Denaverine hydrochloride - CAS 3321-06-0
Catalog number:
3321-06-0
Category:
Inhibitor
Not Intended for Therapeutic Use. For research use only.
Molecular Formula:
C24H34ClNO3
Molecular Weight:
419.99
COA:
Inquire
Targets:
Phosphodiesterase (PDE)
Description:
Denaverine hydrochloride is a phosphodiesterase inhibitor.Denaverine hydrochloride is applied in relaxation and delatation of birth canal in animals and spasms in humans for its anticholinergic effects.
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Brife Description:
phosphodiesterase inhibitor,Phosphodiesterase (PDE),dilatation of the birth canal,spasms
Purity:
>98%
Appearance:
solid powder
Synonyms:
2-(dimethylamino)ethyl 2-(2-ethylbutoxy)-2,2-diphenylacetate; UNII-2AFK8FCD4R;Spasmalgan; Spasmalgan (TN); 2AFK8FCD4R
Solubility:
Soluble in DMSO.
Storage:
Store in a cool and dry place and at0-4℃ for short term(days to weeks)or -66℃ for long term(months to years).
MSDS:
Inquire
Application:
A phosphodiesterase inhibitor used for dilatation of the birth canal and spasms.
Shelf Life:
2 years
Boiling Point:
489.9°Cat760mmHg
InChIKey:
RSDBEODKTNUEMS-UHFFFAOYSA-N
InChI:
InChI=1S/C24H33NO3.ClH/c1-5-20(6-2)19-28-24(21-13-9-7-10-14-21,22-15-11-8-12-16-22)23(26)27-18-17-25(3)4;/h7-16,20H,5-6,17-19H2,1-4H3;1H
Canonical SMILES:
CCC(CC)COC(C1=CC=CC=C1)(C2=CC=CC=C2)C(=O)OCCN(C)C.Cl
1.Denaverine hydrochloride and carbetocin increased welfare during and after parturition and enhanced subsequent fertility in cattle.
Zobel R1, Taponen J2. J Dairy Sci. 2014;97(6):3570-7. doi: 10.3168/jds.2013-7535. Epub 2014 Apr 14.
The objectives of the current study were to investigate the influence of denaverine hydrochloride and carbetocin on softening and dilatation of the birth canal, the need for assistance during parturition, calf mortality, retention of fetal membranes, endometritis, and subsequent fertility. Altogether 200 animals (100 cows and 100 heifers) of the Simmental breed were divided into 2 groups: treatment (n = 100) and control (n = 100). Animals in the treatment group received denaverine hydrochloride and carbetocin (a maximum of twice for each, depending on the progression of labor) during delivery over a maximum of 4 waiting periods (30 min each), whereas control animals experienced the same waiting periods but received no treatment. The treatment protocol had a positive influence on the ease of calving and postpartum reproductive health. The treatment increased the number of animals with the birth canal dilated by more than 25 cm, and halved the need for any assistance at parturition.
2.A validated high-performance liquid chromatographic assay for the simultaneous determination of denaverine and its N-monodemethyl metabolite in human plasma.
Staab A1, Scheithauer S, Fieger-Büschges H, Mutschler E, Blume H. J Chromatogr B Biomed Sci Appl. 2001 Feb 25;751(2):221-8.
An isocratic reversed-phase high-performance liquid chromatographic method for the simultaneous determination of denaverine and its N-monodemethyl metabolite (MD 6) in human plasma is described. The assay involves the extraction with an n-heptane-2-propanol mixture (9:1, v/v) followed by back extraction into 12.5% (w/w) phosphoric acid. The analytes of interest and the internal standard were separated on a Superspher RP8 column using a mobile phase of acetonitrile-0.12 M NH4H2PO4-tetrahydrofuran (24:17.2:1, v/v), adjusted to pH 3 with 85% (w/w) phosphoric acid. Ultraviolet detection was used at an operational wavelength of 220 nm. The retention times of MD 6, denaverine and the internal standard were 5.1, 6.3 and 10.2 min, respectively. The assay was validated according to international requirements and was found to be specific, accurate and precise with a linear range of 2.5-150 ng/ml for denaverine and MD 6. Extraction recoveries for denaverine and MD 6 ranged from 44 to 49% and from 42 to 47%, respectively.
3.Pharmacokinetics and bioavailability of denaverine hydrochloride in healthy subjects following intravenous, oral and rectal single doses.
Staab A1, Schug BS, Larsimont V, Elze M, Thümmler D, Mutschler E, Blume H. Eur J Pharm Sci. 2003 Feb;18(2):121-8.
The neurotropic-musculotropic spasmolytic agent denaverine hydrochloride is used mainly in the treatment of smooth muscle spasms of the gastrointestinal and urogenital tract. Despite its commercial availability as a solution for intravenous or intramuscular administration (ampoule) and as a suppository formulation, no pharmacokinetic data in man was available to date. Therefore, the objectives of this clinical trial were to determine the basic pharmacokinetic parameters of denaverine after intravenous administration, to assess the feasibility of using the oral route of administration and to characterise the bioavailability of the suppository formulation. To achieve this, healthy subjects received 50 mg denaverine hydrochloride intravenously, orally and rectally in aqueous solutions and rectally as suppository in an open, randomised crossover design. Total body clearance, volume of distribution at steady-state and half-life of denaverine are 5.
4.Myometrial response to neurotropic and musculotropic spasmolytic drugs in an extracorporeal perfusion model of swine uteri.
Künzel J1, Geisler K, Hoffmann I, Müller A, Beckmann MW, Dittrich R. Reprod Biomed Online. 2011 Jul;23(1):132-40. doi: 10.1016/j.rbmo.2011.03.026. Epub 2011 Apr 15.
To compare the effects of neurotropic and musculotropic spasmolytic drugs in isolated swine uterus specimens, 80 swine uteri were perfused using an established model for preserving a viable organ that responds to oxytocic hormones and spasmolytic drugs. An intrauterine catheter was used to record pressure changes. Following initiation of rhythmic uterine contractions and recording of spontaneous rhythmic contractions, spasmolytic drugs (butylscopolamine, atropine, denaverine, morphine, metamizole, pethidine and celandine) were administered at various concentrations. The musculotropic relaxant denaverine in particular showed significant results (P ≤ 0.05) for all dosages and parameters investigated. In terms of muscle physiology, musculotropic agents (denaverine and celandine) have clear advantages in comparison with neurotropic (butylscopolamine and atropine) or musculoneurotropic (morphine, metamizole and pethidine) spasmolytic drugs for inhibiting contractions.
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CAS 3321-06-0 Denaverine hydrochloride

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