Conformational variability of the glycine receptor M2 domain in response to activation by different agonists [PDF]
, 2007 Models describing the structural changes mediating cys-loop receptor activation generally give little attention to the possibility that different agonists may promote activation via distinct M2 pore-lining domain structural rearrangements.
Akabas +30 more
core +3 more sources
Is there a role for cannabidiol in obesity, metabolic syndrome and binge eating?
British Journal of Pharmacology, EarlyView.Cannabidiol (CBD) is one of the most abundant phytocannabinoids isolated from the Cannabis sativa plant. CBD is a lipophilic, non‐intoxicating substance that differently from Δ9‐tetrahydrocannabinol (Δ9‐THC) does not present the typical profile of a drug of abuse.
Luca Botticelli +7 more
wiley +1 more source
Combined nutritional stress and a new systemic pesticide (flupyradifurone, Sivanto®) reduce bee survival, food consumption, flight success, and thermoregulation. [PDF]
, 2019 Flupyradifurone (FPF, Sivanto®) is a new butenolide insecticide that, like the neonicotinoids, is a systemic nicotinic acetylcholine receptor (nAChR) agonist.
Nieh, James C, Tong, Linda, Tosi, Simone
core +4 more sources
Evaluation of preclinical antipsychotic models used to support first‐in‐human clinical trials
British Journal of Pharmacology, EarlyView.Abstract Schizophrenia is regarded as a complex and heterogeneous psychiatric disorder, characterised by diverse symptoms and comorbidities, which complicate both clinical management and drug development. Current pharmacological treatment, primarily based on dopamine D2 receptor antagonism or partial agonism, which has not markedly progressed since the
Thi Viet Ha Nguyen +2 more
wiley +1 more source
CellsAcetylcholine signaling is attenuated in early Alzheimer’s disease (AD) and other dementias. A significant reduction in the expression of nicotinic acetylcholine receptors (nAChRs) in the brain of AD patients has also been reported in several molecular ...
Alessio Crestini +10 more
doaj +1 more source
Three Mutations Convert the Selectivity of a Protein Sensor from Nicotinic Agonists to S-Methadone for Use in Cells, Organelles, and Biofluids. [PDF]
J Am Chem Soc, 2022 Muthusamy AK +9 more
europepmc +1 more source
Single-channel behavior of heteromeric α1β glycine receptors: an attempt to detect a conformational change before the channel opens [PDF]
, 2004 The α1β heteromeric receptors are likely to be the predominant synaptic form of glycine receptors in the adult. Their activation mechanism was investigated by fitting putative mechanisms to single-channel recordings obtained at four glycine ...
Beato, M. +4 more
core
Simultaneous release of glutamate and acetylcholine from single magnocellular "cholinergic" basal forebrain neurons [PDF]
, 2006 Basal forebrain (BF) neurons provide the principal cholinergic drive to the hippocampus and cortex. Their degeneration is associated with the cognitive defects of Alzheimer's disease. Immunohistochemical studies suggest that some of these neurons contain
Abogadie, FC, Allen, TGJ, Brown, DA
core +1 more source
A Pharmacological Comparison of Two Isomeric Nicotinic Receptor Agonists: The Marine Toxin Isoanatabine and the Tobacco Alkaloid Anatabine [PDF]
, 2020 Hong Xing +3 more
openalex +1 more source
British Journal of Pharmacology, EarlyView.Abstract Background and Purpose Lactate, historically viewed as a metabolic by‐product, has emerged as a signalling molecule via the G protein–coupled receptor Hydroxycarboxylic Acid Receptor 1 (HCAR1). The receptor is primarily expressed in adipocytes but also found in various other tissues.
Simon Lind +6 more
wiley +1 more source