Search
Search Results
-
Increased rigidity and bioisosteric replacement in the design, synthesis and preliminary evaluation of novel, functionalized 3,3-dialkyl-γ-butyrolactones as sigma-2 ligands
The sigma-2 (σ 2 ) receptor has been linked to several diseases and conditions including cancer, neuropathic drug addiction, Alzheimer’s disease,...
-
Schwann Cell-Derived Exosomes Induced Axon Growth after Spinal Cord Injury by Decreasing PTP-σ Activation on CSPGs via the Rho/ROCK Pathway
Spinal cord injury (SCI) is a severe neurological condition that involves a lengthy pathological process. This process leads to the upregulation of...
-
Discovery of oxazolidinone-based heterocycles as subtype selective sigma-2 ligands
The sigma-2 (σ 2 ) receptor, also known as the Transmembrane Protein 97 (TMEM97, and MAC30 (Meningioma-associated protein), has been linked to a number...
-
The Sigma 2 receptor promotes and the Sigma 1 receptor inhibits mu-opioid receptor-mediated antinociception
The Sigma-1 receptor (σ1R) has emerged as an interesting pharmacological target because it inhibits analgesia mediated by mu-opioid receptors (MOR),...
-
Sigma-1 Receptor Activation Suppresses Microglia M1 Polarization via Regulating Endoplasmic Reticulum–Mitochondria Contact and Mitochondrial Functions in Stress-Induced Hypertension Rats
Exposure to stress plays a detrimental role in the pathogenesis of hypertension via neuroinflammation pathways. Microglial neuroinflammation in the...
-
Synthesis and evaluation of novel, selective, functionalized γ-butyrolactones as sigma-2 ligands
The sigma-2 (σ 2 ) receptor was discovered nearly 40 years ago and was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30...
-
Discovery of novel, selective, functionalized 5-(2-(5-arylhexahydropyrrolo[3,4-c]pyrrol-2(1H)-yl)ethyl)-γ-butyrolactone sigma-2 ligands
The sigma-2 (σ 2 ) receptor was recently identified as the Transmembrane Protein 97 (TMEM97, also known as MAC30 (Meningioma-associated protein)). This...
-
Design, synthesis, and evaluation of novel, selective γ-butyrolactones sigma-2 ligands
Nearly 40 years after the first disclosure of sigma receptors, the sigma-2 (σ2) receptor was recently identified as the Transmembrane Protein 97...
-
Generative Modelling of Cortical Receptor Distributions from Cytoarchitectonic Images in the Macaque Brain
Neurotransmitter receptor densities are relevant for understanding the molecular architecture of brain regions. Quantitative in vitro receptor...
-
Exploring Muscarinic Acetylcholine Receptor Binding Kinetics with Fluorescence Anisotropy
Many different assays are available for measuring ligand binding to muscarinic acetylcholine receptors. Each has advantages and throwbacks, making...
-
Sigma-1 receptor activity in primary sensory neurons is a critical driver of neuropathic pain
The Sigma-1 receptor (σ 1 R) is highly expressed in the primary sensory neurons (PSNs) that are the critical site of initiation and maintenance of pain...
-
Receptor-Functionalized Lipid Membranes as Biomimetic Surfaces for Adhesion of Plasmodium falciparum-Infected Erythrocytes
Here, we describe a detailed protocol of how to manufacture biomimetic, host receptor-functionalized membranes and how to use them in adhesion...
-
Next-generation neuropeptide Y receptor small-molecule agonists inhibit mosquito-biting behavior
BackgroundFemale Aedes aegypti mosquitoes can spread disease-causing pathogens when they bite humans to obtain blood nutrients required for egg...
-
Psychedelics promote plasticity by directly binding to BDNF receptor TrkB
Psychedelics produce fast and persistent antidepressant effects and induce neuroplasticity resembling the effects of clinically approved...
-
Towards a translational physiologically-based pharmacokinetic (PBPK) model for receptor-mediated transcytosis of anti-transferrin receptor monoclonal antibodies in the central nervous system
In this manuscript, we present a translational physiologically-based pharmacokinetic (PBPK) model to characterize receptor-mediated transcytosis...
-
Exploring 1-adamantanamine as an alternative amine moiety for metabolically labile azepane ring in newly synthesized benzo[d]thiazol-2(3H)one σ receptor ligands
In this work we report the structure–affinity relationships, binding properties, and metabolic stability studies of a series of benzo[ d ]thiazol-2(3 H )o...
-
Sigma-1 receptor ligand PD144418 and sigma-2 receptor ligand YUN-252 attenuate the stimulant effects of methamphetamine in mice
RationalePrevious research indicates that the selective sigma-1 receptor ligand PD144418 and the selective sigma-2 ligands YUN-252 can inhibit...
-
Correction to: Activation of Sigma-1 Receptor Enhanced Pericyte Survival Via the Interplay between Apoptosis and Autophagy: Implications for Blood–Brain Barrier Integrity in Stroke
In the original publication of this article, the representative western blot images of β-actin in Fig. 3e was presented repeatedly in Fig. 7b due to...
-
Chemical Probes for Histamine Receptor Subtypes
Ligands with different properties and different selectivity are highly needed for in vitro and in vivo studies on the (patho)physiological influence...
-
The sigma receptor ligand N-phenylpropyl-N′-(4-methoxyphenethyl)3piperazine (YZ-067) enhances the cocaine conditioned-rewarding properties while inhibiting the development of sensitization of cocaine in mice
RationaleThe N -phenylpropyl- N ′-substituted piperazines SA-4503 ( N -phenylpropyl- N ′-(3,4-dimethoxyphenethyl)piperazine) and YZ-185 ( N -phenylpropyl- N ′-(...
