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MedKoo Cat#: 584314 | Name: Acrivastine
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Acrivastine is a short acting histamine H1-receptor antagonist with a rapid onset of action and reduced sedating potential. Double-blind clinical trials have shown acrivastine (usually 8mg three times daily) to be an effective and well tolerated antihistamine in the treatment of chronic urticaria and allergic rhinitis.

Chemical Structure

Acrivastine
Acrivastine
CAS#87848-99-5

Theoretical Analysis

MedKoo Cat#: 584314

Name: Acrivastine

CAS#: 87848-99-5

Chemical Formula: C22H24N2O2

Exact Mass: 348.1838

Molecular Weight: 348.45

Elemental Analysis: C, 75.83; H, 6.94; N, 8.04; O, 9.18

Price and Availability

Size Price Availability Quantity
10mg USD 350.00 2 Weeks
25mg USD 650.00 2 Weeks
50mg USD 950.00 2 Weeks
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Related CAS #
No Data
Synonym
Acrivastine; BW 825C
IUPAC/Chemical Name
2-Propenoic acid, 3-(6-(1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl)-2-pyridinyl)-, (E,E)-
InChi Key
PWACSDKDOHSSQD-IUTFFREVSA-N
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+
SMILES Code
O=C(O)/C=C/C1=NC(/C(C2=CC=C(C)C=C2)=C/CN3CCCC3)=CC=C1
Appearance
Solid powder
Purity
>95% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO (2 mg/mL)
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info

Preparing Stock Solutions

The following data is based on the product molecular weight 348.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
1: Neittaanmäki H, Fräki JE, Gibson JR. Comparison of the new antihistamine acrivastine (BW 825C) versus cyproheptadine in the treatment of idiopathic cold urticaria. Dermatologica. 1988;177(2):98-103. PubMed PMID: 2901993. 2: Bojkowski CJ, Gibbs TG, Hellstern KH, Major EW, Mullinger B. Acrivastine in allergic rhinitis: a review of clinical experience. J Int Med Res. 1989;17 Suppl 2:54B-68B. Review. PubMed PMID: 2570003. 3: Ballmer-Weber BK, Gex-Collet C, Wüthrich B. Inhibition of histamine or allergen-induced wheals by a single dose of acrivastine, fexofenadine or cetirizine. J Investig Allergol Clin Immunol. 1999 Nov-Dec;9(6):351-5. PubMed PMID: 10664928. 4: Davadra PM, Dabhi B, Singh MK, Jain MR, Joshi HS, Bapodra AH. Chromatographic separation and spectroscopic characterization of the E/Z isomers of acrivastine. Chirality. 2011 Nov;23(10):955-60. doi: 10.1002/chir.21022. Epub 2011 Sep 26. PubMed PMID: 21953883. 5: He JC, Feng EF, Liu M, Li HL, Tian M, Zhang Q, Dong LC, Xu GL. Development and validation of a liquid chromatography-tandem mass spectrometry method for the simultaneous determination of acrivastine and pseudoephedrine in human plasma and its application in pharmacokinetics. Arzneimittelforschung. 2012 Oct;62(10):449-56. doi: 10.1055/s-0032-1314877. Epub 2012 Aug 30. PubMed PMID: 22936420. 6: Gibbs TG, McDonnell KA, Stokes T, Graham AA. Acrivastine in two doses compared with placebo in a multicentre, parallel group study for the treatment of seasonal allergic rhinitis. Br J Clin Pract. 1989 Jan;43(1):11-4. PubMed PMID: 2574054. 7: Gouda AA, Hashem H, Jira T. Development and validation of a rapid stability indicating HPLC-method using monolithic stationary phase and two spectrophotometric methods for determination of antihistaminic acrivastine in capsules. Spectrochim Acta A Mol Biomol Spectrosc. 2014 Sep 15;130:480-7. doi: 10.1016/j.saa.2014.04.015. Epub 2014 Apr 18. PubMed PMID: 24813276. 8: Gervais P, Bruttman G, Pedrali P, Charpin J, Michel FB, Grilliat JP. French multicentre double-blind study to evaluate the efficacy and safety of acrivastine as compared with terfenadine in seasonal allergic rhinitis. J Int Med Res. 1989;17 Suppl 2:47B-53B. PubMed PMID: 2570002. 9: Fernández Torres R, Callejón Mochón M, Jiménez Sánchez JC, Bello López MA, Guiraúm Perez A. Electrochemical behaviour and determination of acrivastine in pharmaceuticals and human urine. J Pharm Biomed Anal. 2002 Nov 7;30(4):1215-22. PubMed PMID: 12408912. 10: McNulty MJ, Deal DL, Nelson FR, Weller S, Chandrasurin P, Shockcor J, Findlay JW. Disposition of acrivastine in the male beagle dog. Drug Metab Dispos. 1992 Sep-Oct;20(5):679-87. PubMed PMID: 1358572. 11: Balasubramanian R, Klein KB, Pittman AW, Liao SH, Findlay JW, Frosolono MF. Pharmacokinetics of acrivastine after oral and colonic administration. J Clin Pharmacol. 1989 May;29(5):444-7. PubMed PMID: 2567739. 12: Lang DG, Wang CM, Wenger TL. Terfenadine alters action potentials in isolated canine Purkinje fibers more than acrivastine. J Cardiovasc Pharmacol. 1993 Sep;22(3):438-42. PubMed PMID: 7504135. 13: Cohen AF, Hamilton MJ, Peck AW. The effects of acrivastine (BW825C), diphenhydramine and terfenadine in combination with alcohol on human CNS performance. Eur J Clin Pharmacol. 1987;32(3):279-88. PubMed PMID: 2885203. 14: Ramaekers JG, O'Hanlon JF. Acrivastine, terfenadine and diphenhydramine effects on driving performance as a function of dose and time after dosing. Eur J Clin Pharmacol. 1994;47(3):261-6. PubMed PMID: 7867679. 15: Petersen LJ, Bindslev-Jensen C, Poulsen LK, Malling HJ. Time of onset of action of acrivastine in the skin of pollen-allergic subjects. A double-blind, randomized, placebo-controlled comparative study. Allergy. 1994 Jan;49(1):27-30. PubMed PMID: 7911009. 16: Rolan PE, Adams J, Posner J. Comparison of the onset of H1-antagonism with acrivastine and terfenadine by histamine bronchial challenge in volunteers. J Int Med Res. 1989;17 Suppl 2:35B-39B. PubMed PMID: 2570000. 17: Leyh F, Harvey SG, Gibson JR, Manna VK. A comparison of acrivastine versus clemastine and placebo in the treatment of patients with chronic idiopathic urticaria. J Int Med Res. 1989;17 Suppl 2:22B-24B. PubMed PMID: 2569997. 18: Dockhorn RJ, Williams BO, Sanders RL. Efficacy of acrivastine with pseudoephedrine in treatment of allergic rhinitis due to ragweed. Ann Allergy Asthma Immunol. 1996 Feb;76(2):204-8. PubMed PMID: 8595542. 19: Nielsen L, Johnsen CR, Bindslev-Jensen C, Poulsen LK. Efficacy of acrivastine in the treatment of allergic rhinitis during natural pollen exposure: onset of action. Allergy. 1994 Sep;49(8):630-6. PubMed PMID: 7653742. 20: Lahti A, Haapaniemi T. Initiation of the effects of acrivastine and cetirizine on histamine-induced wheals and itch in human skin. Acta Derm Venereol. 1993 Oct;73(5):350-1. PubMed PMID: 7904400.

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