Propiverine hydrochloride

Propiverine hydrochloride is a bladder spasmolytic with calcium antagonistic and anticholinergic properties. Propiverine hydrochloride can be used for the research of overactive blaqdder and urinary incontinence[1][2].

Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel

Signaling Pathways >> Neuronal Signaling >> mAChR

Signaling Pathways >> GPCR/G Protein >> mAChR

Research Areas >> Neurological Disease

Propiverine (10-3000 nM) inhibits the specific binding of [3H]NMS, with Kis of 339, 193 and 497 nM in the bladder, submaxillary gland and heart of mice respectively[2].

Propiverine (0.5 mg/day; p.o. once daily for 2 weeks) significantly increases UBP and LPP during passive intravesical pressure elevation, and also increases plasma norepinephrine and epinephrine levelsin rats[1]. Propiverine (0.01-1 mg/kg; i.v.) decreases the UBP and totally suppresses the sneeze reflex at the dose of 1 mg/kg in vivo[1]. Animal Model: Female adult Sprague-Dawley rats (250-270 g)[1] Dosage: 5 mg dissolved in distilled water (0.5 mL) Administration: P.o. once daily for 2 weeks Result: Increased urethral baseline pressure (UBP) and leak-point pressure (LPP) significantly. Increased plasma epinephrine and norepinephrine levels. No significant changes were observed in body weight.

[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.

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