Rizatriptan Benzoate(MK-462 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。
CAS NO: | 145202-66-0 |
规格: | ≥98% |
包装与价格:
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 |
产品介绍
理化性质和储存条件
Molecular Weight (MW) | 391.47 |
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Formula | C22H25N5O2 |
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CAS No. | 145202-66-0 |
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Storage | -20℃ for 3 years in powder form |
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-80℃ for 2 years in solvent |
Solubility (In vitro) | DMSO: 20 mg/mL (51.08 mM) |
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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 |
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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; |
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实验参考方法
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. |
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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. |
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Animal model | Rats |
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Formulation & Dosage | N/A |
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References | Eur J Pharmacol. 1997 Jun 5;328(1):61-4. |
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