2. GPCR/G Protein Neuronal Signaling
  3. 5-HT Receptor
  4. Rizatriptan

Rizatriptan (MK 462 free base) is an orally active 5-HT1B/5-HT1D 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.

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Rizatriptan

Rizatriptan Chemical Structure

CAS No. : 144034-80-0

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Rizatriptan Related Antibodies

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Description

Rizatriptan (MK 462 free base) is an orally active 5-HT1B/5-HT1D 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].

IC50 & Target

5-HT1D Receptor

 

5-HT1B Receptor

 

Cellular Effect
Cell Line Type Value Description References
CHO EC50
8.4 nM
Compound: Rizatriptan
Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.
Measurement of agonist induced [35S]GTP-gamma-S, binding in CHO cells stably transfected with 5-hydroxytryptamine 1D receptor.
[PMID: 9357514]
CHO IC50
11 nM
Compound: Rizatriptan
Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
Binding affinity by displacement to human cloned 5-hydroxytryptamine 1D receptor in CHO cells by [3H]5-HT displacement.
[PMID: 9357514]
CHO IC50
41 nM
Compound: Rizatriptan
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
Binding affinity to human cloned 5-hydroxytryptamine 1B receptor in CHO cells by [3H]5-HT binding displacement.
[PMID: 9357514]
Oocyte IC50
2.9 μM
Compound: 18
Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
[PMID: 18182301]
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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: C57BL/6J (female, 8-10 weeks old, 20-30 g, SPF grade, NTG-induced medication overuse headache model)[1]
Dosage: 0.02 mg/kg
Administration: oral; voluntary free-choice access; during NTG stimulation phase until day 14
Result: Exacerbated NTG-induced cutaneous allodynia, with hind paw mechanical pain thresholds significantly lower than control groups during modeling phase and returning to baseline only by day 40.
Showed a stable, fluctuating upward preference for rizatriptan solution, with consumption ratio to total liquid consistently above 0.5 and significantly higher on days 4, 6, 8, 10, 12, and 14.
Exhibited more rapid decrease in head and hind paw mechanical pain thresholds and slower recovery after SNP stimulation on day 40.
Had significantly lower time in open arms/total time, lower proportion of open arm entries, higher time in closed arms/total time, and higher proportion of closed arm entries.
Had significantly shorter residence time in central zone, shorter freezing time in central zone, shorter activity distance in central zone, and fewer entries into central zone.
Showed significantly increased c-Fos positive cell counts in 25 brain regions.
Clinical Trial
Molecular Weight

269.34

Formula

C15H19N5
CAS No.
SMILES

CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3
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Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Rizatriptan Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Rizatriptan144034-80-0MK 462MK462MK-4625-HT ReceptorSerotonin Receptor5-hydroxytryptamine ReceptorMonoamine Oxidase A5-HT 1 B/ 1 D receptorprelimbic cortexrat livercentral sensitizationextracerebral blood vesselsnitroglycerin-induced cutaneous allodyniaMonoamine Oxidase Bfemale C57BL/6J miceintracranial blood vessels
Inhibitorinhibitorinhibit

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