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Rizatriptan Benzoate 5-HT Receptor agonist

Cat.No.S1607

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

Batch: Purity: 99.98%
99.98

Solubility

In vitro
Batch:

DMSO : 78 mg/mL (199.24 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Water : 78 mg/mL

Ethanol : Insoluble

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In vivo
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )

Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.

Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.

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Chemical Information, Storage & Stability

Molecular Weight 391.47 Formula

C22H25N5O2

Storage (From the date of receipt)
CAS No. 145202-66-0 Download SDF Storage of Stock Solutions

Synonyms MK-462 Benzoate SMILES CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O

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Mechanism of Action

Targets/IC50/Ki
5-HT1
In vivo
Rizatriptan Benzoate blocks neurogenic vasodilation via an action on 5-HT(1D) receptors located on perivascular trigeminal nerves to inhibit CGRP release in anaesthetized guinea-pigs. This compound evokes a transient reduction in dural blood vessel diameter which recovered to baseline values within 10 min in anaesthetized guinea-pigs. It significantly inhibits dural plasma protein extravasation produced by high intensity electrical stimulation of the trigeminal ganglion. This chemical significantly reduces electrically stimulated dural vasodilation in anaesthetised rats. It significantly reduced SP mRNA levels in the midbrains of normal and model group rats, indicating that this compound can downregulate SP gene expression in the rat midbrain. It 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. This chemical 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. It markedly reduces the number of head-flicks in the rats. This compound also significantly reduces the duration of grooming behavior by nearly 2-fold when compared with that without treatment.
References
  • [4] https://pubmed.ncbi.nlm.nih.gov/20934408/
  • [5] https://pubmed.ncbi.nlm.nih.gov/20971093/

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2025-10-01)

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06473597 RECRUITING
Migraine
Antonios Likourezos
2024-09-01 PHASE4
NCT05550207 COMPLETED
Migraine
Axsome Therapeutics, Inc.
2022-08-31 PHASE3
NCT04384367 COMPLETED
Migraine
Eurofarma Laboratorios S.A.
2022-12-30 PHASE3
NCT04068051 COMPLETED
Migraine
Axsome Therapeutics, Inc.
2019-07-06 PHASE3
NCT02447991 COMPLETED
Vestibular Migraine; Migrainous Vertigo
Robert W. Baloh
2014-12 PHASE2; PHASE3
NCT04163185 COMPLETED
Migraine
Axsome Therapeutics, Inc.
2019-10-08 PHASE3

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