AMPA receptor

NBQX disodium is a potent and selective competitive antagonist of the AMPA receptor. It exhibits neuroprotective properties and demonstrates anticonvulsant activity, making it valuable for research into neurological disorders and seizure models. This compound is instrumental in studies aimed at understanding glutamate receptor-mediated signaling pathways and their implications in neurodegenerative diseases.

IDRA 21 is a positive allosteric modulator of the AMPA receptor, specifically enhancing signaling through GluR1/2 subtypes. This compound promotes excitatory neurotransmission, making it a valuable tool in the investigation of cognitive and memory disorders, including age-related decline. Its properties establish IDRA 21 as a promising candidate for research focusing on synaptic plasticity and cognitive enhancement.

Pesampator (PF-04958242) is a selective positive allosteric modulator of the AMPA receptor, enhancing glutamatergic neurotransmission. With an EC50 of 310 nM and a Ki of 170 nM, it potentiates AMPA receptor activity, making it a valuable tool for research in neuropharmacology and cognitive enhancement studies. It can be utilized to investigate the mechanisms underlying synaptic plasticity and the potential therapeutic effects on neurological disorders.

CX 717 is a positive allosteric modulator of the AMPA receptor, enhancing synaptic transmission and activity. It exhibits antidepressant-like effects, making it a valuable tool in the investigation of mood disorders. Additionally, CX 717 is relevant for research into adult attention deficit hyperactivity disorder (ADHD), providing insights into neurotransmission and behavioral modulation.

CX614 is a positive allosteric modulator of AMPA receptors that enhances excitatory postsynaptic potentials by inhibiting and prolonging the inactivation of glutamate responses. This compound can evoke excitatory postsynaptic currents in neuronal cultures, making it particularly useful in the investigation of neurophysiological processes. CX614 has potential applications in the study of psychiatric disorders, including depression.

JNJ-55511118 is a selective modulator of AMPA receptors, specifically targeting TARP γ-8, with an inhibition constant (Ki) of 26 nM. This compound demonstrates significant biological activity by reducing voluntary intake of sweetened alcohol in male murine models. In addition, it disrupts hippocampal neurotransmission, alters specific electroencephalogram frequency bands, induces transient hyperlocomotion, and impairs cognitive functions such as learning and memory, while also exhibiting anticonvulsant properties. JNJ-55511118 is valuable for research focused on alcohol use disorders and seizure mechanisms.

HBT1 is a selective AMPA receptor (AMPAR) potentiator that enhances receptor activity in the presence of AMPA by binding to its ligand-binding domain. Unlike traditional AMPA-R potentiators, HBT1 exhibits a limited agonistic effect, minimizing the risk of bell-shaped dose-response curves related to brain-derived neurotrophic factor (BDNF) production. This unique profile allows for broader research applications in neurological and psychiatric disorders, including depression and Alzheimer’s disease.

TAT-GluA2 3Y is an AMPAR inhibitor that interferes with the endocytosis of AMPA receptors, thereby blocking long-term depression (LTD) at glutamatergic synapses. This peptide has been shown to mitigate pentobarbital-induced spatial memory deficits, highlighting its potential in studying synaptic plasticity and memory-related research applications. TAT-GluA2 3Y serves as a valuable tool for exploring the mechanisms underlying synaptic transmission and cognitive function.

CX1739 is an AMPA-glutamate receptor (AMPAR) enhancer that significantly enhances long-term potentiation in a dose-dependent manner in mouse models. This compound effectively mitigates amphetamine-induced locomotor activity and rapidly reverses opioid-induced respiratory depression. Research applications for CX1739 include studies related to dementia, neuropsychiatric disorders, and complications arising from opiate-induced suppression of endogenous inspiratory breathing rhythms.