68844-77-9
68844-77-9
Chemical Structure
Astemizole
Synonym(s): R 43512
- CAS No.: 68844-77-9
- Formula:C28H31FN4O
- Molecular Weight:458.57
IUPAC Name: 1-(4-fluorobenzyl)-N-(1-(4-methoxyphenethyl)piperidin-4-yl)-1H-benzo[d]imidazol-2-amine
InChIKey: GXDALQBWZGODGZ-UHFFFAOYSA-N
SMILES: COC1=CC=C(CCN2CCC(NC3=NC4=CC=CC=C4N3CC5=CC=C(F)C=C5)CC2)C=C1
Biological Activity: 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].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
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Astemizole | 99.77% | 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. | ||||||||||||||||||||
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Astemizole (Standard) | ≥98% | Astemizole (Standard) is the analytical standard of Astemizole. This product is intended for research and analytical applications. 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. | ||||||||||||||||||||
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References
- [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. [Content Brief]
- [2]. Richards DM, et al. Astemizole. A review of its pharmacodynamic properties and therapeutic efficacy. Drugs. 1984 Jul;28(1):38-61. [Content Brief]
