Astemizole-d3

Astemizole-d3 is the deuterium labeled Astemizole. Astemizole (R 43512), a second-generation antihistamine drug 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

[1189961-39-4]

UNSPSC

12352005

Target

Histamine Receptor; Isotope-Labeled Compounds; Potassium Channel

Related Pathways

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

Field of Research

Inflammation/Immunology; Endocrinology

Purity

97.78

Solubility

10 mM in DMSO

Smiles

[2H]C([2H])([2H])OC(C=C1)=CC=C1CCN(CC2)CCC2NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F

Molecular Formula

C28H28D3FN4O

Molecular Weight

461.59

References & Citations

[1]Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53 (2) :211-216. |[2]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.|[3]Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28 (1) :38-61.