Results 31 to 40 of about 75,386 (292)

(+)-4-Phosphonophenylglycine (PPG) a new group III selective metabotropic glutamate receptor agonist

Bioorganic & Medicinal Chemistry Letters, 2000
A new synthesis of (R,S)-PPG (4-phosphonophenylglycine) and the separation of the protected enantiomers leading after deprotection to (+)- and (-)-PPG are described. Pharmacological characterization at the group III metabotropic glutamate receptors hmGluR4a and hmGluR7b revealed (+)-PPG as the active enantiomer.
F. Gasparini, Werner Inderbitzin, Eric Francotte, Gabrielle Lecis, Paul Richert, Zorica Dragic, Rainer Kühn, Peter J. Flor   +7 more
openalex   +3 more sources

Emotional Impairment and Persistent Upregulation of mGlu5 Receptor following Morphine Abstinence: Implications of an mGlu5-MOPr Interaction. [PDF]

, 2016
BACKGROUND: A difficult problem in treating opioid addicts is the maintenance of a drug-free state because of the negative emotional symptoms associated with withdrawal, which may trigger relapse.
Bailey, A, Chen, Y, Georgiou, P, Gonzalez, LR, Hourani, S, Kieffer, BL, Kitchen, I, Winsky-Sommerer, R, Zanos, P   +8 more
core   +1 more source

[³H]‐L‐2‐amino‐4‐phosphonobutyrate labels a metabotropic glutamate receptor, mGluR4a [PDF]

British Journal of Pharmacology, 1995
1. The ligand binding site of subtype mGluR4a of the metabotropic glutamate receptor family was characterized by using [3H]-L-2-amino-4-phosphonobutyrate ([3H]-L-AP4) binding. 2. Specific [3H]-L-AP4 binding to membranes prepared from baby hamster kidney (BHK) cells transfected with a vector encoding mGluR4a accounted for 60-70% of the total binding ...
Lisbeth Eriksen, C. Thomsen
openalex   +4 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

mGlu1 Receptors Monopolize the Synaptic Control of Cerebellar Purkinje Cells by Epigenetically Down-Regulating mGlu5 Receptors [PDF]

, 2018
In cerebellar Purkinje cells (PCs) type-1 metabotropic glutamate (mGlu1) receptors play a key role in motor learning and drive the refinement of synaptic innervation during postnatal development.
Atsu Aiba, Cristina Zappulla, Ferdinando Nicoletti, Francesca Liberatore, Giada Mascio, Giorgio Carmignoto, Giuseppe Battaglia, Harumi Nakao, Marta Motolese, Masahiko Watanabe, Micaela Zonta, Michele Madonna, Milena Cannella, Pamela Scarselli, Roberto Gradini, Serena Notartomaso, Valeria Bruno   +16 more
core   +2 more sources

Alleviating Pain Hypersensitivity through Activation of Type 4 Metabotropic Glutamate Receptor [PDF]

The Journal of Neuroscience, 2013
Hyperactivity of the glutamatergic system is involved in the development of central sensitization in the pain neuraxis, associated with allodynia and hyperalgesia observed in patients with chronic pain. Herein we study the ability of type 4 metabotropic glutamate receptors (mGlu4) to regulate spinal glutamate signaling and alleviate chronic pain.
Vilar, Bruno, Busserolles, Jérôme, Ling, Bing, Laffray, Sophie, Ulmann, Lauriane, Malhaire, Fanny, Chapuy, Eric, Aissouni, Youssef, Etienne, Monique, Bourinet, Emmanuel, Acher, Francine, Pin, Jean-Philippe, Eschalier, Alain, Goudet, Cyril   +13 more
openaire   +3 more sources

Participation of the Cholinergic System in Ameliorating Effect of Vasopressin Fragment by Group I Metabotropic Glutamate–Receptor Blockade

Journal of Pharmacological Sciences, 2008
The effect of [pGlu4,Cyt6,Arg8]-vasopressin fragment 4-9 (AVP4-9) on group I metabotropic glutamate (mGlu1) receptor antagonist–induced memory deficits was studied using 8-arm radial maze performance with 4 arms baited.
Tadatsugu Tarumi, Azusa Mikami, Kenichi Shimada, Chiaki Kamei   +3 more
doaj   +1 more source

Antiparkinsonian Effects of a Metabotropic Glutamate Receptor 4 Agonist in MPTP-Treated Marmosets [PDF]

Journal of Parkinson's Disease, 2020
Background: Increased firing across glutamatergic synapses may contribute to both the motor dysfunction and L-DOPA-induced dyskinesia seen in Parkinson’s disease. Given their ability to reduce glutamate release, activation of group III metabotropic glutamate receptors such as metabotropic glutamate receptor 4 may prove effective against both motor ...
Mann, Lizzie, Jackson, Michael, Lincoln, Louise, Fisher, Ria, Rose, Sarah, Duty, Susan   +5 more
openaire   +4 more sources

mGluR5 antagonism inhibits cocaine reinforcement and relapse by elevation of extracellular glutamate in the nucleus accumbens via a CB1 receptor mechanism. [PDF]

, 2018
Metabotropic glutamate receptor 5 (mGluR5) antagonism inhibits cocaine self-administration and reinstatement of drug-seeking behavior. However, the cellular and molecular mechanisms underlying this action are poorly understood.
Bi, Guo-Hua, Gardner, Eliot L, He, Yi, Jordan, Chloe J, Li, Jie, Li, Xia, Peng, Xiao-Qing, Xi, Zheng-Xiong, Yang, Hong-Ju, Zhang, Hai-Ying   +9 more
core   +2 more sources

Targeting mGlu5 metabotropic glutamate receptors in the treatment of cognitive dysfunction in a mouse model of phenylketonuria [PDF]

, 2018
We studied group-I metabotropic glutamate (mGlu) receptors in Pah(enu2) (ENU2) mice, which mimic the genetics and neurobiology of human phenylketonuria (PKU), a metabolic disorder characterized, if untreated, by autism, and intellectual disability (ID ...
Battaglia, Giuseppe, Colamartino, Marco, Di Menna, Luisa, Fiori, Elena, Iacovelli, Luisa, Leuzzi, Vincenzo, Nardecchia, Francesca, Nicoletti, Ferdinando, Nistico, Robert, Orlando, Rosamaria, Pascucci, Tiziana, Piccinin, Sonia, Puglisi-Allegra, Stefano   +12 more
core   +2 more sources