[HTML][HTML] Distinct inactive conformations of the dopamine D2 and D3 receptors correspond to different extents of inverse agonism

JR Lane, AM Abramyan, P Adhikari, AC Keen, KH Lee… - Elife, 2020 - elifesciences.org
By analyzing and simulating inactive conformations of the highly homologous dopamine D2
and D3 receptors (D2R and D3R), we find that eticlopride binds D2R in a pose very similar …

Enhancing the signaling of GPCRs via orthosteric ions

HCS Chan, Y Xu, L Tan, H Vogel, J Cheng… - ACS Central …, 2020 - ACS Publications
G protein-coupled receptors play essential roles in cellular processes such as neuronal
signaling, vision, olfaction, tasting, and metabolism. As GPCRs are the most important drug …

[HTML][HTML] A complete assessment of dopamine receptor-ligand interactions through computational methods

B Bueschbell, CAV Barreto, AJ Preto, AC Schiedel… - Molecules, 2019 - mdpi.com
Background: Selectively targeting dopamine receptors (DRs) has been a persistent
challenge in the last years for the development of new treatments to combat the large variety …

[HTML][HTML] Distinct Dopamine D2 Receptor Antagonists Differentially Impact D2 Receptor Oligomerization

E Wouters, AR Marín, JAR Dalton, J Giraldo… - International journal of …, 2019 - mdpi.com
Dopamine D2 receptors (D2R) are known to form transient homodimer complexes, of which
the increased formation has already been associated with development of schizophrenia …

Homogeneous, real-time NanoBRET binding assays for the histamine H3 and H4 receptors on living cells

TAM Mocking, EWE Verweij, HF Vischer, R Leurs - Molecular pharmacology, 2018 - ASPET
Receptor-binding affinity and ligand-receptor residence time are key parameters for the
selection of drug candidates and are routinely determined using radioligand competition …

[HTML][HTML] Inverse salt sensitivity of blood pressure is associated with an increased renin-angiotensin system activity

JJ Gildea, P Xu, KA Schiermeyer, W Yue, RM Carey… - Biomedicines, 2022 - mdpi.com
High and low sodium diets are associated with increased blood pressure and
cardiovascular morbidity and mortality. The paradoxical response of elevated BP in low salt …

[HTML][HTML] The action of a negative allosteric modulator at the dopamine D2 receptor is dependent upon sodium ions

CJ Draper-Joyce, RK Verma, M Michino, J Shonberg… - Scientific Reports, 2018 - nature.com
Sodium ions (Na+) allosterically modulate the binding of orthosteric agonists and
antagonists to many class AG protein-coupled receptors, including the dopamine D2 …

Trace amine-associated receptor 1 agonists RO5263397 and RO5166017 attenuate quinpirole-induced yawning but not hypothermia in rats

JN Siemian, Y Zhang, JX Li - Behavioural pharmacology, 2017 - journals.lww.com
Increasing evidence suggests that trace amine-associated receptor 1 (TAAR1) is an
important modulator of the dopaminergic system. Existing molecular evidence indicates that …

[HTML][HTML] Machine-learning-based analytics for risk forecasting of anaphylaxis during general anesthesia

S Liu, Y Suzuki, T Yorozuya, M Mogi - ImmunoInformatics, 2022 - Elsevier
Perioperative anaphylaxis has a risk of mortality and compromised quality of patient care. It
is difficult to design an evaluation system for risk of anaphylaxis using preoperative tests …

Close Homolog of L1 (CHL1) and its role in the dopaminergic system: biochemical and behavioral consequences of CHL1 and dopamine receptor type 2 interaction

L Fernandes - 2023 - ediss.sub.uni-hamburg.de
Dopamine is a neurotransmitter essential to coordinate biochemical and behavioral
functions in the striatum by modulating dopamine receptor signaling, including the …