Results 81 to 90 of about 13,221 (154)

An aptamer agonist of the insulin receptor acts as a positive or negative allosteric modulator, depending on its concentration. [PDF]

Exp Mol Med, 2022
Yunn NO, Lee J, Lee HS, Oh EJ, Park M, Park S, Jin SY, Shin E, Lee JWY, Kim Y, Bae SS, Ryu SH.   +11 more
europepmc   +1 more source

Effects of GABAAR modulators CL218872 and MRK-016 on neural repair and synaptic plasticity in mice with Intracerebral hemorrhage.

PLoS ONE
BackgroundIntracerebral hemorrhage (ICH) is a devastating condition characterized by rapid onset, high rates of disability and mortality, and prolonged recovery.
Tingting Chen, Hongxia He, Fei Huang, Junwu Liu, Hongli Zhou, Lei Xu   +5 more
doaj   +1 more source

Influence of the TARP γ8-Selective Negative Allosteric Modulator JNJ-55511118 on AMPA Receptor Gating and Channel Conductance. [PDF]

Mol Pharmacol, 2022
Coombs ID, Sexton CA, Cull-Candy SG, Farrant M.   +3 more
europepmc   +1 more source

Membrane Lipids Are an Integral Part of Transmembrane Allosteric Sites in GPCRs: A Case Study of Cannabinoid CB1 Receptor Bound to a Negative Allosteric Modulator, ORG27569, and Analogs. [PDF]

J Med Chem, 2022
Obi P, Natesan S.
europepmc   +1 more source

Novel GluN2B-Selective NMDA Receptor Negative Allosteric Modulator Possesses Intrinsic Analgesic Properties and Enhances Analgesia of Morphine in a Rodent Tail Flick Pain Model. [PDF]

ACS Chem Neurosci, 2023
Harris LD, Regan MC, Myers SJ, Nocilla KA, Akins NS, Tahirovic YA, Wilson LJ, Dingledine R, Furukawa H, Traynelis SF, Liotta DC.   +10 more
europepmc   +1 more source

Sustained treatment with an α5 GABA A receptor negative allosteric modulator delays excitatory circuit development while maintaining GABAergic neurotransmission. [PDF]

Neuropharmacology, 2021
Nuwer JL, Brady ML, Povysheva NV, Coyne A, Jacob TC.   +4 more
europepmc   +1 more source

The Negative Allosteric Modulator EU1794-4 Reduces Single-Channel Conductance and Ca²⁺ Permeability of GluN1/GluN2A N-Methyl-d-Aspartate Receptors. [PDF]

Mol Pharmacol, 2021
Perszyk RE, Zheng Z, Banke TG, Zhang J, Xie L, McDaniel MJ, Katzman BM, Pelly SC, Yuan H, Liotta DC, Traynelis SF.   +10 more
europepmc   +1 more source

RO4938581, a GABA_A-α5 negative allosteric modulator rescued behavioral and EEG phenotypes of a mouse model of Dup15q syndrome. [PDF]

Mol Psychiatry
Nakagawa R, Nani F, Hipp JF, Honer M, Knoflach F, Gasser R, Ozmen L, Tamada K, Fjeldskaar F, Takacs L, Vautheny A, Morairty SR, Saxe M, Takumi T, Hernandez MC.   +14 more
europepmc   +1 more source

Blocking glutamate mGlu₅ receptors with the negative allosteric modulator CTEP improves disease course in SOD1^G93A mouse model of amyotrophic lateral sclerosis. [PDF]

Br J Pharmacol, 2021
Milanese M, Bonifacino T, Torazza C, Provenzano F, Kumar M, Ravera S, Zerbo AR, Frumento G, Balbi M, Nguyen TPN, Bertola N, Ferrando S, Viale M, Profumo A, Bonanno G.   +14 more
europepmc   +1 more source

The Pathway to Proof-of-Concept for BNC210, a Negative Allosteric Modulator of the Alpha-7 Nicotinic Acetylcholine Receptor (nAChR), for Treatment of Psychiatric Disease. [PDF]

Clin Pharmacol Drug Dev
Rolan P, Doolin E, Paul D, Crossman J, Odontiadis M, Danjou P, Smith M, Papapetropoulos S.   +7 more
europepmc   +1 more source