Pizotifen is a clinically effective anti-migraine agent with potent anti-serotonin and anti-histamine properties. Pizotifen is equipotent in blocking contractions of the canine basilar artery induced by serotonin, norepinephrine or calcium chloride. As a result, the primary action of pizotifen in the canine basilar artery system appears to be calcium channel blockade and not selective antagonism of serotonin or norepinephrine. Calcium channel blocking ability may be related to the clinical efficacy of pizotifen in the treatment of migraine.
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