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产品价格:电议      采购度:1599      原产地:美洲
发布时间:2021/7/23 22:22:07 所属地区:上海 上海市
简要描述:
Deramciclane 对 5-HT2A 和 5-HT2C 受体具有高亲和力。Deramciclane 作为两种受体亚型的拮抗剂,对 5-HT2C 受体具有反向激动剂特性,无直接刺激激动剂。
标签:EGIS-3886
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CAS No. : 120444-71-5
MCE 站:Deramciclane
产品活性:Deramciclane 对 5-HT2A 和 5-HT2C 受体具有高亲和力。Deramciclane 作为两种受体亚型的拮抗剂,对 5-HT2C 受体具有反向激动剂特性,无直接刺激激动剂。
研究领域:GPCR/G Protein | Neuronal Signaling
作用靶点:5-HT Receptor
In Vitro: Deramciclane is a novel anxiolytic agent that binds with high affinity to 5-HT2A/2C receptors. The interactions of Deramciclane with the serotonin 5-HT2C receptor are characterized further using receptor phosphoinositide hydrolysis assays and receptor autoradiography. Deramciclane antagonizes 5-HT2C receptor mediated 5-HT-stimulated phosphoinositide hydrolysis with an IC50 value of 168 nM. Deramciclane also decreases basal phosphoinositide hydrolysis by up to 33% (EC50= 93 nM) in a physiological system in the choroid plexus, suggesting that Deramciclane possesses inverse agonist properties at this receptor.
In Vivo: Deramciclane 3 and 10 mg/kg does not change the dopamine levels significantly at any time point versus the basal level whereas 30 mg/kg of Deramciclane significantly increases the levels at 40-100 min and at 160-240 min (P<0.05). Deramciclane is a putative antiserotonergic compound that reduces 5-HT-induced phosphoinositol hydrolysis and a variety of actions caused by serotonergic agonists. The receptor binding profile of Deramciclane is rather similar to that of ritanserin. Deramciclane has a high affinity for 5-HT2A and 5-HT2C receptors; it acts as an antagonist at both receptor subtypes and has inverse agonist properties at the 5-HT2C receptors without direct stimulatory agonist effects. Deramciclane has been shown to have anxiolytic-like activity in several animal tests.
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更新时间:2024/1/2 10:14:29
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