54556-98-8

• 常用中文名：盐酸丙哌维林
• 常用英文名：Propiverine hydrochloride
• CAS号：54556-98-8
• 分子式：C₂₃H₃₀ClNO₃
• 分子量：403.942
• 相关类别： 原料药 泌尿系统用药 尿崩症用药
• 发布时间：2018-04-15 08:00:00
• 更新时间：2024-01-04 19:24:44
• 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。

名称

• 中文名: 盐酸丙哌维林
• 英文名: Propiverine Hydrochloride
• 中文别名: 罗匹外宁; 1-甲基-4-哌啶基二苯基丙氧乙酸酯盐酸盐
• 英文别名: Mictonetten; Mictonorm; Propiverine hydrochloride; Propiverine Hydrochlorride; 1-Methyl-4-piperidinyl diphenyl(propoxy)acetate hydrochloride (1:1); Propiverine HCl; UNII-DC4GZD10H3; Benzeneacetic acid, α-phenyl-α-propoxy-, 1-methyl-4-piperidinyl ester, hydrochloride (1:1); 1-Methylpiperidin-4-yl diphenyl(propoxy)acetate hydrochloride (1:1)

物化性质

• 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

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.

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

安全

• 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

合成路线

106-52-5 94686-44-9 ~% 54556-98-8

文献：WO2011/114195 A1, ; Page/Page column 6-7 ;

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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%