Astemizole

Astemizole (R 43512), a second-generation antihistamine agent to diminish allergic symptoms with a long duration of action, is a histamine H1-receptor antagonist, with an IC50 of 4 nM. Astemizole also shows potent hERG K+ channel blocking activity with an IC50 of 0.9 nM. Astemizole has antipruritic effects[1][2].

Product Specifications

CAS Number

[68844-77-9]

Product Name Alternative

R 43512

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Histamine Receptor; Potassium Channel

Type

Reference compound

Related Pathways

GPCR/G Protein; Immunology/Inflammation; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Endocrinology

Assay Protocol

https://www.medchemexpress.com/astemizole.html

Purity

99.77

Solubility

DMSO : 125 mg/mL (ultrasonic)

Smiles

COC1=CC=C(CCN2CCC(NC3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C=C1

Molecular Formula

C28H31FN4O

Molecular Weight

458.57

Precautions

H302, H315, H319, H335

References & Citations

[1]Laduron PM, et al. In vitro and in vivo binding characteristics of a new long-acting histamine H1 antagonist, astemizole. Mol Pharmacol. 1982 Mar;21 (2) :294-300.|[2]Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28 (1) :38-61.|[3]Ikuo Horii, et al. Development of telemetry system in the common marmoset--cardiovascular effects of astemizole and nicardipine. J Toxicol Sci. 2002 May;27 (2) :123-30.|[4]Hiroko Izumi-Nakaseko, et al. Possibility as an anti-cancer drug of astemizole: Evaluation of arrhythmogenicity by the chronic atrioventricular block canine model. J Pharmacol Sci. 2016 Jun;131 (2) :150-3.