Pizotifen malate is a highly selective 5-HT receptor blocking agent, which is a benzocycloheptane based drug.
Target: 5-HT receptor
Pizotifen, malate is a benzocycloheptane based drug used as a medicine, primarily as a preventative to reduce the frequency of recurrent migraine headaches. Pizotifen malate proved to be a highly selective 5-HT receptor blocking agent both in vivo (on saphenous veins) and in vitro (on saphenous veins and basilar arteries) from dogs and humans.
Three groups of pregnant mice were treated daily with oral doses (0.24, 0.6 and 1.2 mg/kg) of pipethiadene and pizotifen malate from day 4 to day 16 of gestation. The following parameters were investigated: reproductive health of the dams, external, skeletal and visceral malformations of fetuses and frequencies of micronuclei and chromosome aberrations in bone marrow cells of dams. Oral administration of Pipethiadene or Pizotifen maleate produced no teratogenic effects. However, the significant reduction of fetal weight after all doses of Pipethiadene or Pizotifen maleate was found to correlate well with the decreased values of the mitotic indices of bone marrow cells of mice.
Toxicity: sedation; dry mouth; drowsiness; increased appetite and weight gain

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