tacrine

Tacrine (CS 12602) 一种间接胆碱能激动剂和中枢作用的抗胆碱酯酶。它被批准用于治疗阿尔茨海默病。

Tacrine hydrochloride hydrate (Tetrahydroaminacrine) 是一种乙酰胆碱酯酶 (AChE) 和丁酰胆碱酯酶 (BChE) 的抑制剂，它们的IC50值分别为 31 nM 和 25.6 nM。

Bis(7)-tacrine dihydrochloride 衍生自 tacrine ，是一种二聚体乙酰胆碱酯酶 (AChE) 抑制剂，具有治疗阿尔茨海默病的潜力。Bis(7)-tacrine dihydrochloride 通过阻断 NMDA 受体防止谷氨酸诱导的神经元凋亡。Bis(7)-tacrine dihydrochloride 是一种有效的 GABAA 受体拮抗剂。

Tacrine is a indirect cholinergic agonist and centrally acting anticholinesterase. Tacrine hydrochloride hydrate is an inhibitor of acetyl (AChE) and butyryl-cholinestrase (BChE) with IC50s of 31 nM and 25.6 nM, respectively.

Dimetacrine is a useful antidepressant.

Hydroxytacrine maleate (Velnacrine maleate) 是一种胆碱酯酶(cholinesterase) 抑制剂，可增强啮齿动物的记忆力，可用于研究阿尔茨海默型老年性痴呆（SDAT）。

Monometacrine 是一种胆固醇酯酶抑制剂，具有抗抑郁作用。

Dimetacrine tartrate is a tricyclic antidepressant (TCA) used for the therapy of depression in Europe and formerly in Japan.

7-Bromotacrine is a biochemical.

Velnacrine (1,2,3,4-tetrahydro-9-aminoacridin-1-ol maleate) 是一种生化物质。

TA-03 (7-Meota) 是一种有效的 AChE 抑制剂，可治疗 AD 的认知表现。

6,9-Dichloro-1,2,3,4-tetrahydroacridine is a synthetic intermediate in the synthesis of tacrine-based acetylcholinesterase (AChE) inhibitors.1It is also an intermediate in the synthesis of multifunctional tacrine hybrids that possess radical scavenging, amyloid-β aggregation inhibitory, and or β-secretase 1 (BACE1) inhibitory activities in addition to their activity as AChE inhibitors.2,3 1.Recanatini, M., Cavalli, A., Belluti, F., et al.SAR of 9-amino-1,2,3,4-tetrahydroacridine-based acetylcholinesterase inhibitors: Synthesis, enzyme inhibitory activity, QSAR, and structure-based CoMFA of tacrine analoguesJ. Med. Chem.43(10)2007-2018(2000) 2.Digiacomo, M., Chen, Z., Wang, S., et al.Synthesis and pharmacological evaluation of multifunctional tacrine derivatives against several disease pathways of ADBioorg. Med. Chem. Lett.25(4)807-810(2015) 3.Li, S.Y., Jiang, N., Xie, S.S., et al.Design, synthesis and evaluation of novel tacrine-rhein hybrids as multifunctional agents for the treatment of Alzheimer's diseaseOrg. Biomol. Chem.12(5)801-814(2014)

AChE-IN-9 是一种Tacrine 连接乙酰化 β-葡萄糖的糖缀合物。AChE-IN-9 也是一种AChE 抑制剂，IC50为 0.4 μM，对健康细胞的肝毒性低。Tacrine 可用于阿兹海默症的研究。

OctaHydraminoacridine 是一种 Tacrine 类似物，是一种有效的乙酰胆碱酯酶 (AChE) 和丁酰胆碱酯酶 (BChE) 抑制剂。OctaHydraminoacridine 可用于阿尔茨海默病 (AD) 研究。

Torilin and torilolone show hepatoprotective effects on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells,the EC50 values are 20.6 +/- 1.86 and 3.6 +/- 0.1 microM, respectively; and silybin as a positive control shows an EC50 value of 69.0

Picfeltarraenin X shows stronger AChE inhibition than the known AChE inhibitor Tacrine.

ZLMT-12 (compound 35) 是他克宁衍生物，是一种有效的 CDK2 (IC50: 0.011 μM) 和 CDK9 (IC50: 0.002 μM) 抑制剂。ZLMT-12 能够较弱的抑制 AChE (IC50: 19.023 μM) 和 BuChE (IC50: 2.768 μM)。ZLMT-12 具抗增殖活性，且细胞毒性较低。ZLMT-12 能够将细胞周期阻滞在 S 期和 G2 M 期，并诱导细胞凋亡。

Onitin shows super-oxide and DPPH free radical scavenging effects.It also exhibits hepatoprotective activity on tacrine-induced cytotoxicity in human liver-derived Hep G2 cells.

Picfeltarraenin IA (Picfeltarraenin A) 是一种Picriafel-terraeLour (P.fel-terrae) 中提取的三萜类化合物，是一种乙酰胆碱酯酶抑制剂。它可用于感染，癌症和炎症的研究。

1,3,5,6-Tetrahydroxyxanthone shows moderate hepatoprotective activity with EC(50) values of 160.2 +/- 0.6 microM against tacrine-induced cytotoxicity in HepG2 cells. It can inhibit angiotensin-I-converting-enzyme activity in a dose-dependent manner.