product name Rizatriptan Benzoate
Description: Rizatriptan Benzoate (also known as MK-462 Benzoate) is an agonist at serotonin 5-HT1B and 5-HT1D receptors, used to treat acute migraine attacks. It 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.
References: Br J Pharmacol. 2001 Aug;133(7):1029-34; Eur J Pharmacol. 1997 Jun 5;328(1):61-4.
391.47
Formula
C22H25N5O2
CAS No.
145202-66-0
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 20 mg/mL (51.08 mM)
Water: 46 mg/mL (117.5 mM)
Ethanol: <1 mg/mL
Solubility (In vivo)
Synonyms
MK-462 Benzoate
other peoduct :
| In Vitro |
In vitro activity: Kinase Assay: Cell Assay: |
|---|---|
| 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. 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. 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. |
| Animal model | |
| Formulation & Dosage | |
| References | Eur J Pharmacol. 1997 Jun 5;328(1):61-4. |
