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盐酸丙哌维林

盐酸丙哌维林用途

Propiverine hydrochloride 是具有钙拮抗和抗胆碱能特性的膀胱痉挛剂。Propiverine hydrochloride 可用于研究膀胱过度活动和尿失禁。

盐酸丙哌维林名称

[ CAS 号 ]:
54556-98-8

[ 中文名 ]:
盐酸丙哌维林

[ 英文名 ]:
Propiverine hydrochloride

[中文别名 ]:

[英文别名 ]:

Mictonetten
Mictonorm
Propiverine hydrochloride
Propiverine Hydrochlorride
Propiverine HCl
UNII-DC4GZD10H3

盐酸丙哌维林生物活性

[ 描述 ]:

Propiverine hydrochloride 是具有钙拮抗和抗胆碱能特性的膀胱痉挛剂。Propiverine hydrochloride 可用于研究膀胱过度活动和尿失禁。

[ 相关类别 ]:

信号通路 >> 跨膜转运 >> 钙通道

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

[体外研究]

丙三嗪(10-3000nm)抑制[3H]NMS的特异性结合,小鼠膀胱、颌下腺和心脏的Kis分别为339、193和497nm[2]。

[体内研究]

丙肾上腺素(0.5毫克/天；每天一次,持续2周)在被动膀胱内压升高期间显著增加UBP和LPP,并增加大鼠血浆去甲肾上腺素和肾上腺素水平[1]。在体剂量为1mg/kg时,丙肾上腺素(0.01-1mg/kg；静脉注射)可降低UBP并完全抑制喷嚏反射[1]。动物模型：雌性成年Sprague-Dawley大鼠(250-270g)[1]剂量：5mg溶于蒸馏水(0.5ml)给药：P.o.每日1次,连续2周。结果：尿道基线压(UBP)和漏点压(LPP)显著升高。肾上腺素和肾上腺素水平升高。体重无明显变化。

[参考文献]

[1]. Kitta T, et, al. Effects of propiverine hydrochloride, an anticholinergic agent, on urethral continence mechanisms and plasma catecholamine concentration in rats. Int Urogynecol J. 2013 Apr; 24(4): 683-8.

[2]. Ito Y, et, al. Muscarinic Receptor Binding and Plasma Drug Concentration after the Oral Administration of Propiverine in Mice. Low Urin Tract Symptoms. 2010 Apr; 2(1):43-9.

盐酸丙哌维林物理化学性质

[ 沸点 ]:
494.7ºC at 760 mmHg

[ 熔点 ]:
213-216ºC

[ 分子式 ]:
C₂₃H₃₀ClNO₃

[ 分子量 ]:
403.942

[ 闪点 ]:
253ºC

[ 精确质量 ]:
403.191437

[ PSA ]:
38.77000

[ LogP ]:
4.73410

[ 外观性状 ]:
白色晶体粉末

[ 储存条件 ]:
-20°C Freezer

盐酸丙哌维林毒性和生态

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AH3297000

CHEMICAL NAME :: Acetic acid, diphenylpropoxy-, 1-methyl-4-piperidyl ester, hydrochloride

CAS REGISTRY NUMBER :: 54556-98-8

LAST UPDATED :: 199403

DATA ITEMS CITED :: 6

MOLECULAR FORMULA :: C23-H29-N-O3.Cl-H

MOLECULAR WEIGHT :: 403.99

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 :: GEXXA8 German (East) Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #139212

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

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 29 mg/kg

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

REFERENCE :: GEXXA8 German (East) Patent Document. (U.S. Patent and Trademark Office, Foreign Patents, Washington, DC 20231) Volume(issue)/page/year: #139212 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 18200 mg/kg/1Y-I

TOXIC EFFECTS :: Sense Organs and Special Senses (Eye) - mydriasis (pupillary dilation) Liver - changes in liver weight Endocrine - changes in pituitary weight

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 15,107,1990 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 250 mg/kg

SEX/DURATION :: female 17-21 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 - other neonatal measures or effects

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 14(Suppl 2),221,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 50 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Newborn - behavioral Reproductive - Effects on Newborn - physical Reproductive - Effects on Newborn - delayed effects

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 14(Suppl 2),221,1989

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 250 mg/kg

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

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus)

REFERENCE :: JTSCDR Journal of Toxicological Sciences. (Japanese Soc. of Toxicological Sciences, 4th Floor, Gakkai Center Bldg., 4-16, Yayoi 2-chome, Bunkyo-ku, Tokyo 113, Japan) V.1- 1976- Volume(issue)/page/year: 14(Suppl 2),221,1989

盐酸丙哌维林安全信息

[ 符号 ]:

GHS05, GHS07

[ 信号词 ]:
Danger

[ 危害声明 ]:
H315-H318-H335

[ 警示性声明 ]:
P261-P280-P305 + P351 + P338

[ 危害码 (欧洲) ]:
Xi

[ 风险声明 (欧洲) ]:
37/38-41

[ 安全声明 (欧洲) ]:
26-39

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

[ RTECS号 ]:
AH3297000

[ 海关编码 ]:
2933399090

盐酸丙哌维林合成路线

详细合成路线

盐酸丙哌维林上下游产品

盐酸丙哌维林上游产品

盐酸丙哌维林下游产品

盐酸丙哌维林海关

[ 海关编码 ]: 2933399090

[ 中文概述 ]:
2933399090. 其他结构含非稠合吡啶环的化合物. 增值税率:17.0%. 退税率:13.0%. 监管条件:无. 最惠国关税:6.5%. 普通关税:20.0%

[ 申报要素 ]: 品名, 成分含量, 用途, 乌洛托品请注明外观, 6－己内酰胺请注明外观, 签约日期

[ Summary ]:
2933399090. other compounds containing an unfused pyridine ring (whether or not hydrogenated) in the structure. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

盐酸丙哌维林文献

Excitatory effect of propiverine hydrochloride on urethral activity in rats.

Int. J. Urol. 19(6) , 575-82, (2012)

To investigate the effects of the antimuscarinic agent, propiverine, on the bladder and urethra in rats.A total of 54 female rats were given propiverine, imidafenacin (an antimuscarinic agent), or dis...

[Additional effect of propiverine for naftopidil-resistant nocturia in the patient with benign prostate hypertrophy].

Hinyokika Kiyo. 57(2) , 71-6, (2011)

The efficacy and safety of additional administration of propiverine were prospectively studied for naftopidil-resistant nocturia in patients with benign prostatic hypertrophy (BPH). Patients of 50 yea...

An overview on mixed action drugs for the treatment of overactive bladder and detrusor overactivity.

Urol. Int. 89(3) , 259-69, (2012)

To provide an overview on the efficacy, tolerability, safety and health-related quality of life (HRQoL) of drugs with a mixed action used in the treatment of overactive bladder (OAB).MEDLINE database ...

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