For research use only. Not for therapeutic Use.
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].
Astemizole (p.o., 10 and 30 mg/kg) and (i.v., 1 and 3 mg/kg) has no effect on respiratory rate, heart rate and blood pressure, and even at high doses of 30 mg/kg and 3 mg/kg, also has no effect on body temperature and exercise capacity in male common marmosets. But Astemizole can prolong the QT interval and induce premature ventricular contractions at 30 mg/kg (po) and 1 mg/kg (iv)[3].
Astemizole (p.o., 3 and 30 mg/kg) shows that the pre-drug control values (C) of the idioventricular rate, QT interval and QTcF are 31 beats/min, 319 ms and 256 at dose of 3 mg/kg, while those are 31 beats/min, 331 ms and 270 at dose of 30 mg/kg, respectively in mice. Moreover, Astemizole at a dose of 30 mg/kg (po) may cause tip-twisting ventricular tachycardia by inhibiting hERG K+ channels[4].
| Catalog Number | R009677 |
| CAS Number | 68844-77-9 |
| Synonyms | 1-[(4-fluorophenyl)methyl]-N-[1-[2-(4-methoxyphenyl)ethyl]piperidin-4-yl]benzimidazol-2-amine |
| Molecular Formula | C28H31FN4O |
| Purity | ≥95% |
| InChI | InChI=1S/C28H31FN4O/c1-34-25-12-8-21(9-13-25)14-17-32-18-15-24(16-19-32)30-28-31-26-4-2-3-5-27(26)33(28)20-22-6-10-23(29)11-7-22/h2-13,24H,14-20H2,1H3,(H,30,31) |
| InChIKey | GXDALQBWZGODGZ-UHFFFAOYSA-N |
| SMILES | COC1=CC=C(C=C1)CCN2CCC(CC2)NC3=NC4=CC=CC=C4N3CC5=CC=C(C=C5)F |
| Reference | [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. |
