Pimethixene is antihistamine and antiserotonergic compound, acts as an antimigraine agent. Pimethixene is a highly potent antagonist of 5-HT 1A , 5-HT 2A , 5-HT 2B , 5-HT 2C , histamine H 1 , dopamine D 2 and D 4.4 as well as muscarinic M 1 and M 2 receptors, with pK i s of 7.63, 10.22, 10.44, 8.42, 10.14, 8.19, 7.54, 8.61 and 9.38, respectively.
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