Doxazosin Mesylateα1-adrenergic receptor antagonist CAS# 77883-43-3 |
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Quality Control & MSDS
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| Cas No. | 77883-43-3 | SDF | Download SDF |
| PubChem ID | 62978 | Appearance | Powder |
| Formula | C24H29N5O8S | M.Wt | 547.58 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | UK 33274 | ||
| Solubility | DMSO : 33.33 mg/mL (60.87 mM; Need ultrasonic) H2O : 1 mg/mL (1.83 mM; Need ultrasonic) | ||
| Chemical Name | 4-Amino-2-[4-(1,4-benzodioxan-2-car | ||
| SMILES | COc1cc2nc(nc(N)c2cc1OC)N3CCN(CC3)C(=O)C4COc5ccccc5O4.C[S](O)(=O)=O | ||
| Standard InChIKey | VJECBOKJABCYMF-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C23H25N5O5.CH4O3S/c1-30-18-11-14-15(12-19(18)31-2)25-23(26-21(14)24)28-9-7-27(8-10-28)22(29)20-13-32-16-5-3-4-6-17(16)33-20;1-5(2,3)4/h3-6,11-12,20H,7-10,13H2,1-2H3,(H2,24,25,26);1H3,(H,2,3,4) | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Selective α1-adrenoceptor antagonist (pKi values are 9.0, 8.5 and 8.4 for human α1B, α1A and α1D receptors respectively). Displays antihypertensive activity. |
Doxazosin Mesylate Dilution Calculator
Doxazosin Mesylate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8262 mL | 9.1311 mL | 18.2622 mL | 36.5243 mL | 45.6554 mL |
| 5 mM | 0.3652 mL | 1.8262 mL | 3.6524 mL | 7.3049 mL | 9.1311 mL |
| 10 mM | 0.1826 mL | 0.9131 mL | 1.8262 mL | 3.6524 mL | 4.5655 mL |
| 50 mM | 0.0365 mL | 0.1826 mL | 0.3652 mL | 0.7305 mL | 0.9131 mL |
| 100 mM | 0.0183 mL | 0.0913 mL | 0.1826 mL | 0.3652 mL | 0.4566 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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Doxazosin Mesylate is a selective, long-lasting antagonist of α1-adrenergic receptor [1].
Doxazosin Mesylate has been reported to potentiate contraction response to 5-HT in a dose-dependent manner [1]. Doxazosin significantly reduced alcohol drinking and increased water intake in adult male P rats [2].
Studies has indicated that doxazosin could inhibit TNF-α expression in LPS-induced systemic inflammation model as well as reduce the MCP-1 production in LPS-induced pulmonary inflammation model. Additionally, Doxazosin decreased thickness of footpad in the delayed-type hypersensitivity mice model. Doxazosin had been reported to slightly reduce MCP-1 level in the peritoneal cavity of mice induced by thioglycollate [3].
References:
[1] Zhao Y1, Cao XB, Ren LM. Doxazosin selectively potentiates contraction to serotonin via 5-HT₂A receptors in longitudinal muscle strips of the rabbit gastric body. Can J Physiol Pharmacol. 2014 Mar;92(3):197-204.
[2] O'Neil ML1, Beckwith LE, Kincaid CL, Rasmussen DD. The α1-adrenergic receptor antagonist, doxazosin, reduces alcohol drinking in alcohol-preferring (P) Rats. Alcohol Clin Exp Res. 2013 Feb;37(2):202-12.
[3] Tung D1, Ciallella J, Cheung PH, Saha S. Novel anti-inflammatory effects of doxazosin in rodent models of inflammation. Pharmacology. 2013;91(1-2):29-34.
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[Longbishu Capsule combined with mesylate doxazosin: an efficacious therapy for benign prostatic hyperplasia].[Pubmed:25796693]
Zhonghua Nan Ke Xue. 2015 Feb;21(2):165-9.
OBJECTIVE: To assess the clinical effect and safety of the Chinese medicine Longbishu Capsule combined with mesylate doxazosin in the treatment of benign prostatic hyperplasia (BPH) of the kidney deficiency and blood stagnation type. METHODS: This was a randomized, double-blind, double-simulation control study. We equally assigned 60 men diagnosed with BPH of the kidney deficiency and blood stagnation type to an experimental and a control group, the former treated with mesylate doxazosin plus Longbishu Capsule and the latter with mesylate doxazosin plus placebo. We compared the International Prostate Symptom Score (IPSS), quality of life (QOL), Chinese symptom score (CSS), maximal urinary flow rate (Qmax), and prostate volume between the two groups of patients before and after 6 months of medication. RESULTS: After treatment, there were 5 cured cases, 13 markedly effective cases, 9 effective cases, 1 ineffective case, and 2 eliminated cases in the experimental group, as compared with 2 cured cases, 8 markedly effective cases, 10 effective cases, 7 ineffective cases, and 3 eliminated cases in the control group. The total effectiveness rate was obviously higher in the former (96.4%) than in the latter (74.1%). IPSS, Qmax, and CSS were improved in both of the groups after medication, even more significantly in the experimental than in the control group (IPSS: 15.22 +/- 2.98 vs 18.15 +/- 5.88, P <0.05; Qmax: [13.56 +/- 2.26] ml/s vs [11.78 +/- 2.97] ml/s, P <0.05; CSS: 6.18 +/- 2.13 vs 9.52 +/- 3.15, P <0.05). Because of the difference in the QOL score between the two groups at the baseline (P = 0.038 <0.05), no more comparison was made in this aspect after treatment. CONCLUSION: The combination of Longbishu Capsule with mesylate doxazosin is safe and effective for the treatment of BPH.
Determination of Doxazosin Mesylate in Tablets by RP-HPLC.[Pubmed:22131637]
Indian J Pharm Sci. 2011 Jan;73(1):120-2.
A simple, precise and rapid RP-HPLC method was developed for the determination of Doxazosin Mesylate in pharmaceutical formulations. The method was carried out on a Chromolith RP-C(18) column using a mixture of potassium phosphate buffer and methanol (40:60 v/v) and detection was done at 251 nm. The linearity range was 1-5 mug/ml. The retention time of the drug was 3.8 min. The LOD and LOQ were found to be 0.1 mug/ml and 0.5 mug/ml, respectively.
Preparation and evaluation of sustained-release doxazosin mesylate pellets.[Pubmed:23385960]
Chem Pharm Bull (Tokyo). 2013;61(4):371-8. Epub 2013 Feb 4.
Doxazosin Mesylate (DXM) sustained release pellets were prepared by an extrusion-spheronization and fluid-bed coating technique. The core pellets containing DXM were prepared by extrusion-spheronization technique, and coated by a fluid-bed coater to control the release of DXM. The factors affecting to properties of pellets, such as diluent content, type and coating level of coating agents and plasticizers were studied in the present study. Polymethacrylate derivatives (Eudragit(R) RS PO and RL PO) were used for coating agents, and polyethylene glycol 6000 (PEG 6000), triethyl citrate (TEC) and castor oil were as plasticizers. To evaluate the properties of prepared pellets, the size of prepared pellets was investigated by sieve analysis technique and the morphology of pellets was evaluated by scanning electron microscopy. Through the dissolution test, factors that have an effect on the dissolution of the drug were evaluated. As the content ratio of microcrystalline cellulose (MCC) had increased, the dissolution was proportionally sustained. Eudragit(R) RS PO had more marked sustaining effect on the dissolution rate than Eudragit(R) RL PO, and the effect was more pronounced with the increased coating level. PEG 6000 was an appropriate plasticizer for DXM pellets, and increasing the content of PEG 6000, was also slightly decreasing the dissolution rate.
Determination of Alkyl Methanesulfonates in Doxazosin Mesylate by Gas Chromatography-mass Spectrometer.[Pubmed:22131634]
Indian J Pharm Sci. 2011 Jan;73(1):107-10.
High sensitive rapid gas chromatography-mass spectrometry method for the determination of four carcinogenic alkyl methanesulfonates viz. methyl methanesulfonate, ethyl methanesulfonate, isopropyl methanesulfonate and n-butyl methanesulfonate in Doxazosin Mesylate has been presented by using selective ion monitoring mode. The optimum separation was achieved between methyl methanesulfonate, ethyl methanesulfonate, isopropyl methanesulfonate and n-butyl methanesulfonate on a DB-5 (30 mx0.32 mmx1.0 mum) capillary column under programming temperature. Acetonitrile, water and ammonia (90:9:1 v/v/v) mixture was used as diluent. Various factors involved in the gas chromatography-mass spectrometry method development are also presented. This method was validated as per International Conference on Harmonization guidelines. The limit of quantitation of methyl methanesulfonate, ethyl methanesulfonate, isopropyl methanesulfonate and n-butyl methanesulfonate is 6 ppm with respect to 30 mg/ml of Doxazosin Mesylate.
The alpha 1-adrenoceptor antagonist profile of doxazosin: preclinical pharmacology.[Pubmed:2871857]
Br J Clin Pharmacol. 1986;21 Suppl 1:9S-17S.
The antihypertensive efficacy of the new alpha 1-adrenoceptor antagonist doxazosin is described, and its selectivity for alpha 1-adrenoceptors is reported from both in vivo and in vitro studies. Groups of beagle dogs with chronic perinephritic hypertension were given doxazosin orally, and systolic blood pressure was recorded indirectly from an exteriorized carotid loop. Dogs given doxazosin 0.5 mg kg-1 daily for 10 days showed consistent daily falls in systolic pressure in addition to a progressive reduction in daily pre-dose pressures. A clear indication of antihypertensive action in excess of 24 h post dose was evident. Heart rate changes were minimal. In pentobarbitone anaesthetized dogs pretreated with desimipramine, doxazosin 10-500 micrograms kg-1 i.v. reduced responses of the nictitating membrane to electrical stimulation of the vagosympathetic-depressor nerve trunk (an alpha 1-adrenoceptor response) but had no effect on the chronotropic response of the heart to electrical stimulation of the ansa subclavia. In contrast, the prejunctional alpha 2-adrenoceptor antagonist activity of yohimbine 10-100 micrograms kg-1 i.v. was manifest as a marked dose-related increase in both the heart rate and nictitating membrane responses. The lack of effect of doxazosin on postjunctional alpha 2-adrenoceptors in vivo was demonstrated in the anaesthetized cat. Doxazosin at 50 and 100 micrograms kg-1 i.v. inhibited pressor responses to injected phenylephrine (an alpha 1-adrenoceptor agonist) but had no effect on pressor responses to either alpha-methylnoradrenaline (an alpha 2-adrenoceptor agonist) or angiotensin II.(ABSTRACT TRUNCATED AT 250 WORDS)
