Multitargeting the Action of 5-HT6 Serotonin Receptor Ligands by Additional Modulation of Kinases in the Search for a New Therapy for Alzheimer's Disease: Can It …

K Czarnota-Łydka, K Kucwaj-Brysz, P Pyka… - International Journal of …, 2022 - mdpi.com
In view of the unsatisfactory treatment of cognitive disorders, in particular Alzheimer's
disease (AD), the aim of this review was to perform a computer-aided analysis of the state of …

Effects of the 5-HT6 receptor antagonist idalopirdine on extracellular levels of monoamines, glutamate and acetylcholine in the rat medial prefrontal cortex

A Mørk, RV Russell, IEM de Jong, G Smagin - European Journal of …, 2017 - Elsevier
Idalopirdine (Lu AE58054) is a high affinity and selective antagonist for the human serotonin
5-HT 6 receptor (K i 0.83 nM) in phase III development for mild-to-moderate Alzheimer's …

The hybrid compounds as multi-target ligands for the treatment of Alzheimer's disease: considerations on donepezil

HO Gulcan, M Kosar - Current Topics in Medicinal Chemistry, 2022 - ingentaconnect.com
The strategies to combat Alzheimer's Disease (AD) have been changing with respect to the
failures of many drug candidates assessed in clinical studies, the complex pathophysiology …

The selective 5-HT6 receptor antagonist SLV has putative cognitive-and social interaction enhancing properties in rodent models of cognitive impairment

N De Bruin, A Van Loevezijn, KM Wicke… - … of Learning and …, 2016 - Elsevier
In the present study, our aim was to investigate whether the novel highly selective 5-
hydroxytryptamine 6 (5-HT 6) receptor antagonist SLV can ameliorate impairments in …

Dopamine and serotonin modulation of motor and non-motor functions of the non-human primate striato-pallidal circuits in normal and pathological states

V Sgambato-Faure, L Tremblay - Journal of Neural Transmission, 2018 - Springer
Thanks to the non-human primate (NHP), we have shown that the pharmacological
disturbance of the anterior striatum or of external globus pallidus triggers a set of motivation …

[HTML][HTML] 5-HT6 Receptor neutral antagonists protect astrocytes: a lesson from 2-phenylpyrrole derivatives

M Drop, P Koczurkiewicz-Adamczyk, O Bento… - European Journal of …, 2024 - Elsevier
ABSTRACT The serotonin type 6 receptor (5-HT 6 R) displays a strong constitutive activity,
suggesting it participates largely in the physiological and pathological processes controlled …

Natural product-based multitargeted ligands for Alzheimer's disease treatment?

NT Tzvetkov, AG Atanasov - Future Medicinal Chemistry, 2018 - Taylor & Francis
Alzheimer's disease (AD) belongs to the most intensively investigated and discussed
disorders in modern medicine and community worldwide. Only few clinical diagnoses evoke …

Alzheimer's Disease: Dawn of a New Era?

F Amirrad, E Bousoik, K Shamloo, H Al-Shiyab… - 2017 - digitalcommons.chapman.edu
Alzheimer's disease (AD) is an irreversible neurodegenerative disease characterized by a
progressive decline in cognition and memory, leading to significant impairment in daily …

Synthesis of azepino [4, 5-b] indol-4-ones via MCR/free radical cyclization and in vitro–in silico studies as 5-Ht6R ligands

A Renteria-Gomez, A Islas-Jácome… - Bioorganic & Medicinal …, 2016 - Elsevier
A series of nine new 3-acetamide-azepino [4, 5-b] indol-4-ones were synthesized in two
steps:(i) multicomponent reaction (Ugi-4CR/SN 2) and (ii) free radical-mediated cyclization …

Sonochemical synthesis and biological evaluation of isoquinolin-1 (2H)-one/isoindolin-1-one derivatives: discovery of a positive ago-allosteric modulator (PAAM) of …

JS Kumar, R Naimisha, B Thirupataiah, GS Reddy… - Bioorganic …, 2022 - Elsevier
Efforts have been devoted for the discovery and development of positive allosteric
modulators (PAMs) of 5-HT 2C R because of their potential advantages over the orthosteric …