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Merck
CN

SML0119

Acrivastine

≥98% (HPLC)

别名:

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

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关于此项目

经验公式(希尔记法):
C22H24N2O2
化学文摘社编号:
分子量:
348.44
NACRES:
NA.77
PubChem Substance ID:
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Quality level:
Storage condition:
desiccated
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产品名称

Acrivastine, ≥98% (HPLC)

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 string

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

InChI key

PWACSDKDOHSSQD-IUTFFREVSA-N

assay

≥98% (HPLC)

form

powder

storage condition

desiccated

color

white to beige

solubility

DMSO: >2 mg/mL (warmed)

storage temp.

2-8°C

Quality Level

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.

存储类别

11 - Combustible Solids

wgk

WGK 3

flash_point_f

Not applicable

flash_point_c

Not applicable

法规信息

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分析证书(COA)

Lot/Batch Number

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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
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)
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
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.

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