Microscopy and spectroscopy approaches to study GPCR structure and function
British Journal of Pharmacology, EarlyView.Abstract The GPCR signalling cascade is a key pathway responsible for the signal transduction of a multitude of physical and chemical stimuli, including light, odorants, neurotransmitters and hormones. Understanding the structural and functional properties of the GPCR cascade requires direct observation of signalling processes in high spatial and ...
Tomáš Fessl +2 more
wiley +1 more source
A brain imaging study of dopamine receptor D2 availability in cannabis dependent users after recovery from cannabis-induced psychosis. [PDF]
Front Psychiatry, 2023 Weinstein AM.
europepmc +1 more source
On the potassium conductance increase activated by GABAB and dopamine D2 receptors in rat substantia nigra neurones. [PDF]
, 1988 M.G. Lacey +2 more
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Differential G protein activation by the long and short isoforms of the dopamine D2 receptor
British Journal of Pharmacology, EarlyView.Background and Purpose The dopamine D2 receptor is expressed as a short (D2S) and a long (D2L) isoform with 29 additional amino acids in the third intracellular loop. The D2S isoform shows higher presynaptic expression than the D2L isoform, and decreased D2S expression has recently been linked to an increased risk for schizophrenia.
David Reiner‐Link +4 more
wiley +1 more source
Study of changes in rs2283265 polymorphisms in dopamine receptor D2 and rs27072 in dopamine transporter gene (SLC6A3) in patients with attention-deficit hyperactivity disorder. [PDF]
Iran J Child Neurol, 2022 Safavi P +5 more
europepmc +1 more source
ERNEST COST action overview on the (patho)physiology of GPCRs and orphan GPCRs in the nervous system
British Journal of Pharmacology, EarlyView.G protein‐coupled receptors (GPCRs) are a large family of cell surface receptors that play a critical role in nervous system function by transmitting signals between cells and their environment. They are involved in many, if not all, nervous system processes, and their dysfunction has been linked to various neurological disorders representing important
Necla Birgül Iyison +15 more
wiley +1 more source
Modulation of Adenylyl Cyclase Activity in Rat Striatal Homogenate by Dopaminergic Receptors
Journal of Pharmacological Sciences, 2008 We have characterized the modulation of adenylyl cyclase (AC) activity by ligands of dopaminergic receptors in rat striatal homogenate and compared the results with receptor-ligand binding affinities.
Argo Vonk, Reet Reinart, Ago Rinken
doaj
The World of GPCR dimers - Mapping dopamine receptor D2 homodimers in different activation states and configuration arrangements. [PDF]
Comput Struct Biotechnol J, 2023 Bueschbell B +6 more
europepmc +1 more source
Multi-objective generative AI for designing novel brain-targeting small molecules [PDF]
arXivThe strict selectivity of the blood-brain barrier (BBB) represents one of the most formidable challenges to successful central nervous system (CNS) drug delivery. Computational methods to generate BBB permeable drugs in silico may be valuable tools in the CNS drug design pipeline.
arxiv
British Journal of Pharmacology, EarlyView.Abstract G protein‐coupled receptors (GPCRs) are one of the major drug targets. In recent years, computational drug design for GPCRs has mainly focused on static structures obtained through X‐ray crystallography, cryogenic electron microscopy (cryo‐EM) or in silico modelling as a starting point for virtual screening campaigns. However, GPCRs are highly
Marta Lopez‐Balastegui +6 more
wiley +1 more source