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Merck

SML0119

Sigma-Aldrich

Acrivastine

≥98% (HPLC)

Sinónimos:

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

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About This Item

Fórmula empírica (notación de Hill):
C22H24N2O2
Número de CAS:
Peso molecular:
348.44
Número MDL:
Código UNSPSC:
12352200
ID de la sustancia en PubChem:
NACRES:
NA.77

Nivel de calidad

Ensayo

≥98% (HPLC)

Formulario

powder

condiciones de almacenamiento

desiccated

color

white to beige

solubilidad

DMSO: >2 mg/mL (warmed)

temp. de almacenamiento

2-8°C

cadena SMILES

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+

Clave InChI

PWACSDKDOHSSQD-IUTFFREVSA-N

Información sobre el gen

human ... HRH1(3269)

Aplicación

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.

Acciones bioquímicas o fisiológicas

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.

Código de clase de almacenamiento

11 - Combustible Solids

Clase de riesgo para el agua (WGK)

WGK 3

Punto de inflamabilidad (°F)

Not applicable

Punto de inflamabilidad (°C)

Not applicable


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Ilari Paakkari
Toxicology letters, 127(1-3), 279-284 (2002-06-08)
Although the new second-generation nonsedative antihistamines terfenadine and astemizole were launched as highly selective and specific H(1)-receptor antagonists, they were later found to cause prolongation of the QT-interval and severe cardiac arrhythmias. The prolongation of the QT-interval is caused by
K Wieland et al.
The Journal of biological chemistry, 274(42), 29994-30000 (1999-10-09)
We combined in a previously derived three-dimensional model of the histamine H(1) receptor (Ter Laak, A. M., Timmerman, H., Leurs, H., Nederkoorn, P. H. J., Smit, M. J., and Donne-Op den Kelder, G. M. (1995) J. Comp. Aid. Mol. Design.
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
B K Ballmer-Weber et al.
Journal of investigational allergology & clinical immunology, 9(6), 351-355 (2000-02-09)
Certirizine, a potent H1-blocking agent, is often recommended as an emergency drug in anaphylactic reactions because of its well documented fast onset of action. In this randomized, cross-over study we compared the onset of action after a single dose of

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