Results 51 to 60 of about 4,488 (204)

Optimizing the Expression of Human Dopamine Receptors in Escherichia coli [PDF]

, 2021
The human dopamine receptors D2S and D3 belong to the group of G protein-coupled receptors (GPCRs) and are important drug targets. Structural analyses and development of new receptor subtype specific drugs have been impeded by low expression yields or ...
Allikalt, Anni, Boritzki, Vanessa, Gmeiner, Peter, Hübner, Harald, Wöhrl, Birgitta M.   +4 more
core   +2 more sources

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

, 2018
Sodium ions (Na+) allosterically modulate the binding of orthosteric agonists and antagonists to many class A G protein-coupled receptors, including the dopamine D2 receptor (D2R).
Abramyan, AM, Capuano, B, Christopoulos, A, Draper-Joyce, CJ, Herenbrink, CK, Javitch, JA, Kopinathan, A, Lane, JR, Michino, M, Scammells, PJ, Shi, L, Shonberg, J, Thal, DM, Verma, RK   +13 more
core   +1 more source

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

, 2020
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 to that in the D3R/eticlopride structure but incompatible with the D2R ...
Abramyan, Ara M, Adhikari, Pramisha, Javitch, Jonathan A, Keen, Alastair C, Lane, J Robert, Lee, Kuo-Hao, Lim, Herman D, Sanchez, Julie, Shi, Lei, Verma, Ravi Kumar, Yano, Hideaki   +10 more
core   +2 more sources

Platelet Activating Factor Receptor Activation Improves siRNA Uptake and RNAi Responses in Well-differentiated Airway Epithelia

Molecular Therapy: Nucleic Acids, 2014
Well-differentiated human airway epithelia present formidable barriers to efficient siRNA delivery. We previously reported that treatment of airway epithelia with specific small molecules improves oligonucleotide uptake and facilitates RNAi responses ...
Sateesh Krishnamurthy, Mark A Behlke, Michael A Apicella, Paul B McCray, Jr, Beverly L Davidson   +4 more
doaj   +1 more source

Effects of 5-HT2 receptor ligands on tail pinch-induced stress responding and open field behavior [PDF]

, 2005
Stress is known to exert an influence on neuroendocrine, autonomic, hormonal, and immune functioning. As a result of the debilitating effects of stress on numerous bodily systems, there exists a large body of research devoted to the etiology ...
Hearn, John K.
core   +2 more sources

Identification, functional characterization and pharmacological profile of a serotonin type-2b receptor in the medically important insect, Rhodnius prolixus

Frontiers in Neuroscience, 2015
In the Chagas disease vector, Rhodnius prolixus, two diuretic hormones act synergistically to dramatically increase fluid secretion by the Malpighian tubules (MTs) during the rapid diuresis that is initiated upon engorgement of vertebrate blood.
Jean-Paul V Paluzzi, Garima eBhatt, Garima eBhatt, Garima eBhatt, Chang-Hui Jenny Wang, Meet eZandawala, Meet eZandawala, Angela eLange, Angela eLange, Ian eOrchard, Ian eOrchard   +10 more
doaj   +1 more source

Inhibition of Cutaneous Contact Hypersensitivity in the Mouse with Systemic or Topical Spiperone: Topical Application of Spiperone Produces Local Immunosuppression Without Inducing Systemic Neuroleptic Effects

Journal of Investigative Dermatology, 1992
We tested the ability of the neuroleptic agent spiperone (8-[3-(p-fluorobenzoyl)propyl]-1-phenyl-1,3,8-triazaspiro-[4.5] decan-4- one) to influence the tissue swelling and leukocyte infiltration associated with T-cell--dependent immune responses, i.e., contact hypersensitivity reactions, in mice.
Akila Chandrasekar, Richard J. Sharpe, Zheng-Sheng. Wang, Stephen J. Galli, Kenneth A. Arndt   +4 more
openaire   +3 more sources

Aromatic linker variations in novel dopamine D2 and D3 receptor ligands

Archiv der Pharmazie, Volume 357, Issue 8, August 2024.
Within the blueprint motifs of dopamine D2R/D3R ligands, the butyl (tetramethylene) linker was replaced by substituted benzyl or phenethyl linkers, maintaining high affinities at both receptor subtypes. Abstract Dopamine D2‐like receptors, especially D2 and D3 receptor subtypes, are important targets of antipsychotic agents.
Cristian Di Biase, Luisa Leitzbach, Annika Frank, Aleksandra Zivkovic, Holger Stark   +4 more
wiley   +1 more source

Design, synthesis, and biological evaluation of bivalent ligands targeting dopamine D2-like receptors and the μ-opioid receptor [PDF]

, 2018
Currently, there is mounting evidence that intermolecular receptor-receptor interactions may result in altered receptor recognition, pharmacology and signaling.
Huysentruyt, Jelle, Qian, Mingcheng, Risseeuw, Martijn, Stove, Christophe, Van Calenbergh, Serge, Van Craenenbroeck, Kathleen, Vanderheyden, Patrick ML, Vasudevan, Lakshmi   +7 more
core   +2 more sources

Discovery of a Small Molecule Activator of Slack (Kcnt1) Potassium Channels That Significantly Reduces Scratching in Mouse Models of Histamine‐Independent and Chronic Itch

Advanced Science, Volume 11, Issue 15, April 17, 2024.
The potassium channel Slack is highly expressed in sensory neurons that sense itch. In this study, several new compounds that activate Slack are developed. It is found that the lead molecule, compound 6, effectively inhibits scratching elicited by multiple pruritogens in mice establishing Slack activation as a novel pharmacological strategy for the ...
Annika Balzulat, W. Felix Zhu, Cathrin Flauaus, Victor Hernandez‐Olmos, Jan Heering, Sunesh Sethumadhavan, Mariam Dubiel, Annika Frank, Amelie Menge, Maureen Hebchen, Katharina Metzner, Ruirui Lu, Robert Lukowski, Peter Ruth, Stefan Knapp, Susanne Müller, Dieter Steinhilber, Inga Hänelt, Holger Stark, Ewgenij Proschak, Achim Schmidtko   +20 more
wiley   +1 more source