Synthesis and characterization of a bidirectional photoswitchable antagonist toolbox for real-time GPCR photopharmacology

NJ Hauwert, TAM Mocking… - Journal of the …, 2018 - ACS Publications
Noninvasive methods to modulate G protein-coupled receptors (GPCRs) with temporal and
spatial precision are in great demand. Photopharmacology uses photons to control in situ …

A Review on Current Research On H3 And H4 Receptors

V Chaurasiya, V Bhoir, S Bhundere… - Asian Journal of …, 2023 - ajprd.com
This review article provides an overview of the structure, location, and functional uses of H3
and H4 histamine receptors. It examines the current research on the topic, including the …

Histamine inhibits the melanin‐concentrating hormone system: implications for sleep and arousal

GS Parks, ND Olivas, T Ikrar… - The Journal of …, 2014 - Wiley Online Library
Key points Melanin‐concentrating hormone (MCH) neurons express histamine‐3 receptor
(H3R) mRNA but not histamine‐1 (H1R) or histamine‐2 (H2R) receptor mRNA. Histamine …

Histamine H3 Receptor Activation Modulates Glutamate Release in the Corticostriatal Synapse by Acting at CaV2.1 (P/Q-Type) Calcium Channels and GIRK (KIR3) …

H Vázquez-Vázquez, C Gonzalez-Sandoval… - Cellular and Molecular …, 2022 - Springer
The striatum is innervated by histaminergic fibers and expresses a high density of histamine
H 3 receptors (H 3 Rs), present on medium spiny neurons (MSNs) and corticostriatal …

[HTML][HTML] Voltage sensitivities and deactivation kinetics of histamine H3 and H4 receptors

K Sahlholm, J Nilsson, D Marcellino, K Fuxe… - Biochimica et Biophysica …, 2012 - Elsevier
Agonist potency at some neurotransmitter receptors has been shown to be regulated by
voltage, a mechanism which has been suggested to play a crucial role in the regulation of …

Voltage‐dependence of the human dopamine D2 receptor

K Sahlholm, J Nilsson, D Marcellino, K Fuxe… - Synapse, 2008 - Wiley Online Library
The dopamine D2 receptor plays a critical role in activity‐dependent synaptic plasticity in the
striatum, and regulates the transitions between different states of electrical activity. The D2 …

Cocaine produces D2R-mediated conformational changes in the adenosine A2AR-dopamine D2R heteromer

D Marcellino, G Navarro, K Sahlholm, J Nilsson… - Biochemical and …, 2010 - Elsevier
Adenosine A2A receptors (A2ARs) and dopamine D2 receptors (D2Rs) form constitutive
heteromers in living cells and exhibit a strong functional antagonistic interaction. Recent …

[HTML][HTML] Membrane Heteroreceptor Complexes as Second-Order Protein Modulators: A Novel Integrative Mechanism through Allosteric Receptor–Receptor …

M Mirchandani-Duque, M Choucri… - Membranes, 2024 - mdpi.com
Bioluminescence and fluorescence resonance energy transfer (BRET and FRET) together
with the proximity ligation method revealed the existence of G-protein-coupled receptors …

[HTML][HTML] Engineering of an artificial light-modulated potassium channel

LN Caro, CJ Moreau, A Estrada-Mondragón, OP Ernst… - 2012 - journals.plos.org
Ion Channel-Coupled Receptors (ICCRs) are artificial receptor-channel fusion proteins
designed to couple ligand binding to channel gating. We previously validated the ICCR …

Molecular aspects of histamine receptors

TAM Mocking, R Bosma, SN Rahman… - … : Preclinical and clinical …, 2016 - Springer
Histamine mediates a multitude of physiological effects in the human body by activating four
histamine receptor subtypes. Histamine receptors have proven to be promising drug targets …