Rizatriptan Benzoate

Catalog No.S1607 Synonyms: MK-462 Benzoate

For research use only.

Rizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.

Rizatriptan Benzoate  Chemical Structure

CAS No. 145202-66-0

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Biological Activity

Description Rizatriptan Benzoate (MK-462) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks.
5-HT1 [1]
In vivo Rizatriptan blocks neurogenic vasodilation via an action on 5-HT(1D) receptors located on perivascular trigeminal nerves to inhibit CGRP release in anaesthetized guinea-pigs. Rizatriptan evokes a transient reduction in dural blood vessel diameter which recovered to baseline values within 10 min in anaesthetized guinea-pigs. [1] Rizatriptan significantly inhibits dural plasma protein extravasation produced by high intensity electrical stimulation of the trigeminal ganglion. Rizatriptan significantly reduces electrically stimulated dural vasodilation in anaesthetised rats. [2] Rizatriptan Benzoate significantly reduced SP mRNA levels in the midbrains of normal and model group rats, indicating that Rizatriptan Benzoate can downregulate SP gene expression in the rat midbrain. Rizatriptan Benzoate significantly reduces midbrain PENK mRNA expression, decreasing the levels of midbrain met-enkephalin and leu-enkephalin, and thereby weakening the analgesic effects of the endogenous pain modulatory system in rat model of migraine. [3] Rizatriptan Benzoate leads to the number of Fos-like immunoreactive neurons decreased in the spinal trigeminal nucleus caudal partand raphe magnus nucleus, increased the number of Fos-like immunoreactive neurons in the periaqueductal gray and remained unchanged in the ventromedial hypothalamic nucleus and mediodorsal thalamus nucleus in conscious rats. [4] Rizatriptan Benzoate markedly reduces the number of head-flicks in the rats. Rizatriptan Benzoate also significantly reduces the duration of grooming behavior by nearly 2-fold when compared with that without treatment. [5]

Protocol (from reference)

Solubility (25°C)

In vitro

Water 46 mg/mL
(117.5 mM)
DMSO 20 mg/mL
(51.08 mM)
Ethanol Insoluble

Chemical Information

Molecular Weight 391.47


CAS No. 145202-66-0
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O

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Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT00300924 Completed Drug: Rizatriptan co-administered with Acetaminophen Migraine Diamond Headache Clinic|Merck Sharp & Dohme Corp. March 2006 Phase 3

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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