Cyclizine, a piperazine-derivative, is a potent and selective histamine H1 receptor antagonist. Cyclizine can be used for the research of nausea, vomiting, and dizziness[1][2][3].
Cyclizine (100 μM) significantly inhibits nitrite accumulation and iNOS protein levels in the LPS-stimulated in RAW 264.7 cells supernatants[1].Cyclizine inhibits anti-IgE-induced histamine release from isolated human lung fragments, with an IC50 of 5.42 µM[2].
Cyclizine (1, 10 mg/kg) enhances locomotor activity of mice in a dose-dependent manner[3].
[1]. KrÁlovÁ J, et, al. The effects of H1-antihistamines on the nitric oxide production by RAW 264.7 cells with respect to their lipophilicity. Int Immunopharmacol. 2009 Jul;9(7-8):990-5.
[2]. Church MK, et, al. Inhibition of histamine release from human lung in vitro by antihistamines and related drugs. Br J Pharmacol. 1980 Aug;69(4):663-7.
[3]. Leza JC, et, al. Effects of antihistaminics on locomotor activity in mice. Comparison with opiate and amphetamine-induced hyperactivity. Gen Pharmacol. 1991;22(2):293-6.