Results 21 to 30 of about 423,412 (333)

Discovery of 4-(5-Membered)Heteroarylether-6-methylpicolinamide Negative Allosteric Modulators of Metabotropic Glutamate Receptor Subtype 5

ACS Medicinal Chemistry Letters
[Image: see text] This Letter details our efforts to develop novel, non-acetylene-containing metabotropic glutamate receptor subtype 5 (mGlu(5)) negative allosteric modulators (NAMs) with improved pharmacological properties. This endeavor involved replacing the ether-linked pyrimidine moiety, a metabolic liability, with various 5-membered heterocycles.
Elizabeth S. Childress, Rory A. Capstick, Katherine E. Crocker, Miranda L. Ledyard, Aaron M. Bender, Mallory A. Maurer, Natasha B. Billard, Hyekyung P. Cho, Alice L. Rodriguez, Colleen M. Niswender, Weimin Peng, Jerri M. Rook, Sichen Chang, Anna L. Blobaum, Olivier Boutaud, Analisa Thompson Gray, Carrie K. Jones, P. Jeffrey Conn, Andrew S. Felts, Craig W. Lindsley, Kayla J. Temple   +20 more
openalex   +2 more sources

Molecular docking studies of N-substituted 4-methoxy-6-oxo-1-aryl-pyridazine-3-carboxamide derivatives as potential modulators of glutamate receptors [PDF]

Research Results in Pharmacology, 2020
Introduction: The virtual target-oriented screening is a necessary stage of modern drug-design. In the present study, the affinity of pyridazine derivatives for the most promising antiparkinsonian biotargets – I–III groups of metabotropic and ionotropic ...
Hanna I. Severina, Victoriya A. Georgiyants, Sergiy M. Kovalenko, Natalia V. Avdeeva, Artem I. Yarcev, Svetlana N. Prohoda   +5 more
doaj   +3 more sources

Astrocyte activation in the anterior cingulate cortex and altered glutamatergic gene expression during paclitaxel-induced neuropathic pain in mice [PDF]

PeerJ, 2015
Spinal astrocyte activation contributes to the pathogenesis of paclitaxel-induced neuropathic pain (PINP) in animal models. We examined glial fibrillary acidic protein (GFAP; an astrocyte marker) immunoreactivity and gene expression of GFAP, glutamate ...
Willias Masocha
doaj   +2 more sources

Profiling prefrontal cortex protein expression in rats exhibiting an incubation of cocaine craving following short-access self-administration procedures

Frontiers in Psychiatry, 2023
IntroductionIncubation of drug-craving refers to a time-dependent increase in drug cue-elicited craving that occurs during protracted withdrawal.
Laura L. Huerta Sanchez, Mathangi Sankaran, Taylor L. Li, Hoa Doan, Alvin Chiu, Eleanora Shulman, Gabriella Shab, Tod E. Kippin, Tod E. Kippin, Tod E. Kippin, Karen K. Szumlinski, Karen K. Szumlinski, Karen K. Szumlinski   +12 more
doaj   +1 more source

Orofacial antinociceptive activity and anchorage molecular mechanism in silico of geraniol [PDF]

Brazilian Oral Research, 2020
We aimed to evaluate the orofacial antinociceptive effect of geraniol in mice and its molecular anchorage mechanism. Seven mice per group (probabilistic sample) were treated with geraniol (12.5, 25 and 50 mg/kg, i.p.), morphine (6 mg/kg, i.p.) and ...
Tereza Karla Vieira Lopes da COSTA, Mariana Silva BARROS, Renan Marrinho BRAGA, Jéssika de Oliveira VIANA, Frederico Barbosa de SOUSA, Luciana SCOTTI, Marcus Tullius SCOTTI, André Ulisses Dantas BATISTA, Reinaldo Nóbrega de ALMEIDA, Ricardo Dias de CASTRO   +9 more
doaj   +1 more source

Can Metabotropic Glutamate Receptor 7 (mGluR 7) be a Novel Target for Analgesia? [PDF]

Journal of Clinical and Diagnostic Research, 2014
Introduction: The present study was carried out to study the role of metabotropic glutamate receptor 7 (mGluR7) using its agonist, N,N’-bis(diphenylmethyl)-1,-ethanediamine (AMN082) for nociceptive stimuli, in animal models.
Shivaprakash G, Punya Suvarna, Sanjay Hadigal, Priyanka Kamath, Natesh Prabhu, Ashok Shenoy K, Pallavi LC   +6 more
doaj   +1 more source

Acute Alcohol-Induced Changes Measured With Metabotropic Glutamate Receptor 5 Positron Emission Tomography. [PDF]

Addict Biol
This proof‐of‐concept study provides evidence that acute alcohol administration reduces mGluR5 availability and increases relative blood flow in the human brain, as measured by [11C]ABP688 PET. The observed effects align with preclinical evidence of alcohol‐induced glutamate release.
Raval NR, Smart K, Angarita GA, Miller R, Huang Y, Krystal JH, Carson RE, Cosgrove KP, O'Malley SS, Hillmer AT.   +9 more
europepmc   +2 more sources

Accuracy in readout of glutamate concentrations by neuronal cells [PDF]

The European Physical Journal E, 46(4), 30 (2023), 2023
Glutamate and glycine are important neurotransmitters in the brain. An action potential prop- agating in the terminal of a presynatic neuron causes the release of glutamate and glycine in the synapse by vesicles fusing with the cell membrane, which then activate various receptors on the cell membrane of the post synaptic neuron.
arxiv   +1 more source

Functional Availability of ON-Bipolar Cells in the Degenerated Retina: Timing and Longevity of an Optogenetic Gene Therapy

International Journal of Molecular Sciences, 2021
Degenerative diseases of the retina are responsible for the death of photoreceptors and subsequent loss of vision in patients. Nevertheless, the inner retinal layers remain intact over an extended period of time, enabling the restoration of light ...
Jakub Kralik, S. Kleinlogel
semanticscholar   +1 more source

MicroRNA binding site variation is enriched in psychiatric disorders

Human Mutation, Volume 43, Issue 12, Page 2153-2169, December 2022., 2022
Abstract Psychiatric disorders have a polygenic architecture, often associated with dozens or hundreds of independent genomic loci. Most associated loci impact noncoding regions of the genome, suggesting that the majority of disease heritability originates from the disruption of regulatory sequences.
Michael P. Geaghan, William R. Reay, Murray J. Cairns   +2 more
wiley   +1 more source