Acrivastine

Names

[ Name ]:
Acrivastine

[Synonym ]:
2-Propenoic acid, 3-[6-[(1E)-1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propen-1-yl]-2-pyridinyl]-, (2E)-
Semprex
(2E)-3-{6-[(1E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-en-1-yl]pyridin-2-yl}prop-2-enoic acid
(E)-6-[(E)-3-(1-Pyrrolidinyl)-1-p-tolylpropenyl]-2-pyridineacrylic Acid
Acrivastine
BW 270C
Acrivastinum
BW A825C
Acrivastina
(E)-3-[6-[(E)-1-(4-methylphenyl)-3-pyrrolidin-1-ylprop-1-enyl]pyridin-2-yl]prop-2-enoic acid
(2E)-3-{6-[(1E)-1-(4-Methylphenyl)-3-(1-pyrrolidinyl)-1-propen-1-yl]-2-pyridinyl}acrylic acid
(2E)-3-{6-[(1E)-1-(4-Methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl]pyridin-2-yl}acrylic acid
MFCD00869830
Acrivastin
Duact
(2E)-3-{6-[(1E)-1-(4-methylphenyl)-3-(pyrrolidin-1-yl)prop-1-en-1-yl]pyridin-2-yl}prop-2-enoic acid
2-propenoic acid, 3-[6-[(1E)-1-(4-methylphenyl)-3-(1-pyrrolidinyl)-1-propenyl]-2-pyridinyl]-, (2E)-
BW 825C

Biological Activity

[Description]:

Acrivastine (BW825C) is a short acting histamine 1 receptor antagonist for the treatment of allergic rhinitis.

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Histamine Receptor

Signaling Pathways >> Immunology/Inflammation >> Histamine Receptor

Research Areas >> Inflammation/Immunology

[In Vivo]

Acrivastine (usually 8mg three times daily) is an effective and well tolerated antihistamine in the treatment of chronic urticaria and allergic rhinitis. Acrivastine is more effective than placebo and similar in efficacy to clemastine or terfenadine in the treatment of seasonal allergic rhinitis. In the treatment of dermatoses in which histamine has a pathogenetic role, the efficacy of acrivastine is superior to that of placebo and similar to that of usual dosages of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine or terfenadine. Acrivastine causes less drowsiness than clemastine, the incidence of adverse effects being indistinguishable from that with placebo or terfenadine[1]. Both 4 mg and 8 mg acrivastine alleviate the symptoms of seasonal allergic rhinitis with significant improvements in the symptom scores for sneezing, running nose and the calculated overall score. In addition, 8 mg acrivastine reduces the symptom scores for watery eyes and itchy throat. Acrivastine is both well tolerated and effective in the treatment of seasonal allergic rhinitis[2].

[References]

[1]. Brogden RN, et al. Acrivastine. A review of its pharmacological properties and therapeutic efficacy in allergic rhinitis, urticaria and related disorders. Drugs. 1991 Jun;41(6):927-40.

[2]. Gibbs TG, et al. 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.

[Related Small Molecules]

Chemical & Physical Properties

[ Density]:
1.2±0.1 g/cm3

[ Boiling Point ]:
555.1±50.0 °C at 760 mmHg

[ Melting Point ]:
55.5-59.5 °C(lit.)

[ Molecular Formula ]:
C₂₂H₂₄N₂O₂

[ Molecular Weight ]:
348.438

[ Flash Point ]:
289.5±30.1 °C

[ Exact Mass ]:
348.183777

[ PSA ]:
53.43000

[ LogP ]:
4.55

[ Vapour Pressure ]:
0.0±1.6 mmHg at 25°C

[ Index of Refraction ]:
1.627

[ Storage condition ]:
2-8°C

MSDS

Click to get detail MSDS

Safety Information

[ Hazard Codes ]:
Xn,Xi

[ Risk Phrases ]:
R22:Harmful if swallowed. R43:May cause sensitization by skin contact.

[ Safety Phrases ]:
S37/39

[ RIDADR ]:
NONH for all modes of transport

[ WGK Germany ]:
3

[ RTECS ]:
UD3474000

Synthetic Route

Click to get detail synthetic route

Precursor & DownStream

Precursor

DownStream

Articles

Identification of novel functional inhibitors of acid sphingomyelinase.

PLoS ONE 6 , e23852, (2011)

We describe a hitherto unknown feature for 27 small drug-like molecules, namely functional inhibition of acid sphingomyelinase (ASM). These entities named FIASMAs (Functional Inhibitors of Acid Sphing...

Simultaneous analysis of the H1-antihistamine acrivastine and the decongestant pseudoephedrine hydrochloride by high-performance liquid chromatography.

J. Pharm. Biomed. Anal. 37(4) , 663-7, (2005)

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...

Onset-of-action for antihistamine and decongestant combinations during an outdoor challenge.

Ann. Allergy Asthma Immunol. 84(4) , 451-9, (2000)

Medications containing a combination antihistamine-decongestant are commonly used for allergic rhinitis yet onset-of-action comparisons for symptom relief after a single dose have not been performed.T...