Positive AMPA receptor modulation in the treatment of neuropsychiatric disorders: A long and winding road

B Kadriu, L Musazzi, JN Johnston, LE Kalynchuk… - Drug discovery today, 2021 - Elsevier
Glutamatergic transmission is widely implicated in neuropsychiatric disorders, and the
discovery that ketamine elicits rapid-acting antidepressant effects by modulating α-amino-3 …

2-Aminothiophene scaffolds: Diverse biological and pharmacological attributes in medicinal chemistry

K Bozorov, LF Nie, J Zhao, HA Aisa - European journal of medicinal …, 2017 - Elsevier
Aminothiophenes are important five-membered heterocyclic building blocks in organic
synthesis, and the chemistry of these small molecules is still develo** based on the …

Ligand-gated ion channels: new insights into neurological disorders and ligand recognition

D Lemoine, R Jiang, A Taly, T Chataigneau… - Chemical …, 2012 - ACS Publications
1. INTRODUCTION Ligand-gated ion channels (LGICs) mediate intercellular communication
by converting the binding of a neurotransmitter that is released from the presynaptic terminal …

Diversity of AMPA receptor ligands: Chemotypes, binding modes, mechanisms of action, and therapeutic effects

EA Golubeva, MI Lavrov, EV Radchenko, VA Palyulin - Biomolecules, 2022 - mdpi.com
L-Glutamic acid is the main excitatory neurotransmitter in the central nervous system (CNS).
Its associated receptors localized on neuronal and non-neuronal cells mediate rapid …

Cognitive enhancers (nootropics). Part 1: drugs interacting with receptors

W Froestl, A Muhs, A Pfeifer - Journal of Alzheimer's disease, 2012 - content.iospress.com
Cognitive enhancers (nootropics) are drugs to treat cognition deficits in patients suffering
from Alzheimer's disease, schizophrenia, stroke, attention deficit hyperactivity disorder, or …

AMPA receptor potentiators: from drug design to cognitive enhancement

KM Partin - Current opinion in pharmacology, 2015 - Elsevier
Highlights•Better AMPAR positive allosteric modulators are being developed.•New
methodologies and approaches enhance the analysis of their activity in vitro.•AMPA positive …

The Isoxazole Ring and Its N‐Oxide: A Privileged Core Structure in Neuropsychiatric Therapeutics

GN Pairas, F Perperopoulou, PG Tsoungas… - …, 2017 - Wiley Online Library
Mental disorders are neuropsychiatric conditions that are marked by unusual or irregular
thinking, feelings, or behavior, and lead to distress and/or impaired functions. Major …

Structural basis for positive allosteric modulation of AMPA and kainate receptors

K Frydenvang, DS Pickering… - The Journal of …, 2022 - Wiley Online Library
This paper summarizes the present knowledge on how positive allosteric modulators
(PAMs) interact with the ligand‐binding domain (LBD) of AMPA and kainate receptors …

Structure and mechanism of glutamate receptor ion channel assembly, activation and modulation

ML Mayer - Current opinion in neurobiology, 2011 - Elsevier
Ionotropic glutamate receptors (iGluRs) are ligand gated ion channels that mediate
excitatory synaptic transmission in the brain of vertebrates. A rapidly growing body of crystal …

“Reported, but still unknown.” A closer look into 3, 4-bis-and 3, 4, 5-tris (trifluoromethyl) pyrazoles

II Gerus, RX Mironetz, IS Kondratov… - The Journal of …, 2012 - ACS Publications
Straightforward practical synthetic approaches to 3, 4-bis-and 3, 4, 5-tris (trifluoromethyl)
pyrazoles have been developed. The key step of the both syntheses is a transformation of …