Therapeutic strategies for Alzheimer's disease in clinical trials

J Godyń, J Jończyk, D Panek, B Malawska - Pharmacological Reports, 2016 - Elsevier
Alzheimer's disease (AD) is considered to be the most common cause of dementia and is an
incurable, progressive neurodegenerative disorder. Current treatment of the disease …

G-protein-coupled receptors in CNS: a potential therapeutic target for intervention in neurodegenerative disorders and associated cognitive deficits

S Azam, ME Haque, M Jakaria, SH Jo, IS Kim, DK Choi - Cells, 2020 - mdpi.com
Neurodegenerative diseases are a large group of neurological disorders with diverse
etiological and pathological phenomena. However, current therapeutics rely mostly on …

Therapeutic potential of multifunctional tacrine analogues

M Przybyłowska, S Kowalski… - Current …, 2019 - ingentaconnect.com
Tacrine is a potent inhibitor of cholinesterases (acetylcholinesterase and
butyrylcholinesterase) that shows limiting clinical application by liver toxicity. In spite of this …

A new serotonin 5-HT6 receptor antagonist with procognitive activity – Importance of a halogen bond interaction to stabilize the binding

JA González-Vera, RA Medina, M Martín-Fontecha… - Scientific reports, 2017 - nature.com
Serotonin 5-HT6 receptor has been proposed as a promising therapeutic target for cognition
enhancement though the development of new antagonists is still needed to validate these …

AVN-211, Novel and Highly Selective 5-HT6 Receptor Small Molecule Antagonist, for the Treatment of Alzheimer's Disease

AV Ivachtchenko, Y Lavrovsky… - Molecular …, 2016 - ACS Publications
Within the past decade several novel targets have been indicated as key players in
Alzheimer-type dementia and associated conditions, including a “frightening” memory loss …

Neuropathic pain-alleviating effects of pyrazole-conjugated arylsulfonamides as 5-HT6 receptor antagonists

JR Hong, H Choo, G Nam - Bioorganic & Medicinal Chemistry Letters, 2017 - Elsevier
A novel series of arylsulfonylaminomethyl-3-(1-phenyl-5-isopropyl) pyrazoles was evaluated
for serotonin receptor subtype 6 (5-HT 6 R) antagonistic effects in vitro. We also investigated …

5-HT6 receptor antagonist attenuates the memory deficits associated with neuropathic pain and improves the efficacy of gabapentinoids

P Jayarajan, R Nirogi, A Shinde, V Goura… - Pharmacological …, 2015 - Elsevier
Background Memory deficit is a co-morbid disorder in patients suffering from neuropathic
pain. Gabapentin and pregabalin (gabapentinoids) are among the widely prescribed …

AVN-322 is a safe orally bio-available potent and highly selective antagonist of 5-HT6R with demonstrated ability to improve impaired memory in animal models

AV Ivachtchenko, YA Ivanenkov… - Current Alzheimer …, 2017 - ingentaconnect.com
Background: In recent years, 5-hydroxytryptamine subtype 6 receptor (5-HT6 receptor, 5-
HT6R) has emerged as a promising therapeutic target for the treatment of neuropathological …

[DOC][DOC] Preclinical evaluation of AVN-322, novel and highly selective 5-HT6 receptor antagonist, for the treatment of Alzheimer's disease

A Ivachtchenko, Y Ivanenkov, M Veselov - Curr Alzheimer Res, 2016 - avineuro.ru
In recent years, 5-hydroxytryptamine subtype 6 receptor (5-HT 6 receptor, 5-HT 6 R) has
rapidly emerged as a promising therapeutic target for the treatment of neuropathological …