Fig. 1 · Structure

Cat. No.: A10801
CAS No.: 145202-66-0
Formula: C₂₂H₂₅N₅O₂
Mol. Weight: 391.47

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Rizatriptan benzoate

5-HT1 Agonist

Rizatriptan benzoate is a selective agonist of the 5-HT1B and 5-HT1D serotonin receptors. It exhibits vasoconstrictive properties that affect peripheral blood flow and effectively penetrates the blood-brain barrier, thereby inhibiting pain neurotransmission within the central nervous system. This compound is primarily utilized in research focused on migraine pathophysiology and the modulation of serotonergic signaling.

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In Vivo Studies

Healthy adult Wistar rats received Rizatriptan benzoate by intragastric perfusion before modeling, with significantly reduced midbrain PENK and SP mRNA levels in both treatment groups. In male mice, repeated Rizatriptan benzoate administration by oral gavage produced significant reductions in hind paw and head withdrawal thresholds. Cutaneous allodynia and hyperalgesia progressed with repeated dosing before recovery. [1,2]

Literature-reported observations and conditions; not Adooq-tested protocols or general treatment recommendations.

Midbrain PENK mRNA reduction in Wistar rats

Animal study · healthy, adult, Wistar rats [1]

Healthy adult Wistar rats received Rizatriptan benzoate by intragastric perfusion prior to modeling. Midbrain PENK mRNA levels were significantly reduced in both Rizatriptan benzoate groups.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
PENK mRNA levels	Reported result PENK and SP mRNA levels in the rat midbrain were significantly reduced in both rizatriptan benzoate groups (P < 0.05; Table 1).	[1]

Conditions shared by the study groups

Route: intragastrically perfused
Treatment course: for 7 days prior to modeling

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Rizatriptan benzoate 1 mg/kg per day	normal control	PENK and SP mRNA levels in the rat midbrain were significantly reduced in both rizatriptan benzoate groups (P < 0.05; Table 1).	[1]

Rizatriptan benzoate 1 mg/kg per day: Model: healthy, adult, Wistar rats; Reported limits: Not stated in the sentences used: vehicle.

Methods and source locations

Compound reported in the paper: Rizatriptan benzoate

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

RESULTS > Quantitative analysis of experimental animals (S3); RESULTS > PENK and SP mRNA expression in rats with migraine (S16, S18); MATERIALS AND METHODS > Materials (S21); MATERIALS AND METHODS > Methods > Migraine model establishment and interventions (S24)

PENK mRNA levels: PENK mRNA levels; comparator: normal control — RESULTS > PENK and SP mRNA expression in rats with migraine (S16, S18)

Rizatriptan benzoate 1 mg/kg per day · RESULTS > Quantitative analysis of experimental animals (S3); RESULTS > PENK and SP mRNA expression in rats with migraine (S18); MATERIALS AND METHODS > Methods > Migraine model establishment and interventions (S24)

Rizatriptan and hind paw withdrawal thresholds in mice

Animal study · eight-week-old male C57BL/6J mice; n = 21 (nSAL = 10, nRIZ = 11) [2]

Male mice received repeated Rizatriptan benzoate administrations by oral gavage. Hind paw withdrawal thresholds showed significant reductions, with cutaneous allodynia and hyperalgesia progressing during repeated dosing before recovery.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
hind paw withdrawal threshold (PWT)	Reported result PWT and HWT showed significant reductions from day 2 onward; (B) F = 26.840, p < 0.001. This RIZ-induced cutaneous allodynia and hyperalgesia progressed with repeated dosing, reaching its nadir on day 12 before recovering by day 20.	[2]

Conditions shared by the study groups

Route: oral gavage
Treatment course: Day 0, with administrations every other day for six sessions
Vehicle: 0.9% saline

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Rizatriptan benzoate 4 mg/kg	equivalent volume of 0.9% saline	PWT and HWT showed significant reductions from day 2 onward; (B) F = 26.840, p < 0.001. This RIZ-induced cutaneous allodynia and hyperalgesia progressed with repeated dosing, reaching its nadir on day 12 before recovering by day 20.	[2]

Rizatriptan benzoate 4 mg/kg: Model: eight-week-old male C57BL/6J mice; n = 21 (nSAL = 10, nRIZ = 11)

Methods and source locations

Compound reported in the paper: Rizatriptan benzoate

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

Methods > Animals (S2); Methods > Mouse model of triptan-induced MOH (S7, S8, S12); Methods > Von Frey filament test (S15); Results > Repeated RIZ administration induces cutaneous allodynia in mice (S130, S131, S132, S133); Fig. 1 legend (S199, S200)

hind paw withdrawal threshold (PWT): hind paw withdrawal threshold (PWT); comparator: equivalent volume of 0.9% saline — Methods > Von Frey filament test (S15); Results > Repeated RIZ administration induces cutaneous allodynia in mice (S132, S133); Fig. 1 legend (S200)

Rizatriptan benzoate 4 mg/kg · Methods > Mouse model of triptan-induced MOH (S7, S12); Results > Repeated RIZ administration induces cutaneous allodynia in mice (S130, S132, S133); Fig. 1 legend (S200)

Midbrain SP mRNA reduction in Wistar rats

Animal study · healthy, adult, Wistar rats [1]

Healthy adult Wistar rats received Rizatriptan benzoate by intragastric perfusion prior to modeling. Midbrain SP mRNA levels were significantly reduced in both Rizatriptan benzoate groups.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
SP mRNA levels	Reported result PENK and SP mRNA levels in the rat midbrain were significantly reduced in both rizatriptan benzoate groups (P < 0.05; Table 1).	[1]

Conditions shared by the study groups

Route: intragastrically perfused
Treatment course: for 7 days prior to modeling

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Rizatriptan benzoate 1 mg/kg per day	normal control	PENK and SP mRNA levels in the rat midbrain were significantly reduced in both rizatriptan benzoate groups (P < 0.05; Table 1).	[1]

Rizatriptan benzoate 1 mg/kg per day: Model: healthy, adult, Wistar rats; Reported limits: Not stated in the sentences used: vehicle.

Methods and source locations

Compound reported in the paper: Rizatriptan benzoate

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

SP mRNA levels: SP mRNA levels; comparator: normal control — RESULTS > PENK and SP mRNA expression in rats with migraine (S16, S18)

Rizatriptan and head withdrawal thresholds in mice

Animal study · eight-week-old male C57BL/6J mice; n = 21 (nSAL = 10, nRIZ = 11) [2]

Male mice received repeated Rizatriptan benzoate administrations by oral gavage. Head withdrawal thresholds showed significant reductions, with cutaneous allodynia and hyperalgesia progressing during repeated dosing before recovery.

Measured endpoints — not treatment concentrations
Endpoint	Reported result	Reference
head withdrawal threshold (HWT)	Reported result PWT and HWT showed significant reductions from day 2 onward; (C) F = 43.470, p < 0.001. This RIZ-induced cutaneous allodynia and hyperalgesia progressed with repeated dosing, reaching its nadir on day 12 before recovering by day 20.	[2]

Conditions shared by the study groups

Route: oral gavage
Treatment course: Day 0, with administrations every other day for six sessions
Vehicle: 0.9% saline

Study groups and reported outcomes
Group / dose	Comparator	Observed result	Reference
Rizatriptan benzoate 4 mg/kg	equivalent volume of 0.9% saline	PWT and HWT showed significant reductions from day 2 onward; (C) F = 43.470, p < 0.001. This RIZ-induced cutaneous allodynia and hyperalgesia progressed with repeated dosing, reaching its nadir on day 12 before recovering by day 20.	[2]

Rizatriptan benzoate 4 mg/kg: Model: eight-week-old male C57BL/6J mice; n = 21 (nSAL = 10, nRIZ = 11)

Methods and source locations

Compound reported in the paper: Rizatriptan benzoate

Literature evidence for the named compound in the stated model; no Adooq product-use or lot-performance claim.

head withdrawal threshold (HWT): head withdrawal threshold (HWT); comparator: equivalent volume of 0.9% saline — Methods > Von Frey filament test (S15); Results > Repeated RIZ administration induces cutaneous allodynia in mice (S132, S133); Fig. 1 legend (S200)

Specifications

Manufacturer	Adooq Bioscience
Actions	Agonist
CAS Number	145202-66-0
Applications	5-HT1 Agonist
Formula	C₂₂H₂₅N₅O₂
Molecular Weight	391.47
Synonyms	MK 462
SMILES	CN(C)CCC1=CNC2=C1C=C(CN3N=CN=C3)C=C2.O=C(O)C4=CC=CC=C4

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

Research References

[1] Yao G, Man Y, Luo X, et al. Rizatriptan benzoate influences the endogenous pain modulatory system in a rat model of migraine. Neural Regen Res (2012). PMID: 25767488 DOI: 10.3969/j.issn.1673-5374.2012.02.009 Source material
[2] Zhai D, Yang C, Gong Z, et al. A neural substrate for targeted analgesia associated with attenuated serotonergic transmission in a mouse model of medication overuse headache. J Headache Pain (2026). PMID: 42129633 DOI: 10.1186/s10194-026-02391-2 Source material

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Rizatriptan benzoate

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