Cyclic nucleotide-gated channels: structural basis of ligand efficacy and allosteric modulation [PDF]
Most working proteins, including metabolic enzymes, transcription regulators, and membrane receptors, transporters, and ion channels, share the property of allosteric coupling. The term 'allosteric' means that these proteins mediate indirect interactions
Lester, Henry A.+2 more
core +1 more source
Examining the predictive validity of alcohol‐seeking following punishment‐imposed abstinence in mice
Animal models of alcohol use disorder are critical to understand the neurochemical mechanisms underlying this disorder to inform targeted medication development. However, quite often the validity of commonly used animal models remains untested. Here, we optimized a highly used model of abstinence in mice and demonstrated the predictive validity of the ...
Linh Tran+3 more
wiley +1 more source
Effects of nicotine administration on amyloid precursor protein metabolism, neural cell genesis and acquisition of spatial memory [PDF]
Nicotine is reported to improve learning and memory in experimental animals. Improved learning and memory has also been related to increased neural cell genesis in the dentate gyrus of the brain hippocampal formation.
Scerri, Charles
core
Abstract Background and Aims Substance use disorders (SUD) lead to a high burden of disease, yet treatment options are limited. Cannabidiol (CBD) is being investigated as a potential therapeutic target due to its pharmacological properties and mode of action in the endocannabinoid system.
Bertrand Redonnet+4 more
wiley +1 more source
A fluorophore attached to nicotinic acetylcholine receptor beta M2 detects productive binding of agonist to the alpha delta site [PDF]
To study conformational transitions at the muscle nicotinic acetylcholine (ACh) receptor (nAChR), a rhodamine fluorophore was tethered to a Cys side chain introduced at the beta-19' position in the M2 region of the nAChR expressed in Xenopus oocytes ...
Auyeung, Vincent C.+7 more
core
Psychedelic‐assisted treatment for substance use disorder: A narrative systematic review
Abstract Background and aims This is the first systematic review of the extant literature on all major psychedelic‐assisted treatment for alcohol use disorder (AUD), tobacco use disorder (TUD) and other substance use disorders (SUD). We aimed to summarise the evidence for efficacy of psychedelic‐assisted treatment for AUD, TUD, and SUD; to evaluate its
Theodore Piper+7 more
wiley +1 more source
G protein-coupled receptors not currently in the spotlight: free fatty acid receptor 2 and GPR35 [PDF]
It is widely appreciated that G protein-coupled receptors have been the most successfully exploited class of targets for the development of small molecule medicines. Despite this, to date, less than 15% of the non-olfactory G protein-coupled receptors in
Milligan, Graeme
core +1 more source
Abstract Background and Objectives Existing opioid agonist therapy (OAT) guidelines are far from sufficient to address rising opioid tolerances and potency of the unregulated opioid market in North America. Inadequate starting doses of OAT are a universally recognized barrier for people who use fentanyl.
Pouya Azar+11 more
wiley +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]
Muthusamy AK+9 more
europepmc +1 more source
Differential Contribution of Subunit Interfaces to α 9 α 10 Nicotinic Acetylcholine Receptor Function [PDF]
Nicotinic acetylcholine receptors can be assembled from either homomeric or heteromeric pentameric subunit combinations. At the interface of the extracellular domains of adjacent subunits lies the acetylcholine binding site, composed of a principal ...
Boffi, Juan Carlos+11 more
core +3 more sources