Phentolamine MesylateAlpha 1/2-blocking agent CAS# 65-28-1 |
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Quality Control & MSDS
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Chemical structure
3D structure
| Cas No. | 65-28-1 | SDF | Download SDF |
| PubChem ID | 91430 | Appearance | Powder |
| Formula | C18H23N3O4S | M.Wt | 377.46 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Synonyms | Phentolamine methanesulfonate | ||
| Solubility | H2O : ≥ 50 mg/mL (132.46 mM) *"≥" means soluble, but saturation unknown. | ||
| Chemical Name | 3-[N-(4,5-dihydro-1H-imidazol-2-ylmethyl)-4-methylanilino]phenol;methanesulfonic acid | ||
| SMILES | Cc1ccc(cc1)N(CC2=NCCN2)c3cccc(O)c3.C[S](O)(=O)=O | ||
| Standard InChIKey | OGIYDFVHFQEFKQ-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C17H19N3O.CH4O3S/c1-13-5-7-14(8-6-13)20(12-17-18-9-10-19-17)15-3-2-4-16(21)11-15;1-5(2,3)4/h2-8,11,21H,9-10,12H2,1H3,(H,18,19);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 | Non-selective adrenergic α receptor antagonist (pKB = 8.07). Intravenous injection causes hypotension and tachycardia in rats. Intraperitoneal injection in mice increases plasma FGF21 levels. |
Phentolamine Mesylate Dilution Calculator
Phentolamine Mesylate Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 2.6493 mL | 13.2464 mL | 26.4929 mL | 52.9857 mL | 66.2322 mL |
| 5 mM | 0.5299 mL | 2.6493 mL | 5.2986 mL | 10.5971 mL | 13.2464 mL |
| 10 mM | 0.2649 mL | 1.3246 mL | 2.6493 mL | 5.2986 mL | 6.6232 mL |
| 50 mM | 0.053 mL | 0.2649 mL | 0.5299 mL | 1.0597 mL | 1.3246 mL |
| 100 mM | 0.0265 mL | 0.1325 mL | 0.2649 mL | 0.5299 mL | 0.6623 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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Phentolamine Mesylate is a alpha 1- and alpha 2-blocking agent. Phentolamine leads to an increase in FBM by preferentially antagonizing presynaptic alpha 2-adrenoreceptors over postsynaptic alpha 1-adrenoreceptors. This influence of phentolamine on FBM ma
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Effectiveness and safety of phentolamine mesylate in routine dental care.[Pubmed:28126226]
J Am Dent Assoc. 2017 Mar;148(3):149-156.
BACKGROUND: Phentolamine Mesylate (PM) is widely used to reverse local anesthesia after dental procedures. Limited knowledge is available regarding effectiveness and safety in routine dental practice. METHODS: The authors conducted 2 national, prospective, noninterventional, postauthorization effectiveness studies (OraVerse Post-Authorization Efficacy Study [ORAPAES] controlled, OraVerse Non-Interventional Study [ORANIS] uncontrolled) in patients receiving a local anesthetic as part of their dental treatment. They investigated time to recovery of normal sensation and function and the frequency of adverse events (AEs). The authors used Kaplan-Meier methods to analyze times to recovery; in ORAPAES, they used hazard ratios based on Cox models using the control group as a reference. RESULTS: In ORAPAES (n = 856), PM reduced the time to recovery of normal sensation and function with a difference in the median time of 70 and 79 minutes, respectively, with similar results observed in ORANIS (n = 445). In ORAPAES, patients in the PM group had, at any time point, a 2.77-fold higher chance of recovery to normal sensation (hazard ratio, 2.77; 95% confidence interval [CI], 2.35-3.26; P < .001) and for normal function 2.94-fold higher chance of recovery to normal sensation (95% CI, 2.49-3.47; P < .001) than in the control group. The observed incidence of AEs with PM treatment was 8.4% in ORAPAES (95% CI, 6.2-10.9) and 9.7% (95% CI, 7.1-12.7) in ORANIS. No serious AEs occurred. CONCLUSIONS: PM substantially reduced the time to recovery of normal sensation and function after local anesthesia in routine dental treatment. The results confirm the effectiveness, safety, and tolerability of PM used in patients with routine dental conditions in Germany, and that PM augments the safety of dental treatments. PRACTICAL IMPLICATIONS: The authors determined that PM is well suited to reverse local anesthesia after routine dental procedures.
Phase Four, Randomized, Double-Blinded, Controlled Trial of Phentolamine Mesylate in Two- to Five-year-old Dental Patients.[Pubmed:28292340]
Pediatr Dent. 2017 Jan 15;39(1):39-45.
PURPOSE: The purpose of this study was to evaluate, using a randomized, double-blind methodology: (1) the safety of Phentolamine Mesylate (Oraverse) in accelerating the recovery of soft tissue anesthesia following the injection of two percent lidocaine plus 1:100,000 epinephrine in two- to five-year-olds; and (2) efficacy in four- to five-year-olds only. METHODS: One hundred fifty pediatric dental patients underwent routine dental restorative procedures with two percent lidocaine plus 1:100,000 epinephrine with doses based on body weight. Phentolamine Mesylate or a sham injection (two to one ratio) was then administered. Subjects were monitored for safety and, in four- to five-year-olds, for efficacy during the two-hour evaluation period. RESULTS: There were no significant differences in adverse events between the phentolamine and sham injections. Compared to sham, phentolamine was not associated with nerve injury, increased analgesic use, or abnormalities of the oral cavity. Phentolamine was associated with transient decreased blood pressure in some children. In four- and five-year-olds, phentolamine induced more rapid recovery of lip anesthesia by 48 minutes (P<0.0001). CONCLUSIONS: Phentolamine was well tolerated and safe in three- to five-year-olds; in four- to five-year-olds, a statistically significant more rapid recovery of lip sensation compared to sham injections was determined.
Phentolamine mesylate: It's role as a reversal agent for unwarranted prolonged local analgesia.[Pubmed:26381625]
J Indian Soc Pedod Prev Dent. 2015 Oct-Dec;33(4):265-8.
Administration of local anesthesia is an integral procedure prior to dental treatments to minimize the associated pain. It is learned that its effect stays more than the time required for the dental procedure to be completed. This prolonged soft tissue anesthesia (STA) can be detrimental, inconvenient, and unnecessary. Phentolamine Mesylate, a Food and Drug Administration-approved drug essentially serves the purpose of faster recovery from numbness at the site of local anesthesia. This article reviews the development of the drug Phentolamine Mesylate and its indication as a local anesthetic reversal agent. A literature search for Phentolamine Mesylate as a STA reversal agent was conducted in PubMed using the terms "dental local anesthesia reversal, Phentolamine Mesylate" up to March 2014. The search was limited to articles published in English. The search revealed 13 PubMed indexed articles stating the development and application of Phentolamine Mesylate. Phentolamine Mesylate is an important step in the progress of developing patient care as well as an aid to the dental clinician.
Phentolamine mesylate to reverse oral soft-tissue local anesthesia: A systematic review and meta-analysis.[Pubmed:26409985]
J Am Dent Assoc. 2015 Oct;146(10):751-9.e3.
BACKGROUND: Knowing that patients desire reduced duration of local anesthesia, the authors performed a meta-analysis to evaluate the efficacy of Phentolamine Mesylate (PM) in reducing anesthesia duration and the occurrence of adverse effects. TYPES OF STUDIES REVIEWED: The authors searched studies in 4 electronic databases up to December 18, 2014. For each study, the methodological quality was assessed according to the Cochrane Collaboration's tool for assessing risk of bias. Randomized controlled trials (RCTs) that used PM met the inclusion criteria. RESULTS: Six RCTs met the inclusion criteria and were used to carry out a meta-analysis of the effectiveness of PM and a qualitative analysis of its adverse effects. The use of PM was more effective in reversing the anesthetic effect on the lower lip and tongue than was applying a placebo. Adverse effects reported in the studies were not statistically significant, the most frequent being headache, pain during injection, and postprocedure pain. CONCLUSIONS AND PRACTICAL IMPLICATIONS: Based on limited evidence, PM is effective in reducing the persistence of anesthesia duration on the lower lip and tongue, with infrequent adverse effects of little clinical significance.
