Rizatriptan

Rizatriptan (MK 462 free base) is an orally active 5-HT_1B/5-HT_1D receptor agonist, with BBB permeability. Rizatriptan exerts significant anti-migraine effects by constricting intracranial and extracranial blood vessels and inhibiting neuropeptide release. Rizatriptan exhibits species- and tissue-specific metabolic characteristics; for example, it undergoes oxidative deamination mainly by MAO-A in the liver of brown rats, so co-administration with MAO-A inhibitors is prohibited. Rizatriptan may also exacerbate nitroglycerin-induced cutaneous allodynia, prolong the duration of central sensitization, and increase anxiety-like behavior and active drug-seeking behavior in mice. Rizatriptan has been widely used in studies related to migraine and medication-overuse headache^[1][2]. In Vivo:Rizatriptan (0.02 mg/kg; oral; voluntary free-choice access; during NTG stimulation phase until day 14) exacerbates Nitroglycerin (NTG)-induced cutaneous allodynia, prolongs central sensitization, increases anxiety-like behavior, and drives active medication-seeking behavior in female C57BL/6J mice, with the prelimbic cortex and spinal trigeminal nucleus caudalis acting as key hub brain regions^[1].