Results 231 to 240 of about 48,073 (302)

Relevance of G protein‐coupled receptor (GPCR) dynamics for receptor activation, signalling bias and allosteric modulation

British Journal of Pharmacology, Volume 182, Issue 14, Page 3211-3224, July 2025.
Abstract G protein‐coupled receptors (GPCRs) are one of the major drug targets. In recent years, computational drug design for GPCRs has mainly focused on static structures obtained through X‐ray crystallography, cryogenic electron microscopy (cryo‐EM) or in silico modelling as a starting point for virtual screening campaigns. However, GPCRs are highly
Marta Lopez‐Balastegui, Tomasz Maciej Stepniewski, Małgorzata M. Kogut‐Günthel, Antonella Di Pizio, Mette Marie Rosenkilde, Jiafei Mao, Jana Selent   +6 more
wiley   +1 more source

Progress on the development of Class A GPCR‐biased ligands

British Journal of Pharmacology, Volume 182, Issue 14, Page 3249-3300, July 2025.
Class A G protein‐coupled receptors (GPCRs) continue to garner interest for their essential roles in cell signalling and their importance as drug targets. Although numerous drugs in the clinic target these receptors, over 60% GPCRs remain unexploited. Moreover, the adverse effects triggered by the available unbiased GPCR modulators, limit their use and
Paula Morales, Magdalena M. Scharf, Marcel Bermudez, Attila Egyed, Rafael Franco, Olivia K. Hansen, Nadine Jagerovic, Jan Jakubík, György M. Keserű, Dóra Judit Kiss, Pawel Kozielewicz, Olav Larsen, Maria Majellaro, Ana Mallo‐Abreu, Gemma Navarro, Rubén Prieto‐Díaz, Mette M. Rosenkilde, Eddy Sotelo, Holger Stark, Tobias Werner, Laura M. Wingler   +20 more
wiley   +1 more source

Propofol decreases stimulated dopamine release in the rat nucleus accumbens by a mechanism independent of dopamine D2, GABAA and NMDA receptors

, 2000
D Schulte, Luís F. Callado, Colin Davidson, Paul E. M. Phillips, Norbert Roewer, J. Schulte am Esch, Jon Stamford   +6 more
openalex   +1 more source

ESG‐1‐60 and ESG‐1‐61: Novel dopamine D3 receptor‐preferring partial agonists/antagonists that inhibit cocaine taking and seeking in rodents

British Journal of Pharmacology, Volume 182, Issue 13, Page 2997-3016, July 2025.
Abstract Background and Purpose Preclinical studies suggest that highly selective dopamine D3 receptor (D3R) antagonists or partial agonists hold promise for treating substance use disorders. However, their limited effectiveness in reducing cocaine self‐administration is a major drawback.
Omar Soler‐Cedeño, Bradley M. Keegan, Hannah Alton, Guo‐Hua Bi, Emily Linz, Caleb D. Vogt, Emma S. Gogarnoiu, Lei Shi, Amy Hauck Newman, Zheng‐Xiong Xi   +9 more
wiley   +1 more source

Differential Modulation of Dopamine D2 Receptor on Somatostatin and Parvalbumin Interneurons in the CA1 Area of the Dorsal Hippocampus

European Journal of Neuroscience, Volume 62, Issue 1, July 2025.
In this current study, we investigated the cellular mechanisms underlying dopaminergic modulation in the hippocampus by combining pharmacology and electrophysiology in organotypic hippocampal slices. We identified that dopamine D2 receptors are expressed in somatostatin and, to a lesser extent, parvalbumin interneurons.
Pola Tuduri, Audrey Mignon, Emmanuel Valjent, Jeanne Ster   +3 more
wiley   +1 more source

Hypersomatotropism and Hypercortisolism Caused by a Plurihormonal Pituitary Adenoma in a Dog

Journal of Veterinary Internal Medicine, Volume 39, Issue 4, July/August 2025.
ABSTRACT A 12‐year‐old, male Labrador Retriever was presented because of polyuria, polydipsia, polyphagia, joint pain, and physical features consistent with acromegaly. Circulating insulin‐like growth factor‐1 (IGF‐1) concentration was increased (> 1000 ng/mL; reference interval [RI], 42–449), suggestive of hypersomatotropism.
Elber A. Soler Arias, Ricardo Rodas Elvir, Adrian F. Daly, Hans S. Kooistra   +3 more
wiley   +1 more source

Advances in Mechanochemical Methods for One‐Pot Multistep Organic Synthesis

Chemistry – A European Journal, Volume 31, Issue 34, June 17, 2025.
This review highlights recent advances in mechanochemical methods for multistep organic synthesis, focusing on sequential one‐pot approaches performed by grinding or ball milling. The presented transformations are discussed in terms of efficiency, applicability, and sustainability, assessing both the challenges and potential of solvent‐free one‐pot ...
Nina Biedermann, Michael Schnürch
wiley   +1 more source

Ex vivo stimulation of the trigeminal nucleus caudalis induces peripheral CGRP release in the trigeminal ganglion and reveals a distinct dopamine-endocannabinoid mechanism relevant to migraine. [PDF]

J Headache Pain
Christiansen IM, Reducha PV, Edvinsson L, Holm A, Haanes KA.   +4 more
europepmc   +1 more source

Using cocaine and apomorphine self-administration in rats to measure the pharmacokinetics of competitive dopamine receptor antagonists administered by different routes. [PDF]

Sci Rep
Song HJ, Desai JN, Norman MK, Norman AB.
europepmc   +1 more source