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TAK-147 (Takeda).
Mucke H. Mucke H. Curr Opin Investig Drugs. 2001 Nov;2(11):1595-9. Curr Opin Investig Drugs. 2001. PMID: 11763163 Review.
TAK-147 is a CNS-specific acetylcholinesterase inhibitor under development by Takeda as a potential treatment for Alzheimer's disease. ...
TAK-147 is a CNS-specific acetylcholinesterase inhibitor under development by Takeda as a potential treatment for Alzheimer's
Comparison of the effect of TAK-147 (zanapezil) and E-2020 (donepezil) on extracellular acetylcholine level and blood flow in the ventral hippocampus of freely moving rats.
Hatip-Al-Khatib I, Takashi A, Egashira N, Iwasaki K, Fujiwara M. Hatip-Al-Khatib I, et al. Brain Res. 2004 Jun 25;1012(1-2):169-76. doi: 10.1016/j.brainres.2004.03.067. Brain Res. 2004. PMID: 15158174
The effects of zanapezil (TAK-147) and donepezil (E2020) on extracellular acetylcholine (ACh) levels were investigated by HPLC-microdialysis of ventral hippocampus (VH) in freely moving intact rats. ...The first increment was obtained between 5 and 40 min (11 …
The effects of zanapezil (TAK-147) and donepezil (E2020) on extracellular acetylcholine (ACh) levels were investigated …
Effect of oral administration of zanapezil (TAK-147) for 21 days on acetylcholine and monoamines levels in the ventral hippocampus of freely moving rats.
Hatip-Al-Khatib I, Iwasaki K, Yoshimitsu Y, Arai T, Egashira N, Mishima K, Ikeda T, Fujiwara M. Hatip-Al-Khatib I, et al. Br J Pharmacol. 2005 Aug;145(8):1035-44. doi: 10.1038/sj.bjp.0706288. Br J Pharmacol. 2005. PMID: 15951830 Free PMC article.
Zanapezil (TAK-147 (3-[1benzylpiperdin-4-yl]-1-(2,3,4,5-tetrahydro-1 H-1-benzazepin-8-yl) propan-1-one fumarate)) is a selective acetylcholine (ACh) esterase inhibitor under investigation as a drug for Alzheimer's disease (AD) treatment. ...TAK-147
Zanapezil (TAK-147 (3-[1benzylpiperdin-4-yl]-1-(2,3,4,5-tetrahydro-1 H-1-benzazepin-8-yl) propan-1-one fumarate)) is a
Central selective acetylcholinesterase inhibitor with neurotrophic activity: structure-activity relationships of TAK-147 and related compounds.
Ishihara Y, Goto G, Miyamoto M. Ishihara Y, et al. Curr Med Chem. 2000 Mar;7(3):341-54. doi: 10.2174/0929867003375272. Curr Med Chem. 2000. PMID: 10637368 Review.
TAK-147 also activates the monoaminergic systems and energy metabolism. ...This article reviews design and structure-activity relationships of TAK-147 and related compounds. Preclinical pharmacology of TAK-147 is also summarized....
TAK-147 also activates the monoaminergic systems and energy metabolism. ...This article reviews design and structure-activity
Direct β-Alkylation of Ketones and Aldehydes via Pd-Catalyzed Redox Cascade.
Wang C, Dong G. Wang C, et al. J Am Chem Soc. 2018 May 16;140(19):6057-6061. doi: 10.1021/jacs.8b03530. Epub 2018 May 2. J Am Chem Soc. 2018. PMID: 29708741
Both cyclic and acyclic ketones, as well as alpha-branched aldehydes, are suitable substrates for coupling with secondary and tertiary alkyl bromides. Concise formal synthesis of Zanapezil is achieved using this beta-alkylation method....
Both cyclic and acyclic ketones, as well as alpha-branched aldehydes, are suitable substrates for coupling with secondary and tertiary alkyl …
Reversal of scopolamine-induced spatial memory deficits in rats by TAK-147.
Chen Z, Xu AJ, Li R, Wei EQ. Chen Z, et al. Acta Pharmacol Sin. 2002 Apr;23(4):355-60. Acta Pharmacol Sin. 2002. PMID: 11931694 Free article.
TAK-147 has a little potent efficacy to donepezil, and was more potent than tacrine. ...CONCLUSION: TAK-147 plays an important role in spatial cognition, and this result provides additional evidence that TAK-147 is an ideal AChE inhibitor
TAK-147 has a little potent efficacy to donepezil, and was more potent than tacrine. ...CONCLUSION: TAK-147 play
Homology Modeling, de Novo Design of Ligands, and Molecular Docking Identify Potential Inhibitors of Leishmania donovani 24-Sterol Methyltransferase.
Sakyi PO, Broni E, Amewu RK, Miller WA 3rd, Wilson MD, Kwofie SK. Sakyi PO, et al. Front Cell Infect Microbiol. 2022 Jun 2;12:859981. doi: 10.3389/fcimb.2022.859981. eCollection 2022. Front Cell Infect Microbiol. 2022. PMID: 35719359 Free PMC article.
Structural similarity search via DrugBank identified vabicaserin, daledalin, zanapezil, imipramine, and cefradine with antileishmanial properties suggesting that the de-novo compounds could be explored as potential antileishmanial agents....
Structural similarity search via DrugBank identified vabicaserin, daledalin, zanapezil, imipramine, and cefradine with antileishmania …
Neurochemical effects of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1H-1-b enzazepin-8-yl)-1-propanone fumarate (TAK-147), a novel acetylcholinesterase inhibitor, in rats.
Hirai K, Kato K, Nakayama T, Hayako H, Ishihara Y, Goto G, Miyamoto M. Hirai K, et al. J Pharmacol Exp Ther. 1997 Mar;280(3):1261-9. J Pharmacol Exp Ther. 1997. PMID: 9067312
By contrast, TAK-147 was the least potent inhibitor of butyrylcholinesterase activity in rat plasma (IC50 = 23,500 nM). ...These results suggest that TAK-147 activates the central cholinergic system by specific inhibition of AChE activity without affec …
By contrast, TAK-147 was the least potent inhibitor of butyrylcholinesterase activity in rat plasma (IC50 = 23,500 nM). ...The …
TAK-147, an acetylcholinesterase inhibitor, increases choline acetyltransferase activity in cultured rat septal cholinergic neurons.
Kato K, Hayako H, Ishihara Y, Marui S, Iwane M, Miyamoto M. Kato K, et al. Neurosci Lett. 1999 Jan 22;260(1):5-8. doi: 10.1016/s0304-3940(98)00943-4. Neurosci Lett. 1999. PMID: 10027686
The effects of TAK-147 were greater in the presence of NGF, suggesting a synergistic action of TAK-147 and NGF. TAK-147 and donepezil showed high affinity for sigma receptors, whereas tacrine and physostigmine did not. ...
The effects of TAK-147 were greater in the presence of NGF, suggesting a synergistic action of TAK-147 and NGF. …
Effects of 3-[1-(phenylmethyl)-4-piperidinyl]-1-(2,3,4,5-tetrahydro-1 -H-1-benzazepin-8-yl)-1-propanone fumarate (TAK-147), a novel acetylcholinesterase inhibitor, on impaired learning and memory in animal models.
Miyamoto M, Takahashi H, Kato K, Hirai K, Ishihara Y, Goto G. Miyamoto M, et al. J Pharmacol Exp Ther. 1996 Jun;277(3):1292-304. J Pharmacol Exp Ther. 1996. PMID: 8667190
At 1 to 3 mg/kg, TAK-147 ameliorated the passive avoidance deficit induced by diazepam. ...These results indicate that TAK-147 ameliorates learning and memory impairment in animal models without affecting the general behavior or causing behavioral depr …
At 1 to 3 mg/kg, TAK-147 ameliorated the passive avoidance deficit induced by diazepam. ...These results indicate that TAK
23 results