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Rizatriptan Benzoate
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Rizatriptan Benzoate图片
CAS NO:145202-66-0
包装与价格:
包装价格(元)
5 mg电议
10 mg电议
25 mg电议
50 mg电议
100 mg电议
200 mg电议
1 mL*10 mM(in DMSO)电议

产品名称
苯甲酸利扎曲坦
MK-462 Benzoate
产品介绍
Rizatriptan benzoate 是 5-HT1激动剂,通过选择性结合并激活血清素 (5-HT) 1B 受体和 5-HT 1D 受体,从而缓解偏头痛。

产品描述

Rizatriptan benzoate selectively binds to and activates serotonin (5-HT) 1B receptors and 5-HT 1D receptors providing relief of migraine headaches.

体内活性

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. [1] 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. [2] 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. [3] Rizatriptan Benzoate leads to the number of Fos-like immunoreactive neurons decreased in the spinal trigeminal nucleus caudal partand raphe magnus nucleus, increased the number of Fos-like immunoreactive neurons in the periaqueductal gray and remained unchanged in the ventromedial hypothalamic nucleus and mediodorsal thalamus nucleus in conscious rats. [4] Rizatriptan Benzoate markedly reduces the number of head-flicks in the rats. Rizatriptan Benzoate also significantly reduces the duration of grooming behavior by nearly 2-fold when compared with that without treatment. [5]

Cas No.

145202-66-0

分子式

C22H25N5O2

分子量

391.475

别名

苯甲酸利扎曲坦;MK-462 Benzoate

储存和溶解度

DMSO:19.6 mg/mL (50 mM)
H2O:39.2 mg/mL (100 mM)
Powder: -20°C for 3 years
In solvent: -80°C for 2 years