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T29633
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| AD 5 is a bioactive chemical. |
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T1180
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Sigma receptor
Adrenergic Receptor
5-HT Receptor
Dopamine Receptor
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| Blonanserin 是一种有效的5-HT2A 和多巴胺 D2 受体拮抗剂，Ki 为 0.812 和 0.142 nM，是一种非典型的抗精神病试剂。 |
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T10558
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Others
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| Blonanserin D5 is a deuterium-labeled Blonanserin. Blonanserin (AD-5423) is a dopamine D2/5-HT2 receptor antagonist with an atypical antipsychotic effect. |
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T10559
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Others
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| Blonanserin D8 is a deuterium-labeled Blonanserin. Blonanserin (AD-5423) is a dopamine D2/5-HT2 receptor antagonist with an atypical antipsychotic effect. |
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T72893
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| Dual AChE-MAO B-IN-5 是一种茚满酮衍生物，是一种有效的双重 AChE/MAO-B 抑制剂，对 AChE、MAO-B 和 MAO-A 的IC50值分别为 0.0224、0.0412 和 0.1116 μM。Dual AChE-MAO B-IN-5 具有抗氧化活性，防止 β-淀粉样斑块聚集。Dual AChE-MAO B-IN-5 可用于阿尔茨海默病 (AD) 研究。 |
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T14138
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EGFR
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| AG-825(Tyrphostin AG-825) is a potential agent for overcoming Mn-induced neurotoxicity or AD development[5] and is a selective and ATP-competitive ErbB2 inhibitor which suppresses tyrosine phosphorylation, with an IC50 of 0.35 μM. AG825 significantly acce |
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T27269
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| Ensaculin is a NMDA antagonist and a 5HT1A agonist potentially for the treatment of Alzheimer's disease (AD). Ensaculin showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. It e |
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T74461
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| ChalconesA-N-5 是一种三羟基查耳酮衍生物化合物。ChalconesA-N-5 在浓度低于 100 µM (IC50> 1 mM) 时不显示细胞毒性，但对促进细胞增殖有显着作用。ChalconesA-N-5 可能促进受损脑组织中神经元细胞的生长。ChalconesA-N-5 还抑制由 RSL 或 erastin 诱导的铁死亡，并降低由 Aβ1-42 蛋白聚集诱导的脂质过氧化水平。ChalconesA-N-5 是一种很有前途的分子骨架候选物，可用于进一步开发用于体内试验的先导化合物以研究 AD。 |
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T63216
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| 5-{8-[（3，4'-二氟[1，1'-联苯]-4-基）甲氧基]-2-甲基咪唑并[1，2-a]吡啶-3-基}-N-甲基吡啶-2-甲酰胺（1o）具有较高的体外效力和脑暴露效果，能够使脑Aβ42水平的明显降低，且对细胞色素p450酶无抑制作用。此外，化合物1o 在AD 模型小鼠中表现出优异的抗认知缺陷作用。 |
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T38002
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| LEO 39652 is a dual-soft PDE4 inhibitor with IC50s of 1.2 nM, 1.2 nM, 3.0 nM and 3.8 nM for PDE4A, PDE4B, PDE4C and PDE4D, respectively. LEO 39652 also inhibits TNF-α with an IC50 value of 6.0 nM. LEO 39652 is used for topical research of Atopic dermatitis (AD) [1].
LEO 39652 shows unbound in vitro potency when measured as LPS induced TNF-α release in human peripheral blood mononuclear cells (PBMC), incubated in serum free medium. LEO 39652 shows a relatively high binding to human serum albumin[2].
LEO 39652 is inactivated both in blood and liver (dual-soft) while stabled in the skin[1].Pharmacokinetic AnalysisLEO 39652 exhibits total clearance (rats 930, minipigs 200 and monkey 300 mL/min/kg) and ratio to total AUC (rats 4, minipigs 6 and monkey 6 %) following intravenous administration (rats 0.075, minipigs 0.5 and monkeys 2.0 mg/kg)[1].
[1]. Jens Larsen, et al. Discovery and Early Clinical Development of Isobutyl 1-[8-Methoxy-5-(1-oxo-3 H-isobenzofuran-5-yl)-[1,2,4]triazolo[1,5- a]pyridin-2-yl]cyclopropanecarboxylate (LEO 39652), a Novel Dual-Soft" PDE4 Inhibitor for Topical Treatment of Atopic Dermatitis. J Med Chem. 2020 Dec 10;63(23):14502-14521.[2]. Stefan Eirefelt |
