induction, or change in blood or tissue levels - transaminases Related to Chronic Data - death

REFERENCE :: KSRNAM Kiso to Rinsho. Clinical Report. (Yubunsha Co., Ltd., 1-5, Kanda Suda-Cho, Chiyoda-ku, KS Bldg., Tokyo 101, Japan) V.1- 1960- Volume(issue)/page/year: 8,1954,1974 *** NIOSH STANDARDS DEVELOPMENT AND SURVEILLANCE DATA *** NIOSH OCCUPATIONAL EXPOSURE SURVEY DATA : NOHS - National Occupational Hazard Survey (1974) NOHS Hazard Code - 84599 No. of Facilities: 805 (estimated) No. of Industries: 1 No. of Occupations: 1 No. of Employees: 805 (estimated) NOES - National Occupational Exposure Survey (1983) NOES Hazard Code - 84599 No. of Facilities: 188 (estimated) No. of Industries: 1 No. of Occupations: 4 No. of Employees: 9355 (estimated) No. of Female Employees: 8012 (estimated)

点击显示

盐酸双环维林安全信息

[ 符号 ]:

GHS07

[ 信号词 ]:
Warning

[ 危害声明 ]:
H302-H315-H319-H335

[ 警示性声明 ]:
P301 + P312 + P330-P305 + P351 + P338

[ 个人防护装备 ]:
dust mask type N95 (US);Eyeshields;Gloves

[ 危害码 (欧洲) ]:
Xn

[ 风险声明 (欧洲) ]:
22-36/37/38

[ 安全声明 (欧洲) ]:
26-36

[ 危险品运输编码 ]:
NONH for all modes of transport

[ WGK德国 ]:
3

[ RTECS号 ]:
DT7350000

盐酸双环维林文献

Treating morning sickness in the United States--changes in prescribing are needed.

Am. J. Obstet. Gynecol. 211(6) , 602-6, (2014)

Presently, 97.7% of prescriptions for the treatment of nausea and vomiting in pregnancy in the United States are with medications not labeled for use in pregnancy, not indicated for nausea and vomitin...

Recommendations for the management of Acanthamoeba keratitis.

J. Med. Microbiol. 63(Pt 5) , 770-1, (2014)

更多文献