The histamine H3 receptor: structure, pharmacology, and function

G Nieto-Alamilla, R Márquez-Gómez… - Molecular …, 2016 - ASPET
Among the four G protein–coupled receptors (H1–H4) identified as mediators of the biologic
effects of histamine, the H3 receptor (H3R) is distinguished for its almost exclusive …

The signaling signature of the neurotensin type 1 receptor with endogenous ligands

É Besserer-Offroy, RL Brouillette, S Lavenus… - European journal of …, 2017 - Elsevier
The human neurotensin 1 receptor (hNTS1) is a G protein-coupled receptor involved in
many physiological functions, including analgesia, hypothermia, and hypotension. To gain a …

Differential Role of Serines and Threonines in Intracellular Loop 3 and C-Terminal Tail of the Histamine H4 Receptor in β-Arrestin and G Protein-Coupled Receptor …

EWE Verweij, B Al Araaj, WR Prabhata… - ACS pharmacology & …, 2020 - ACS Publications
The histamine H4 receptor (H4R) activates Gαi-mediated signaling and recruits β-arrestin2
upon stimulation with histamine. β-Arrestins play a regulatory role in G protein-coupled …

[HTML][HTML] Ligand-directed biased agonism at human histamine H3 receptor isoforms across Gαi/o-and β-arrestin2-mediated pathways

SN Rahman, F Imhaouran, R Leurs… - Biochemical …, 2023 - Elsevier
The histamine H 3 receptor (H 3 R) is a neurotransmitter receptor that is primarily found in
the brain, where it controls the release and synthesis of histamine, as well as the release of …

Discovery of a Tritiated Radioligand with High Affinity and Selectivity for the Histamine H3 Receptor

D Mönnich, M Nagl, L Forster, N Rosier… - ACS Medicinal …, 2023 - ACS Publications
Radioligands used previously for histamine H3 receptor (H3R) are accompanied by a
number of disadvantages. In this study, we report the synthesis of the new H3R radioligand …

Altered Subcellular Distribution of the 75‐kD a DISC 1 Isoform, cAMP Accumulation, and Decreased Neuronal Migration in Schizophrenia and Bipolar Disorder …

J Muñoz‐Estrada, G Benítez‐King… - CNS Neuroscience …, 2015 - Wiley Online Library
Summary Background DISC 1 (Disrupted‐In‐Schizophrenia‐1) is considered a genetic risk
factor for schizophrenia (SZ) and bipolar disorder (BD). DISC 1 regulates microtubule …

[HTML][HTML] Effect of moderate prenatal ethanol exposure on the differential expression of two histamine H3 receptor isoforms in different brain regions of adult rat …

S Davies, KS Lujan, EJ Rappaport… - Frontiers in …, 2023 - frontiersin.org
We have reported that prenatal alcohol exposure (PAE) elevates histamine H 3 receptor
(H3R) agonist-mediated inhibition of glutamatergic neurotransmission in the dentate gyrus …

Inhibition of uterine contractility by thalidomide analogs via phosphodiesterase-4 inhibition and calcium entry blockade

E Fernández-Martínez, H Ponce-Monter… - Molecules, 2016 - mdpi.com
Uterine relaxation is crucial during preterm labor. Phosphodiesterase-4 (PDE-4) inhibitors
have been proposed as tocolytics. Some thalidomide analogs are PDE-4 inhibitors. The aim …

Chronic administration of the histamine H3 receptor agonist immepip decreases l-Dopa-induced dyskinesias in 6-hydroxydopamine-lesioned rats

A Avila-Luna, C Ríos, A Gálvez-Rosas, S Montes… - …, 2019 - Springer
Abstract Rationale Histamine H 3 receptors (H 3 Rs) are co-expressed with dopamine D 1
receptors (D 1 Rs) by striato-nigral medium spiny GABAergic neurons, where they …

In silico and in vitro studies of two non‐imidazole multiple targeting agents at histamine H3 receptors and cholinesterase enzymes

N Ghamari, S Dastmalchi, O Zarei… - Chemical Biology & …, 2020 - Wiley Online Library
Recently, multi‐target directed ligands have been of research interest for multifactorial
disorders such as Alzheimer's disease (AD). Since H3 receptors (H3Rs) and …