[HTML][HTML] G protein-coupled receptors regulated by membrane potential

D David, Z Bentulila, M Tauber… - International Journal of …, 2022 - mdpi.com
G protein-coupled receptors (GPCRs) are involved in a vast majority of signal transduction
processes. Although they span the cell membrane, they have not been considered to be …

[HTML][HTML] TAAR1 dependent and independent actions of the potential antipsychotic and dual TAAR1/5-HT1A receptor agonist SEP-363856

M Saarinen, I Mantas, I Flais, R Ågren… - …, 2022 - nature.com
Abstract SEP-363856 (SEP-856) is a novel antipsychotic under clinical development. It
displays a unique pattern of receptor interaction, with only weak (partial agonist) activity at …

[HTML][HTML] Role of iso-receptors in receptor-receptor interactions with a focus on dopamine iso-receptor complexes

LF Agnati, D Guidolin, C Cervetto… - Reviews in the …, 2016 - degruyter.com
Intercellular and intracellular communication processes consist of signals and
recognition/decoding apparatuses of these signals. In humans, the G protein-coupled …

[PDF][PDF] A novel voltage sensor in the orthosteric binding site of the M2 muscarinic receptor

O Barchad-Avitzur, MF Priest, N Dekel, F Bezanilla… - Biophysical journal, 2016 - cell.com
G protein-coupled receptors (GPCRs) mediate many signal transduction processes in the
body. The discovery that these receptors are voltage-sensitive has changed our …

The fast-off hypothesis revisited: A functional kinetic study of antipsychotic antagonism of the dopamine D2 receptor

K Sahlholm, H Zeberg, J Nilsson, SO Ögren… - European …, 2016 - Elsevier
Newer,“atypical” antipsychotics carry a lower risk of motor side-effects than older,“typical”
compounds. It has been proposed that a~ 100-fold faster dissociation from the dopamine D …

[HTML][HTML] Voltage-dependent dopamine potency at D1-like dopamine receptors

R Ågren, K Sahlholm - Frontiers in Pharmacology, 2020 - frontiersin.org
In recent years, transmembrane voltage has been found to modify agonist potencies at
several G protein-coupled receptors (GPCRs). Whereas the voltage sensitivities of the Gα i/o …

[HTML][HTML] Membrane potential controls the efficacy of catecholamine-induced β1-adrenoceptor activity

A Birk, A Rinne, M Bünemann - Journal of Biological Chemistry, 2015 - ASBMB
G protein-coupled receptors (GPCRs) are membrane-located proteins and, therefore, are
exposed to changes in membrane potential (VM) in excitable tissues. These changes have …

Agonist and Antagonist Effects of Aripiprazole on D2-Like Receptors Controlling Rat Brain Dopamine Synthesis Depend on the Dopaminergic Tone

GF Ma, N Raivio, J Sabrià, J Ortiz - International Journal of …, 2015 - academic.oup.com
Background: The atypical antipsychotic drug aripiprazole binds with high affinity to a number
of G protein coupled receptors, including dopamine D2 receptors, where its degree of …

Voltage dependence of prostanoid receptors

M Kurz, AL Krett, M Bünemann - Molecular Pharmacology, 2020 - ASPET
G protein–coupled receptors (GPCRs) are the largest class of transmembrane receptors and
serve as signal mediators to transduce information from extracellular signals such as …

[HTML][HTML] Dopamine-induced arrestin recruitment and desensitization of the dopamine D4 receptor is regulated by G protein-coupled receptor kinase-2

V Burström, R Ågren, N Betari, M Valle-León… - Frontiers in …, 2023 - frontiersin.org
The dopamine D 4 receptor (D 4 R) is expressed in the retina, prefrontal cortex, and
autonomic nervous system and has been implicated in attention deficit hyperactivity disorder …