Rizatriptan Benzoate(MK-462 Benzoate)

Molecular Weight (MW)	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
SMILES Code	CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O
Synonyms	MK-462 Benzoate;izatriptan Benzoate; MK-0462; 2-(5-((1H-1,2,4-TRIAZOL-1-YL)METHYL)-1H-INDOL-3-YL)-N,N-DIMETHYLETHANAMINE BENZOATE; MK 462; rizatriptan benzoate; Maxalt; MK 0462; MK 462;

Molecular Weight (MW)

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

SMILES Code

CN(C)CCC1=CNC2=C1C=C(C=C2)CN3C=NC=N3.C1=CC=C(C=C1)C(=O)O

Synonyms

MK-462 Benzoate;izatriptan Benzoate; MK-0462; 2-(5-((1H-1,2,4-TRIAZOL-1-YL)METHYL)-1H-INDOL-3-YL)-N,N-DIMETHYLETHANAMINE BENZOATE; MK 462; rizatriptan benzoate; Maxalt; MK 0462; MK 462;

In Vitro	In vitro activity: Rizatriptan Benzoate (also known as MK-462 Benzoate) is a novel, potent and selective agonist at serotonin 5-HT1B and 5-HT1D receptors, it can be potentially used to treat acute migraine attacks.
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	Rats
Formulation & Dosage	N/A
References	Eur J Pharmacol. 1997 Jun 5;328(1):61-4.

In Vitro

In vitro activity: Rizatriptan Benzoate (also known as MK-462 Benzoate) is a novel, potent and selective agonist at serotonin 5-HT1B and 5-HT1D receptors, it can be potentially used to treat acute migraine attacks.

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

Rats

Formulation & Dosage

N/A

References

Eur J Pharmacol. 1997 Jun 5;328(1):61-4.

CAS NO:	145202-66-0
规格:	≥98%

包装	价格(元)
10mg	电议
25mg	电议
50mg	电议
100mg	电议
250mg	电议
500mg	电议
1g	电议