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.
For research use only. We do not sell to patients.
- CAS No.: 144034-80-0
- Formula: C15H19N5
- Molecular Weight:269.34
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
All 5-HT Receptor Isoforms
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Biological Activity
Description
IC50 & Target
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5-HT1D Receptor |
5-HT1B Receptor |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHO | EC50 |
8.4 nM
Compound: Rizatriptan
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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.
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[PMID: 9357514] |
| CHO | IC50 |
11 nM
Compound: Rizatriptan
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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.
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[PMID: 9357514] |
| CHO | IC50 |
41 nM
Compound: Rizatriptan
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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.
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[PMID: 9357514] |
| Oocyte | IC50 |
2.9 μM
Compound: 18
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Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
Inhibition of human aquaporin 4 M23 isoform expressed in Xenopus laevis oocytes
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[PMID: 18182301] |
| Vero C1008 | IC50 |
>2.0 × 105M
Compound: COVC-1751177664
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Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
Antiviral activity determined as inhibition of SARS-CoV-2 induced cytotoxicity of VERO-6 cells at 10 uM after 48 hours exposure to 0.01 MOI SARS CoV-2 virus by high content imaging
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10.6019/CHEMBL4651402 |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J (female, 8-10 weeks old, 20-30 g, SPF grade, NTG-induced medication overuse headache model)[1]
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Dosage:0.02 mg/kg
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Administration:oral; voluntary free-choice access; during NTG stimulation phase until day 14
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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
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 144034-80-0
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Molecular Weight 269.34
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Formula C15H19N5
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SMILES
CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3
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Synonyms
MK 462 free base
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Protocols
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Protocol for Open Field Test (OF)
The Open Field Test is a rodent behavioral assay that measures spontaneous locomotion, exploratory behavior, and anxiety-like behavior when an animal is placed in a novel open arena. The main readouts are total distance traveled, movement time, velocity, center-zone entries, center-zone time, peripheral-zone time, and thigmotaxis. The assay is based on the conflict between exploration of a novel environment and avoidance of exposed open areas; higher center exploration is commonly interpreted as lower anxiety-like behavior, whereas increased wall-following or peripheral occupancy is interpreted as higher anxiety-like behavior.
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Protocol for Elevated Plus Maze Test
The Elevated Plus Maze is a rodent anxiety-like behavior assay based on the conflict between spontaneous exploration and avoidance of open, elevated, exposed spaces. The apparatus contains two open arms and two closed arms arranged in a plus shape, and rodents normally spend more time in closed arms than open arms. The assay readout is generated by recording arm entries, time spent in open and closed arms, and related exploratory behaviors. Increased open-arm time or open-arm entries is commonly interpreted as reduced anxiety-like behavior, whereas reduced open-arm exploration is interpreted as increased anxiety-like behavior.
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Transepithelial/transendothelial electrical resistance assay
TEER measures electrical resistance across epithelial or endothelial monolayers cultured on permeable supports, and the readout reflects ionic conductance through the cell barrier, especially the paracellular pathway regulated by junctional integrity. TEER can be measured without destroying the monolayer and is commonly used before or during transport, permeability, barrier-disruption, and barrier-maturation experiments. TEER values are influenced by biological maturation and technical conditions; reported factors include temperature, medium formulation, passage number, electrode geometry, membrane properties, and junctional length during early monolayer maturation. Therefore, TEER should be interpreted with blank-insert subtraction, area normalization, repeated readings, and, when possible, orthogonal barrier readouts such as FITC-dextran flux or tight-junction staining.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)