Glemanserin (MDL11939) 是有效和选择性5-HT2A受体的拮抗剂,对大鼠 5-HT2A、兔 5-HT2A和人 5-HT2A受体的Ki分别为 2.89、0.54 和 2.5 nM。 MCE 的所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务 GlemanserinChemical Structure ...
生化机理氟班色林是 5-HT1A 受体激动剂和 5-HT2A 受体拮抗剂。氟班色林对人 5-HT1A受体 (Ki = 1 nm) 具有高亲和力,对 5-HT2A (Ki = 49 nm) 和 D4 (Ki = 4–24 nm) 受体亲和力较低,对多种其他神经递质受体和离子通道的亲和力可忽略不计。氟班色林被用作女性绝经前性欲减退 (HSDD) 的一种新...
Ziprasidone(CP88059)是5-HT和多巴胺受体拮抗剂,具有抗精神病活性。 Ziprasidone(CP88059) is a combined 5-HT (serotonin) and dopamine receptor antagonist which exhibits potent effects of antipsychotic activity. 关联靶点(人) 关联靶点(其它物种)
哌啶甲醇的酯和它们作为5HT2A受体拮抗剂MDL110907药物前体的用途本发明涉及式(I)的(+)-α-(2,3-二甲氧基苯基)-1-[2-(4-氟苯基)乙基]-4-哌啶甲醇的酯,其中R是CA·A·卡尔L·E·范希杰夫特R·W·小科斯利
对风湿性关节炎模型大鼠应用5-HT再摄取抑制剂,以增加关节内5,HT的含量,能明显加重该关节的炎症1251。5.HT注入到大鼠膝关节可引致关节滑膜大量炎性物质的渗出。相反,给予5-HT拮抗剂,能大大减轻关节滑膜的炎性渗出和关节疼痛【26】。人体资料也证实5-HT在关节炎发病中的致病作用。如损伤性下...
Introduction [ 11 C]MDL100907 is a high affinity PET ligand for 5-HT2A receptor quantification in vivo. On the basis of ROI analysis, the tracer is usually assumed to be reversible as its kinetics are well described by a two-tissue four-rate constant model [1]. In literature [ 11 C]...
双重作用的多巴胺D2/5-HT2A受体拮抗剂是开发非典型抗精神病药物的有效途径,但最新研究显示,非典型抗精神病药物将显著增加患者因心律失常及其他心脏疾病而猝死的风险,本文对D2/5-HT2A受体拮抗剂的药效团模型以及可能引起心血管风险的α1A肾上腺素受体拮抗剂和hERGK+通道阻断剂的药效团模型进行比较分析,从药效团模型...
24h取材行5-HT2a受体的免疫组织化学检测.实验二:成年雄性SD大鼠双侧海马CA1区埋管,动物恢复7d后行场景条件恐惧学习,学习前122s组大鼠双侧海马CA1区予5-HT2a受体拮抗剂MDL11939(17mmol,1μL/侧,Tocris Bioscience)或溶媒,12s组大鼠双侧海马CA1区予5-HT2a受体激动剂TBC-2(80mmol,1μL/侧,Tocris Bioscience)...
The intricate involvement of the serotonin 5-HT2A receptor (5-HT2AR) both in schizophrenia and in the activity of antipsychotic drugs is widely acknowledged. The currently marketed antipsychotic drugs, although effective in managing the symptoms of schiz
These results suggest that MDL 100,907 may have a unique interaction with dopaminergic systems and support the further development of selective receptor antagonists as a novel therapeutic strategy for . 展开 关键词: Schizophrenia 5-HT2A receptor antagonist MDL 100,907 Amphetamine Latent inhibition Drug...