Background:

Pizotifen (malate) (BC-105 (malate)) is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site.

Pizotifen is a potent 5-HT2 receptor antagonist, with a high affinity for 5-HT1C binding site[1]. Pizotifen is an antidepresent 5-HT2A receptor antagonist and has the capacity to inhibit serotonin-enhanced ADP-induced platelet aggregation[2].

The weights of the fetuses are significantly reduced by all administered doses of Pipethiadene and Pizotifen malate; the weights of the placentas are significantly reduced after 0.6 and 1.2 mg/kg Pipethiadene and only after the middle dose of Pizotifen malate. The means of the implantations, live, dead fetuses, resorptions and the occurrence of external, skeletal and visceral anomalies do not differ from the control group. The number of chromosome aberrations in the bone marrow cells of treated mice does not differ significantly from the negative control group. The micronucleus test reveals no elevation in the frequency of micronuclei as compared to the control group. After the two higher doses of both Pipethiadene and Pizotifen maleate, the mitotic indices are lower than in the control group[3].

参考文献:
[1]. Mylecharane EJ, et al. 5-HT2 receptor antagonists and migraine therapy. J Neurol. 1991;238 Suppl 1:S45-52.
[2]. Lin OA, et al. The antidepressant 5-HT2A receptor antagonists pizotifen and cyproheptadine inhibit serotonin-enhanced platelet function. PLoS One. 2014 Jan 23;9(1):e87026.
[3]. Ujházy E, et al. Teratological and cytogenetical evaluation of two antihistamines (pipethiadene and pizotifen maleate) in mice. Agents Actions. 1988 Apr;23(3-4):376-8.