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N-methylhistamine is a small molecule and a major metabolite of histamine, formed through the Nτ-methylation of histamine by the enzyme histamine N-methyltransferase. It acts as a potent agonist of the histamine H3 receptor and also exhibits agonist properties at the H4 receptor. This compound has been investigated for its therapeutic potential in migraine prophylaxis, where its H3 receptor agonism is believed to inhibit the neurogenic edema response involved in migraine pathophysiology. It is administered subcutaneously and has undergone clinical trials for this indication.
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