中文名:苯甲酸利扎曲坦
英文名:Rizatriptan Benzoate
英文别名:MK-462 Benzoate;N,N-dimethyl-5-(1H-1,2,4-triazol-1-ylmethyl)-1H-indole-3-ethanamine,benzoate (1:1)
纯度:10mM in DMSO
货号:R407790
包装:1ml
Cas号:145202-66-0
存储温度:-80℃储存
产品介绍:
Information
Rizatriptan Benzoate (MK-462) is an agonist at serotonin5-HT1Band5-HT1Dreceptors, used to treat acute migraine attacks.
In vitro
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\u2009min 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. 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. 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.
Cell Data
cell lines:BE2C, IMR5, 1643, SY5Y, CHP134, SKNSH, NGP, KELLY, LAN5, NLF, NB69, SKNDZ, NBSD, NBLS, SKNFI, EBC1, SKNAS, NB16, RPE1 cell lines.
Concentrations:
Incubation Time:
Powder Purity:≥99%
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关键字: MK-462 Benzoate;N,?N-?dimethyl-?5-?(1H-?1,?2,?4-?triazol-?1-?ylmethyl)?-?1H-?indole-?3-?ethanamine,benzoate (1:1)
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