AMPA Receptor Modulator

CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).

Aniracetam (Ro 13-5057) is an orally active neuroprotective agent, possessing nootropics effects. Aniracetam potentiates the ionotropic quisqualate (iQA) responses in the CA1 region of rat hippocampal slices. Aniracetam also potentiates the excitatory post synaptic potentials (EPSPs) in Schaffer collateral-commissural synapses. Aniracetam can prevents the CO₂-induced impairment of acquisition in hypercapnia model rats. Aniracetam can be used to research cerebral dysfunctional disorders.

IDRA 21 is a positive and orally active modulator of the AMPA receptor. IDRA 21 facilitates excitatory neurotransmission via GluR1/2 receptors. IDRA 21 has the potential for the research of cognitive/memory disorders, including those associated with aging.

AMPA-IN-3 is an AMPA receptor inhibitor. AMPA-IN-3 inhibits TARP J2-dependent AMPA receptor activity with a pIC₅₀ value of 10.7. A AMPA-IN-3 can be used for the research of neurological disease.

JNJ-61432059 is a blood-brain barrier-permeable, orally active TARP γ-8-associated AMPAR modulator with anticonvulsant activity. JNJ-61432059 negatively regulates GluA1 and positively modulates GluA2-containing AMPARs. JNJ-61432059 exerts potent protective effects in rodent epilepsy models. JNJ-61432059 is applicable for epilepsy-related research.

Org-26576 is a AMPA receptor positive allosteric modulator.

AMPA receptor modulator-10 (Compound 9a) is an orally active AMPA receptor (AMPAR) positive allosteric modulator. AMPA receptor modulator-10 exhibits potent activity (pEC₅₀ = 5.0) on the GluA2 subtype of AMPAR, significantly enhancing glutamate-induced calcium influx and current responses. AMPA receptor modulator-10 can reverse the memory impairment induced by Scopolamine (HY-N0296) and enhance cognitive function. AMPA receptor modulator-10 can be used for the research of neurological disease, such as schizophrenia.

AMPA receptor modulator-2 (Example 134) is a AMPA receptor modulator, with a pIC₅₀ of 10.1 for TARPγ8 dependent AMPA receptor. pIC₅₀ = -lgIC₅₀.

AMPA receptor modulator-3 is an allosteric AMPA receptor modulator (EC₅₀: 4.4 μM). AMPA receptor modulator-3 can be used in the research of mammalian nervous system, such as learning and memory.

1-BCP (Piperonylic acid piperidide) is a centrally active agent that modulates AMPA receptor gated currents. 1-BCP is a memory-enhancing agent.

AMPA receptor modulator-11 (example 210) is a positive allosteric AMPA receptor modulator. AMPA receptor modulator-11 can be used for research on depression, schizophrenia, Alzheimer's disease or attention deficit hyperactivity disorder (ADHD).

JNJ-56022486 is an orally active and potent negative AMPA receptor modulator (K_i=19 nM) selective for?TARP-γ8. JNJ-56022486 is also a TARP-γ8 receptor antagonist, with blood?brain?barrier (BBB) permeability. JNJ-56022486 can be used for research of Epilepsy.

CX516-d₁₀ is the deuterium labeled CX516. CX516 (BDP 12) is an ampakine and acts as an AMPA receptor positive allosteric modulator for the research of Alzheimer's disease, schizophrenia and mild cognitive impairment (MCI).

AMPA receptor modulator-12 is an orally acrive AMPA receptor positive allosteric modulator. AMPA receptor modulator-12 also exhibits moderate binding affinity for the human dopamine transporter with a K_d of 1.57 μM. AMPA receptor modulator-12 enhances AMPA receptor-mediated ion currents, delays channel deactivation. AMPA receptor modulator-12 prolongs sleep latency, reduces sleep duration, extends forced swimming time, improves rotarod endurance, and alleviates acute sleep deprivation-related behavioral deficits. AMPA receptor modulator-12 does not increase spontaneous locomotion. AMPA receptor modulator-12 can be used for the research of narcolepsy and fatigue-related conditions.

BPAM363 is an orally active, selective positive allosteric modulator (PAM) of AMPARs with blood-brain barrier penetration. BPAM363 selectively potentiates AMPAR activity in human and rat models, with an EC_2x value of 0.96 μM in rat embryonic cortex primary neurons. BPAM363 upregulates BDNF protein expression in rat primary cortical neuronal cultures. BPAM363 enhances AMPA-mediated excitatory postsynaptic responses in rat and mice. BPAM363 can be used for the study of cognitive disorders.

AMPAR modulator-12 is a blood-brain barrier-permeable AMPAR positive allosteric modulator. AMPAR modulator-12 reduces NOX-1 expression, enhances AMPAR-mediated currents, promotes excitatory postsynaptic transmission and restores AMPAR function. AMPAR modulator-12 enhances excitatory and inhibitory synaptic transmission, reduces burst firing in the lateral habenula after withdrawal, and produces rapid and sustained antidepressant-like effects. AMPAR modulator-12 is applicable for the research of depression.

CX1763 is an AMPAR allosteric modulator. CX1763 allosterically potentiates glutamate-evoked currents, accelerates channel opening, and increases the surface levels of AMPAR containing Glur2 (R). CX1763 enhances synaptic transmission in the rat hippocampus. CX1763 improves attention in rats and attenuates amphetamine-induced hyperactivity in mice. CX1763 can be used in studies related to attention deficit hyperactivity disorder and opioid-induced respiratory depression.

Normethyl-ZCAN262 (Normethyl-262) is a blood-brain barrier-permeable selective GluR2/AMPAR receptor modulator. Normethyl-ZCAN262 inhibits AMPA-mediated neurotoxicity, the formation of the GAPDH-GluR2 complex, and GluR2/AMPAR neurotoxicity. Normethyl-ZCAN262 enables in vivo imaging of brain AMPA receptors and is used in research related to multiple sclerosis, amyotrophic lateral sclerosis, neuroinflammation, stroke, epilepsy, Parkinson's disease, Alzheimer's disease, dementia, and Huntington's disease.