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Key Documents

SML0119

Sigma-Aldrich

Acrivastine

≥98% (HPLC)

Synonym(s):

(E)-6-((E)-3-(1-Pyrrolidinyl)-1-p-tolylpropenyl)-2-pyridineacrylic acid

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About This Item

Empirical Formula (Hill Notation):
C22H24N2O2
CAS Number:
Molecular Weight:
348.44
MDL number:
UNSPSC Code:
12352200
PubChem Substance ID:
NACRES:
NA.77

Quality Level

Assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: >2 mg/mL (warmed)

storage temp.

2-8°C

SMILES string

Cc1ccc(cc1)\C(=C/CN2CCCC2)c3cccc(\C=C\C(O)=O)n3

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+

InChI key

PWACSDKDOHSSQD-IUTFFREVSA-N

Gene Information

human ... HRH1(3269)

Application

Acrivastine has been used as an antihistamine to investigate the relation between the increased residence time of antihistamine at the histamine H1 receptor (H1R) and the duration of effective target-inhibition by this antagonist.

Biochem/physiol Actions

Acrivastine is a second-generation antihistamine, an H1-receptor antagonist.
Acrivastine is a second-generation antihistamine. It is a derivative of first-generation compound triprolidine. Acrivastine is effectively used for treating allergic diseases including cholinergic urticaria and histamine-medicated dermatoses.

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable


Certificates of Analysis (COA)

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R D Mann et al.
BMJ (Clinical research ed.), 320(7243), 1184-1186 (2000-04-28)
To investigate the frequency with which sedation was reported in post-marketing surveillance studies of four second generation antihistamines: loratadine, cetirizine, fexofenadine, and acrivastine. Prescription-event monitoring studies. Prescriptions were obtained for each cohort in the immediate post-marketing period. Event data were
Xiaochen Gu et al.
Journal of pharmaceutical and biomedical analysis, 37(4), 663-667 (2005-03-31)
High-performance liquid chromatography (HPLC) was used for the simultaneous quantification of the H(1)-antihistamine acrivastine and the decongestant pseudoephedrine hydrochloride. Both compounds were detected at the wavelength of 214 nm. The influence of the mobile phase and the detection wavelength was
The target residence time of antihistamines determines their antagonism of the G protein-coupled histamine H1 receptor
Bosma R, et al.
Frontiers in Pharmacology, 8(10), 667-667 (2017)
A Reimers et al.
Clinical and experimental allergy : journal of the British Society for Allergy and Clinical Immunology, 32(12), 1763-1768 (2003-03-26)
Leukotriene receptor antagonists have shown some efficacy in t he treatment of asthma. Injection of LTC4, LTD4 and LTE4 into the skin leads to a weal-and-flare reaction, suggesting an involvement of leukotrienes in the pathogenesis of urticaria. Indeed, various reports
M J Mattila et al.
European journal of clinical pharmacology, 55(2), 85-93 (1999-05-21)
Most of the modern non-sedating H1 receptor antagonists (antihistamines) penetrate the brain poorly, allowing the use of doses large enough to counteract allergic processes in peripheral tissues without important central effects. The antihistamines reviewed here are acrivastine, astemizole, cetirizine, ebastine

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