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標簽:(±)-McN 5652
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化學性質:
規格 | 10mg 50mg |
CAS | 96795-89-0 |
別名 |
|
化學名 | (6R,10bS)-6-(4-(methylthio)phenyl)-1,2,3,5,6,10b-hexahydropyrrolo[2,1-a]isoquinoline |
分子式 | C19H21NS |
分子量 | 295.44 |
溶解度 | <14.77mg/ml in 1eq. HCl; <22.16mg/ml in DMSO |
儲存條件 | Store at -20°C |
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 |
產品描述:
(±)-McN 5652 is a highly potent inhibitor of serotonin (5-HT, 5-hydroxytryptamine) uptake with a Ki value of approximately 0.6 nM in rat brain synaptosomes in vitro and an ED50 value of approximately 2 mg/kg p.o. ex vivo [1].
5-HT is a monoaminergic neurotransmitter to modulate numerous sensory, behavioural processes and motor in the mammalian nervous system [2]. There are at least three main groups of 5-HT receptor: 5-HT1, 5-HT2, and 5-HT3. Each group is not only structurally but also operationally distinct. Each receptor group has its own distinct transduction system. 5-HT4 is the more recently identified receptor. It almost represents a fourth 5-HT receptor class [3].
Receptor binding experiments indicated that McN-5652 has a weak affinity for serotonin 5-HT2 receptor (apparent Ki approximately 200 nM) and a very low affinity for serotonin 5-HT1 receptor [1].
In vivo, McN-5652 was required in low doses to potentiate the serotonin syndrome in rats. For this serotonin syndrome, the ED50 value was 1.5 mg/kg 2 hr after p.o. dosing. To potentiate head twitches which were induced by L-5-hydroxytryptophan (L-5HTP) in mice, the ED50 value is just 0.4 mg/kg 2 hr after p.o. dosing. That means McN-5652 is of high potency as a serotonin uptake inhibitor [1].
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原創作者:上海莼試生物技術有限公司
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普票匯款信息
賬 戶 名:上海生物
開 戶 行:中國銀行山東省分行營業部
賬 號:2169 2341 6278