1189961-39-4
Chemical Structure
Astemizole-d3
- CAS No.: 1189961-39-4
- Formula:C28H28D3FN4O
- Molecular Weight:461.59
IUPAC Name: 1-(4-fluorobenzyl)-N-(1-(4-(methoxy-d3)phenethyl-d3)piperidin-4-yl)-1H-benzo[d]imidazol-2-amine
InChIKey: GXDALQBWZGODGZ-FIBGUPNXSA-N
SMILES: [2H]C([2H])([2H])OC(C=C1)=CC=C1CCN(CC2)CCC2NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F
Biological Activity: 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].
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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. | |||||||||||||||||||||
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References
- [1]. Russak EM, et al. Impact of Deuterium Substitution on the Pharmacokinetics of Pharmaceuticals. Ann Pharmacother. 2019;53(2):211-216. [Content Brief]
- [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. [Content Brief]
