AMPA Receptor Activator

Osavampator (TAK-653) is a AMPA receptor positive allosteric modulator. Osavampator selectively binds to AMPA-R in a glutamate-dependent manner and induces Ca2+ influx in hGluA1i CHO cells (EC₅₀ = 3.3 μM). Osavampator improves learning and memory in many models. Osavampator is can be used for the research of depressive disorders.

PEPA is an AMPA receptor allosteric potentiator. PEPA shows preferential action of PEPA on the flop form of AMPA receptors. PEPA is a more potent suppressor of desensitization of receptors containing GluR3 and GluR4 as opposed to those containing GluR1. PEPA has antianxiety effects.

Mibampator (LY451395) is a potent and highly selective potentiator of the AMPA receptors.

LY450108 is a potent AMPA receptor potentiator. LY450108 has the potential for depression and Parkinson's disease research.

Unifiram (DM232) is a AMPA receptor activator and cognitive enhancer. Unifiram activates the AMPA-mediated neurotransmission system. Unifiram reverses NBQX-induced amnesia in the passive avoidance test in mice. Unifiram reverses the antagonistic effect of kynurenic acid on NMDA-mediated [³H]NA release in rat hippocampal slices. Unifiram enhances excitatory synaptic transmission in the rat hippocampus in vitro. Unifiram can be used in studies related to amnesia and cognitive dysfunction, including age-related memory decline, neurodegenerative diseases such as Alzheimer's disease or Parkinson's disease, multiple sclerosis, schizophrenia, and attention deficit hyperactivity disorder.

4,5,6,7-Tetrahydroindazole acts as an Antimicrobial agent, an interleukin-2-induced T-cell kinase inhibitor, a positive allosteric modulator of AMPA receptors, and a ligand for CYP2E1, with a K_d1 value of 0.023 μM for its binding to rabbit-derived CYP2E1. 4,5,6,7-Tetrahydroindazole scavenges DPPH free radicals. It exhibits anti-tumor, anti-tuberculosis, and anti-inflammatory activities.

NPEC- caged-(S)-AMPA, a caged neurotransmitter analog, is a NPEC photoprotecting group caged the (S)-AMPA (HY-100815A) to make caged ligands specific for glutamate receptor sub-types. NPEC- caged-(S)-AMPA selectively activates AMPA receptor.

UoS12258 is a selective positive allosteric modulator of AMPA receptor. UoS12258 enhances AMPA receptor‐mediated synaptic transmission. UoS12258 improves performance in cognition rat models, including Scopolamine (HY-N0296)‐impaired rats and water maze learning and retention in aged rats.