Results 31 to 40 of about 31,985 (308)

Positive Allosteric Modulators of Nicotinic Acetylcholine Receptor [PDF]

open access: yesACS Medicinal Chemistry Letters, 2013
Priority Application: Priority date: July 8, 2011 Inventors: Eskildsen, J.; Sams, A. G.; Pueschl, A. Assignee Company: H. Lundbeck A/S, Den. Disease Area: autism, neurodegenerative diseases Biological Target: nicotinic acetylcholine receptor α7 (α7 nAChR) Summary: The patent application claims cyclopropylcarboxamide derivatives as positive allosteric ...
openaire   +2 more sources

Heroin-piracetam mixture: suggested mechanisms of action and risks of misinterpretation for drug users [PDF]

open access: yes, 2017
Piracetam is a positive allosteric modulator of the α-amino-3-hydroxy-5-methyl-4-isoxazolepropionic acid receptor that has been frequently used in the treatment of cognitive disorders.
Cappelletti, Simone   +4 more
core   +1 more source

Structure-guided peptide engineering of a positive allosteric modulator targeting the outer pore of TRPV1 for long-lasting analgesia

open access: yesNature Communications, 2023
TRPV1 as a drug target suffers from side effects of hypothermia. Here, authors engineer a peptide, sRhTx, as a positive allosteric modulator of TRPV1 channel. It potentiates the activity of TRPV1 to reversibly ablate pain-sensing nerve terminals for long-
Heng Zhang   +8 more
doaj   +1 more source

Mechanism of Positive Allosteric Modulators Acting on AMPA Receptors [PDF]

open access: yesThe Journal of Neuroscience, 2005
Ligand-gated ion channels involved in the modulation of synaptic strength are the AMPA, kainate, and NMDA glutamate receptors. Small molecules that potentiate AMPA receptor currents relieve cognitive deficits caused by neurodegenerative diseases such as Alzheimer's disease and show promise in the treatment of depression.
Rongsheng, Jin   +5 more
openaire   +2 more sources

Novel Electrophilic and Photoaffinity Covalent Probes for Mapping the Cannabinoid 1 Receptor Allosteric Site(s) [PDF]

open access: yes, 2015
ACKNOWLEDGMENTS The work was supported by National Institutes of Health grants DA027113 and EY024717 to G.A.T. and DA09158 to A.M. A portion of this work was submitted in 2011 by A. Kulkarni in partial fulfillment of M.S.
Cascio, Maria G.   +12 more
core   +3 more sources

GABAB receptor allosteric modulators exhibit pathway-dependent and species-selective activity. [PDF]

open access: yes, 2017
Positive modulation of the GABAB receptor (GABABR) represents a potentially useful therapeutic approach for the treatment of nicotine addiction. The positive allosteric modulators (PAMs) of GABABR GS39783 and BHF177 enhance GABA-stimulated [35S]GTP γS ...
Cameron, Michael   +8 more
core   +1 more source

Effects of insecticidal ketones present in mint plants on GABA A receptor from mammalian neurons [PDF]

open access: yes, 2017
The genus Mentha, an important member of the Lamiaceae family, is represented by many species commonly known as mint. The insecticidal activity of Mentha oil and its main components has been tested and established against various insects/pests.
Delgado Marín, Leticia Ester   +2 more
core   +2 more sources

4-Chlorophenylguanidine is an ASIC3 agonist and positive allosteric modulator

open access: yesJournal of Pharmacological Sciences, 2017
Acid-sensing ion channels (ASICs) are proton-sensitive sodium channels that open in response to lowered extracellular pH and are expressed in the central and peripheral nervous systems.
Amruta S. Agharkar, Eric B. Gonzales
doaj   +1 more source

A novel small positive allosteric modulator of neuropeptide receptor PAC1-R exerts neuroprotective effects in MPTP mouse Parkinson’s disease model

open access: yesActa Biochimica et Biophysica Sinica, 2022
As a neuropeptide pituitary adenylate cyclase-activating polypeptide (PACAP)-preferring receptor, PAC1-R mediates effective neuroprotective activity.
Fan Guangchun   +4 more
doaj   +1 more source

The positive allosteric modulator of NMDA receptors, GNE‐9278, blocks the ethanol‐induced decrease of excitability in developing retrosplenial cortex neurons from mice

open access: yesNeuropsychopharmacology Reports, 2023
Binge‐like exposure to ethanol during the brain growth spurt triggers apoptotic neurodegeneration in multiple brain regions, including the retrosplenial cortex, a brain region that is part of the hippocampal‐diencephalic‐cingulate memory network. This is
Clark W. Bird, Carlos F. Valenzuela
doaj   +1 more source

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