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Merck
CN

SML0119

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:
87848-99-5
Molecular Weight:
348.44
MDL number:
MFCD00869830
UNSPSC Code:
12352200
PubChem Substance ID:
329825170
NACRES:
NA.77

Key Documents

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Quality Level

100

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 H1-receptor antagonist.
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

Regulatory Information

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Certificates of Analysis (COA)

Lot/Batch Number
0000321748
0000321748
052M4713V
0000040978
0000040979

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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
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
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)
R N Brogden et al.
Drugs, 41(6), 927-940 (1991-06-01)
Acrivastine is a short acting histamine H1-receptor antagonist with a rapid onset of action. 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
F J de Abajo et al.
British journal of clinical pharmacology, 47(3), 307-313 (1999-04-24)
To quantify and compare the incidence of ventricular arrhythniias associated with the use of five nonsedating antihistamines: acrivastine, astemizole, cetirizine, loratadine and terfenadine. The effects of age, sex, dose, duration of treatment, and the interaction with P450 inhibitor drugs were
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