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Purity: ≥98%
Ritodrine HCl (DU21220; DU21220; ST51015115; ST-51015115; Pre-Par; Utopar), the hydrochloride salt of ritodrine, is a β-2 adrenergic receptor agonist used to treat premature labor.
| Targets |
β2-adrenergic receptor
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| ln Vivo |
Background:
Beta-adrenergic agonists are commonly used to arrest premature labor. Although treatment of preterm labor with these agents can delay delivery by 24 to 48 hours, the potential risks and benefits to the mother and infant before and after delivery have not been adequately assessed. Methods: We randomly assigned 708 women with preterm labor at six hospitals to receive an intravenous infusion of either the beta-adrenergic agonist ritodrine (n = 352) or placebo (n = 356). Assignment was made with stratification according to four categories of gestational age (20 to 23 weeks, 24 to 27 weeks, 28 to 31 weeks, and 32 to 35 weeks). The primary objective was to assess the effect of ritodrine on perinatal mortality. Secondary objectives were the evaluation of the causes of perinatal death, the extent to which delivery was delayed with ritodrine, and the effects on birth weight, maternal morbidity, neonatal morbidity, and infant morbidity at 18 months of postnatal age, corrected for preterm delivery. Results: Among the 771 infants born to the women in the study (including 63 pairs of twins), there were 23 deaths (6.1 percent) in the ritodrine group and 25 deaths (6.4 percent) in the placebo group (event-rate difference, -0.3 percent; 95 percent confidence interval, -3.7 percent to 3.1 percent). There was no difference between the groups in the extent of delay of delivery, the incidence of delivery before 37 weeks' gestation, the proportion of babies weighing less than 2500 g, or measures of neonatal morbidity. Maternal morbidity (such as chest pain and cardiac arrhythmias) occurred more frequently but not exclusively in the ritodrine group. One infant born to a woman in the ritodrine group and five infants born to women in the placebo group had cerebral palsy (P = 0.09). There was a slight but not significant trend toward an improved score on the Bayley Psychomotor Development Index at 18 months of age among the infants of the ritodrine-treated women. Conclusions: We found that the use of ritodrine in the treatment of preterm labor had no significant beneficial effect on perinatal mortality, the frequency of prolongation of pregnancy to term, or birth weight.[1] |
| References |
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| Additional Infomation |
Ritodrine Hydrochloride is the hydrochloride salt form of ritodrine, a phenethylamine derivative with tocolytic activity. Ritodrine hydrochloride binds to and activates beta-2 adrenergic receptors of myocytes in the uterine myometrium, which results in decreased intensity and frequency of uterine contraction. Specifically, ritodrine hydrochloride probably activates adenyl cyclase, thereby increasing production of cyclic adenosine monophosphate (cAMP), which in turn enhancing the efflux of calcium from vascular smooth muscle cells. A lack of intracellular calcium prevents uterine myometrial contraction. In addition, this agent may directly inactivate myosin light chain kinase, a critical enzyme necessary for the initiation of muscle contractions.
An adrenergic beta-2 agonist used to control PREMATURE LABOR. |
| Molecular Formula |
C17H22CLNO3
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|---|---|---|
| Molecular Weight |
323.81
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| Exact Mass |
323.128
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| Elemental Analysis |
C, 63.06; H, 6.85; Cl, 10.95; N, 4.33; O, 14.82
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| CAS # |
23239-51-2
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| Related CAS # |
Ritodrine; 26652-09-5; Ritodrine-d3 hydrochloride
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| PubChem CID |
3040551
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| Appearance |
White to off-white solid powder
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| Density |
1.213 g/cm3
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| Boiling Point |
512.3ºC at 760 mmHg
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| Melting Point |
192-196ºC
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| Flash Point |
175.6ºC
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| Vapour Pressure |
2.55E-11mmHg at 25°C
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| LogP |
3.544
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| Hydrogen Bond Donor Count |
5
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
6
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| Heavy Atom Count |
22
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| Complexity |
284
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| Defined Atom Stereocenter Count |
2
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| SMILES |
Cl[H].O([H])[C@]([H])(C1C([H])=C([H])C(=C([H])C=1[H])O[H])[C@]([H])(C([H])([H])[H])N([H])C([H])([H])C([H])([H])C1C([H])=C([H])C(=C([H])C=1[H])O[H]
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| InChi Key |
IDLSITKDRVDKRV-XHXSRVRCSA-N
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| InChi Code |
InChI=1S/C17H21NO3.ClH/c1-12(17(21)14-4-8-16(20)9-5-14)18-11-10-13-2-6-15(19)7-3-13;/h2-9,12,17-21H,10-11H2,1H3;1H/t12-,17-;/m0./s1
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| Chemical Name |
4-[2-[[(1R,2S)-1-hydroxy-1-(4-hydroxyphenyl)propan-2-yl]amino]ethyl]phenol;hydrochloride
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.71 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.1 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.71 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 17.1 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.71 mg/mL (5.28 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. Solubility in Formulation 4: 50 mg/mL (154.41 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.0882 mL | 15.4412 mL | 30.8823 mL | |
| 5 mM | 0.6176 mL | 3.0882 mL | 6.1765 mL | |
| 10 mM | 0.3088 mL | 1.5441 mL | 3.0882 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00679705 | Completed | Drug: Ritodrine Drug: Atosiban Drug: Placebo |
Healthy | University Hospital, Ghent | May 2008 | Phase 1 |
| NCT02538718 | Completed | Drug: MgSO4 Drug: YTP(Ritodrine) |
Preterm Labor | Seoul National University Hospital |
September 22, 2015 | Not Applicable |
| NCT03040752 | Completed | Drug: Nifedipine 20 Mg Drug: Ritodrine Oral Tablet |
Preterm Birth | Cairo University | January 2015 | Phase 4 |
| NCT00290173 | Completed | Drug: efficacy of oral ritodrine in maintaining uterine quiescence |
Pregnancy | University of Zagreb | August 2005 | Not Applicable |
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