Literature DB >> 12177685

Ensaculin (KA-672 HCl): a multitransmitter approach to dementia treatment.

Robert Hoerr1, Michael Noeldner.   

Abstract

Ensaculin, a novel benzopyranone substituted with a piperazine moiety, showed memory-enhancing effects in paradigms of passive and conditioned avoidance in both normal and artificially amnesic rodents. It exhibited neuroprotective activities in an NMDA toxicity model and neurotrophic effects in primary cultured rat brain cells. The compound could be characterized as a weak NMDA receptor-operated channel blocker. In receptor-binding studies, ensaculin was found to have high affinities to serotonergic 5-HT(1A) and 5-HT(7) receptors, adrenergic alpha(1), and dopaminergic D(2) and D(3) receptors. Due to its unique pharmacodynamic profile, ensaculin may have potential as an antidementia agent acting on various transmitter systems.

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Year:  2002        PMID: 12177685      PMCID: PMC6741668          DOI: 10.1111/j.1527-3458.2002.tb00220.x

Source DB:  PubMed          Journal:  CNS Drug Rev        ISSN: 1080-563X


  7 in total

Review 1.  Non-cholinergic strategies for treating and preventing Alzheimer's disease.

Authors:  P Murali Doraiswamy
Journal:  CNS Drugs       Date:  2002       Impact factor: 5.749

2.  The coumarin scopoletin potentiates acetylcholine release from synaptosomes, amplifies hippocampal long-term potentiation and ameliorates anticholinergic- and age-impaired memory.

Authors:  A Hornick; A Lieb; N P Vo; J M Rollinger; H Stuppner; H Prast
Journal:  Neuroscience       Date:  2011-09-10       Impact factor: 3.590

3.  Coumarin derivatives as acetyl- and butyrylcholinestrase inhibitors: An in vitro, molecular docking, and molecular dynamics simulations study.

Authors:  Marwa N Abu-Aisheh; Amal Al-Aboudi; Mohammad S Mustafa; Mustafa M El-Abadelah; Saman Yousuf Ali; Zaheer Ul-Haq; Mohammad S Mubarak
Journal:  Heliyon       Date:  2019-04-28

Review 4.  Molecular docking studies of coumarin hybrids as potential acetylcholinesterase, butyrylcholinesterase, monoamine oxidase A/B and β-amyloid inhibitors for Alzheimer's disease.

Authors:  Samina Khan Yusufzai; Mohammad Shaheen Khan; Othman Sulaiman; Hasnah Osman; Dalily Nabilah Lamjin
Journal:  Chem Cent J       Date:  2018-12-04       Impact factor: 4.215

5.  Synthesis of New Biscoumarin Derivatives, In Vitro Cholinesterase Inhibition, Molecular Modelling and Antiproliferative Effect in A549 Human Lung Carcinoma Cells.

Authors:  Monika Hudáčová; Slávka Hamuľaková; Eva Konkoľová; Rastislav Jendželovský; Jana Vargová; Juraj Ševc; Peter Fedoročko; Ondrej Soukup; Jana Janočková; Veronika Ihnatova; Tomáš Kučera; Petr Bzonek; Nikola Novakova; Daniel Jun; Lucie Junova; Jan Korábečný; Kamil Kuča; Mária Kožurková
Journal:  Int J Mol Sci       Date:  2021-04-07       Impact factor: 5.923

6.  Multi-Target-Directed Ligands and other Therapeutic Strategies in the Search of a Real Solution for Alzheimer's Disease.

Authors:  Angel Agis-Torres; Monica Sölhuber; Maria Fernandez; J M Sanchez-Montero
Journal:  Curr Neuropharmacol       Date:  2014-01       Impact factor: 7.363

Review 7.  Coumarin-piperazine derivatives as biologically active compounds.

Authors:  Kinga Ostrowska
Journal:  Saudi Pharm J       Date:  2019-12-07       Impact factor: 4.330

  7 in total

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