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NEUROLOGY 1984;34:304
© 1984 American Academy of Neurology

The calcium antagonist properties of cyproheptadine

Implications for antimigraine action

Stephen J. Peroutka, MD, PhD and George S. Allen, MD, PhD

From the Departments of Neurology (Dr. Peroutka) and Neurosurgery (Dr. Allen), The Johns Hopkins Hospital, Baltimore, MD.

Cyproheptadine is equipotent (IC50 = 41 to 45 nM) in blocking contractions of canine basilar artery segments induced by serotonin, norepinephrine, potassium, or calcium. Methysergide and amitriptyline display variable potencies in inhibiting contractions depending on the initiating agent. Propranolol, at concentrations to 10 micromolar, had minimal effect on vessel contractions. We conclude that the primary action of cyproheptadine in preventing induced contractions of the canine basilar artery is antagonism of calcium channels. This action is unique among drugs used for migraine prophylaxis and may have important implications for the treatment of headache and other neurologic disorders.

Address all correspondence and reprint requests to Dr. Peroutka, Department of Neurology, The Johns Hopkins Hospital, 600 North Wolfe Street, Baltimore, MD 21205.

Accepted for publication June 13, 1983.




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