| Size | Price | Stock | Qty |
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| 10mg |
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| 50mg |
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| 100mg |
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| ln Vivo |
For the treatment of allergic rhinitis and chronic urticaria, avastin (usually 8 mg three times daily) is an efficient and well-tolerated antihistamine. Treating seasonal allergic rhinitis with Avastin is more successful than using a placebo and works similarly to clemastine or terfenadine. Akvastine works similarly to commonly used doses of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine, or terfenadine in the treatment of dermatoses in which histamine plays a causative role. It is also more effective than a placebo. Compared to clemastine, avastin is less drowsy, and its side effect profile is similar to that of terfenadine or placebo [1]. Avastin at doses of 4 mg and 8 mg significantly reduced symptoms of seasonal allergic rhinitis, including scores for runny nose, sneezing, and overall scores. Furthermore, the symptom scores for watery eyes and scratchy throat were decreased by 8 mg of acrivastine. When treating seasonal allergic rhinitis, avastin is well tolerated and works well [2].
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| Animal Protocol |
In guinea-pigs, acrivastine was shown to lack anticholinergic effects [1]
In rats and guinea-pigs, brain:plasma concentration ratio of acrivastine after intravenous administration was 0.02 to 0.05, and after oral administration was 0.03 to 0.2, indicating low CNS penetration [1] The principal metabolite of acrivastine (propionic acid analogue) was tested in guinea-pigs for inhibition of histamine-induced bronchospasm and found to be 2 to 3 times more active than acrivastine [1] |
| ADME/Pharmacokinetics |
Absorption, Distribution and Excretion
Following oral administration, acristatin in the compound capsules is rapidly absorbed, with bioavailability comparable to that of acristatin solution. After administration of SEMPREX-D capsules, peak plasma acristatin concentrations were reached at 1.14 ± 0.23 hours. A mass balance study in seven healthy volunteers indicated that acristatin is primarily excreted via the kidneys. During a 72-hour collection period, approximately 84% of the total administered radioactive material was recovered in urine and approximately 13% in feces, for a total recovery rate of approximately 97%. 0.46 ± 0.05 L/kg 2.9 ± 0.7 mL/min/kg Biological Half-Life Following a single oral dose of acristatin, the mean terminal half-life is 1.9 ± 0.3 hours, increasing to 3.5 ± 1.9 hours at steady state. The terminal half-life of propionic acid metabolite is 3.8 ± 1.4 hours. |
| Toxicity/Toxicokinetics |
Hepatotoxicity
Acristatin has not been found to be associated with elevated liver enzymes or clinically significant liver injury. Its relative safety is likely related to its rapid metabolism and low-dose use. Likelihood Score: E (Unlikely to cause clinically significant liver injury). References regarding the safety and potential hepatotoxicity of antihistamines are listed after the "Antihistamines Overview" section. Drug Category: Antihistamines Effects During Pregnancy and Lactation ◉ Overview of Use During Lactation Small, occasional doses of acristatin are not expected to have any adverse effects on breastfed infants. Larger doses or prolonged use may cause infant drowsiness and other adverse reactions, or reduced milk production, especially when used in combination with sympathomimetic drugs (such as pseudoephedrine) or before lactation is fully established. Non-sedating antihistamines are a better option. ◉ Effects on Breastfed Infants As of the revision date, no published information on acristatin has been found. In a telephone follow-up study, mothers reported that 10% of infants exposed to various antihistamines experienced irritability and colic, and 1.6% experienced lethargy. All adverse reactions did not require medical attention. ◉ Effects on Lactation and Breast Milk Higher doses of injected antihistamines can lower baseline serum prolactin levels in non-lactating women and early postpartum women. However, pre-administration of antihistamines by postpartum mothers does not affect suckling-induced prolactin secretion. Whether lower doses of oral antihistamines have the same effect on serum prolactin, and whether this effect on prolactin has any impact on breastfeeding success, is currently unstudied. Prolactin levels in lactating mothers may not affect their ability to breastfeed. Protein BindingAcrilastine binds to human plasma proteins at a rate of 50 ± 2.0%. |
| References |
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| Additional Infomation |
Acrivastine is a pyridine compound with the structure (pyridin-2-yl)acrylic acid substituted at the 6-position with [(1E)-1-(4-methylphenyl)-3-(pyrrolidine-1-yl)prop-1-en-1-yl]. It is a non-sedating antihistamine used to treat hay fever, urticaria, and rhinitis. It is an H1 receptor antagonist. It is an α,β-unsaturated monocarboxylic acid, belonging to the pyridine class of compounds, and is an N-alkylpyrrolidine, as well as an olefin compound. Acrivastine is a triprolidine analog antihistamine suitable for treating allergies and hay fever. As an H1 receptor antagonist, acrivastine works by blocking the binding of histamine to this receptor, thereby preventing symptoms associated with histamine release, such as itching, vasodilation, hypotension, edema, bronchoconstriction, and tachycardia. Currently, acristatin is used in combination with pseudoephedrine as the FDA-approved combination drug Semprex-D. Acristatin is a histamine-1 receptor antagonist. Its mechanism of action is as a histamine H1 receptor antagonist. Acristatin is a second-generation antihistamine used to treat allergic rhinitis. No clinically significant cases of acute liver injury have been found associated with acristatin. Acristatin is a synthetic alkylamine with non-sedating antihistamine activity. Acristatin limits typical anaphylactic and anaphylactic shock responses, including bronchoconstriction, vasodilation, increased capillary permeability, and gastrointestinal smooth muscle spasms, by competitively blocking histamine H1 receptors. These responses are caused by histamine acting on the bronchi, gastrointestinal smooth muscle, and capillaries. The drug also prevents histamine-induced skin and mucous membrane pain and itching. (NCI05)
Drug Indications For the relief of symptoms associated with seasonal allergic rhinitis, such as sneezing, runny nose, itching, tearing, and nasal congestion. FDA Label |
| Molecular Formula |
C22H24N2O2
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| Molecular Weight |
348.4382
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| Exact Mass |
348.183
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| CAS # |
87848-99-5
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| Related CAS # |
Acrivastine-d7;172165-56-9
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| PubChem CID |
5284514
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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 |
555.1±50.0 °C at 760 mmHg
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| Melting Point |
55.5-59.5 °C(lit.)
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| Flash Point |
289.5±30.1 °C
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| Vapour Pressure |
0.0±1.6 mmHg at 25°C
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| Index of Refraction |
1.627
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| LogP |
4.55
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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 |
6
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| Heavy Atom Count |
26
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| Complexity |
514
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1C=CC(C)=CC=1)(\C1C=CC=C(/C=C/C(=O)O)N=1)=C/CN1CCCC1
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| InChi Key |
PWACSDKDOHSSQD-IUTFFREVSA-N
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| InChi Code |
InChI=1S/C22H24N2O2/c1-17-7-9-18(10-8-17)20(13-16-24-14-2-3-15-24)21-6-4-5-19(23-21)11-12-22(25)26/h4-13H,2-3,14-16H2,1H3,(H,25,26)/b12-11+,20-13+
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| Chemical Name |
(E)-3-[6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-yl]prop-2-enoic acid
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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 |
| 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) |
DMSO : ~50 mg/mL (~143.50 mM)
H2O : ~1 mg/mL (~2.87 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (7.17 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 25.0 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: ≥ 2.5 mg/mL (7.17 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 25.0 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: ≥ 2.5 mg/mL (7.17 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.8699 mL | 14.3497 mL | 28.6993 mL | |
| 5 mM | 0.5740 mL | 2.8699 mL | 5.7399 mL | |
| 10 mM | 0.2870 mL | 1.4350 mL | 2.8699 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 |
| NCT01732510 | TERMINATEDWITH RESULTS | Drug: MK-8226 Drug: Placebo |
Atopic Dermatitis | Merck Sharp & Dohme LLC | 2012-12-21 | Phase 1 |
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