| CAS NO: | 121679-20-7 |
| 包装 | 价格(元) |
| 1mg | 电议 |
| 5mg | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| Cas No. | 121679-20-7 |
| 别名 | N-甲基-3-(1,2,3,6-四氢-1-甲基-4-吡啶)-1H-吲哚-5-乙烷磺酰胺,Naratriptan Impurity B |
| 化学名 | N-methyl-3-(1,2,3,6-tetrahydro-1-methyl-4-pyridinyl)-1H-indole-5-ethanesulfonamide |
| Canonical SMILES | O=S(CCC1=CC=C2C(C(C3=CCN(C)CC3)=CN2)=C1)(NC)=O |
| 分子式 | C17H23N3O2S |
| 分子量 | 333.4 |
| 溶解度 | ≤0.1mg/ml in ethanol;10mg/ml in DMSO;10mg/ml in dimethyl formamide |
| 储存条件 | Store at -20℃ |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
| Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
| 产品描述 | pKi: 8.9 of Naratriptan for human 5-HT1B 3,4-dihydro Naratriptan is a selective serotonin 5-HT1B agonist. 5-HT1B receptors are widely distributed throughout the CNS with the highest concentrations found in the basal ganglia, frontal cortex, striatum, and the hippocampus. The function of the 5-HT1B receptor differs depending upon its location. In vitro: 3,4-dihydro Naratriptan is an impurity formed during the preparation of naratriptan. Naratriptan had high affinity for human recombinant 5HT1B and 5HT1D receptors and could cause contractions of dog isolated basilar and middle cerebral artery. Naratriptan also caused small contractions of human isolated coronary arteries [1]. In vivo: In anaesthetized dogs, naratriptan caused selective vasoconstriction of the carotid arterial bed and, in anaesthetized rats, naratriptan selectively inhibited neurogenic plasma protein extravasation in the dura. In various antinociceptive tests, naratriptan had no effect even at high doses. In conscious rats and dogs, naratriptan had high oral bioavailability [1]. Clinical trial: Naratriptan has been approved for acute oral migraine therapy. In two Phase III trials of naratriptan compared with placebo, relief at four hours was obtained in 60% and 68% of patients using the 2.5-mg dose, with recurrence of headache in 24 hours in 27% and 28% of patients. Adverse effects of naratriptan were found to be similar to placebo, and its tolerability appeared superior compared with studies of other oral triptans [2]. References: |
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