| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| 500mg | |||
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| Targets |
Alpha-1 adrenoceptor. Dapiprazole hydrochloride is a potent, selective, and orally active alpha-1 adrenoceptor antagonist. It displays preference for α1A and α1D receptors over α1B receptors. By blocking alpha-adrenergic receptors in the smooth muscle of blood vessels, gastrointestinal tract, and radial smooth muscle of the iris, it causes vasodilation.
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| ln Vitro |
Dapiprazole hydrochloride is a potent alpha-1 adrenoceptor antagonist. It blocks alpha-adrenergic receptors in the smooth muscle of blood vessels, gastrointestinal tract, and radial smooth muscle of the iris, resulting in vasodilation. It suppresses opioid withdrawal symptoms and inhibits amphetamine toxicity. It produces sedation, blocks conditioned avoidance reflexes, and reduces the response to noxious stimuli.
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| ln Vivo |
In mice, dapirazole hydrochloride injections (once intraperitoneal or intravenous; 0–10 mg/kg or 0–3 mg/mouse) lessen the overall severity of opiate withdrawal symptoms [1].
Dapiprazole hydrochloride is used as eye drops for reversing mydriasis after eye examination. It is orally active and suppresses opioid withdrawal symptoms. It inhibits amphetamine toxicity and alcohol and morphine withdrawal syndromes. It produces sedation and reduces the response to noxious stimuli. |
| Enzyme Assay |
Dapiprazole hydrochloride is evaluated in cell-free receptor binding assays using membrane preparations expressing alpha-1 adrenoceptor subtypes. Radioligand binding displacement assays are performed to determine the affinity and selectivity of Dapiprazole for α1A, α1B, and α1D receptors. Competition binding experiments are conducted with increasing concentrations of Dapiprazole and fixed concentrations of labeled reference ligands.
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| Cell Assay |
Dapiprazole hydrochloride is assessed in cell-based functional assays using cells expressing alpha-1 adrenoceptors. Calcium mobilization or other signaling assays are performed to measure receptor antagonism. The compound displays preference for α1A and α1D receptors over α1B receptors.
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| Animal Protocol |
Animal/Disease Models: Swiss albino male CD-1 mouse, body weight 20 -25 g, acute dependence model [1]
Doses: 5, 7.5 and 10 mg/kg (ip) or 0.5, 1 and 3 mg/mouse (icv ), single Route of Administration: intraperitoneal (ip) injection or intracerebroventricular administration, single Experimental Results:diminished jumping behavior, head shaking, and paw shaking when administered before naloxone. Dapiprazole hydrochloride is administered orally or as eye drops in animal models. It is used to reverse mydriasis and to study opioid withdrawal symptoms. The compound suppresses opioid withdrawal symptoms and inhibits amphetamine toxicity. It produces sedation and reduces the response to noxious stimuli. |
| ADME/Pharmacokinetics |
Dapiprazole hydrochloride has a molecular weight of 361.91 and a molecular formula of C19H27N5·HCl. It has a CAS number of 72822-13-0. The compound is soluble in DMSO at 20 mg/mL. It should be stored as a powder at -20°C for up to 3 years. It is an alpha-1 adrenoceptor antagonist.
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| Toxicity/Toxicokinetics |
No detailed toxicity data is available for Dapiprazole hydrochloride beyond its known use as an ophthalmic agent. The compound is used as eye drops for reversing mydriasis after eye examination. It is generally well-tolerated for ophthalmic use. The compound is for therapeutic use and is not for research purposes only.
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| References | |
| Additional Infomation |
Dapiprazole hydrochloride is an alpha-adrenergic antagonist that works by blocking alpha-adrenergic receptors in blood vessels (arteries, arterioles, and veins), the gastrointestinal tract, and the radial smooth muscle of the iris. This prevents smooth muscle contraction, leading to vasodilation. Dapiprazole hydrochloride eye drops can cause pupillary constriction. In the heart, it may antagonize alpha-adrenergic receptors in cardiomyocytes, producing a mild negative inotropic effect.
See also: Dapiprazole (containing the active ingredient). Dapiprazole hydrochloride is a potent, selective, and orally active alpha-1 adrenoceptor antagonist. It has a molecular weight of 361.91 and a molecular formula of C19H27N5·HCl. The compound has a CAS number of 72822-13-0. It is used as eye drops for reversing mydriasis after eye examination. It suppresses opioid withdrawal symptoms and inhibits amphetamine toxicity. It displays preference for α1A and α1D receptors over α1B receptors. The compound is for therapeutic use. |
| Molecular Formula |
C19H27N5.HCL
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|---|---|
| Molecular Weight |
361.91212
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| Exact Mass |
361.203
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| CAS # |
72822-13-0
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| Related CAS # |
Dapiprazole;72822-12-9
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| PubChem CID |
6917787
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| Appearance |
White to off-white solid powder
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| Density |
1.2±0.1 g/cm3
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| Boiling Point |
538.9±60.0 °C at 760 mmHg
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| Flash Point |
279.7±32.9 °C
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| Vapour Pressure |
0.0±1.4 mmHg at 25°C
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| Index of Refraction |
1.658
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| LogP |
2.44
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
4
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| Heavy Atom Count |
25
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| Complexity |
395
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
ZIODNPFQZIHCOE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C19H27N5.ClH/c1-16-6-2-3-7-17(16)23-14-12-22(13-15-23)11-9-19-21-20-18-8-4-5-10-24(18)19;/h2-3,6-7H,4-5,8-15H2,1H3;1H
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| Chemical Name |
3-[2-[4-(2-methylphenyl)piperazin-1-yl]ethyl]-5,6,7,8-tetrahydro-[1,2,4]triazolo[4,3-a]pyridine;hydrochloride
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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. |
| 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) |
H2O : ~100 mg/mL (~276.31 mM)
DMSO : ~12.5 mg/mL (~34.54 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: 50 mg/mL (138.16 mM) in PBS (add these co-solvents sequentially from left to right, and one by one), clear solution; with sonication.
(Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.7631 mL | 13.8156 mL | 27.6312 mL | |
| 5 mM | 0.5526 mL | 2.7631 mL | 5.5262 mL | |
| 10 mM | 0.2763 mL | 1.3816 mL | 2.7631 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.
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