Effects on Migraine Headache of MDL 72,222, an Antagonist at Neuronal 5-HT Receptors. Double-Blind, Placebo-Controlled Study

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Abstract
MDL 72,222 (1aH, 5aH-tropan-3a-yl 3,5-dichlorobenzoate), a novel agent with antagonist activity at neuronal 5-HT receptors, was tested as an acute treatment for migraine pain under double-blind, placebo-controlled conditions. Forty-seven patients with common (n = 29) or classical (n = 8) migraine or mixed type with or without a psychogenic component (n = 10) received 20–40 mg MDL 72,222 (n = 24) or placebo (n = 23) intravenously during the headache phase of a migraine attack. MDL 72,222 was consistently superior to placebo in rapidly alleviating the migraine pain. The treatment was remarkably well tolerated. The results are consistent with the hypothesis that the pain of migraine is related to activation of neuronal 5-HT receptors and suggest that compounds such as MDL 72,222, which block neuronal 5-HT receptors, could be useful new therapeutic agents for the management of migraine.