NMDA Receptor Inhibitor

YY-23 is a selective inhibitor of NMDAR (containing GluN2C or GluN2D). YY-23 inhibits GABAergic neurotransmission and enhances excitatory transmission by inhibiting NMDARs containing GluN2D on GABAergic interneurons in the prefrontal cortex. YY-23 has antidepressant activity and can be used for the research of neurological diseases.

Pregnanolone sulfate is an endogenous neurosteroid and NMDA receptor inhibitor. Pregnanolone sulfate exhibits stronger inhibition of tonically activated NMDA receptors (associated with excitotoxicity) than of phasically activated synaptic receptors. Pregnanolone sulfate enhances glutamate release. Pregnanolone sulfate can be used in research on excitotoxic neurodegenerative diseases.

NMDAR/HDAC-IN-1 (Compound 9d) is a dual NMDAR and HDAC inhibitor with a K_i of 0.59 μM for NMDAR and IC₅₀ values of 2.67, 8.00, 2.21, 0.18 and 0.62 μM for HDAC1, HDAC2, HDAC3, HDAC6 and HDAC8, respectively. NMDAR/HDAC-IN-1 efficiently penetrates the blood brain barrier.

5-Chloro-1,4-dihydro-2,3-quinoxalinedione (Compound 72) is a weak NMDA inhibitor with an IC₅₀ of 56.3 μM. 5-Chloro-1,4-dihydro-2,3-quinoxalinedione can be used for the research of neurological disease.

MN-05 is a dual neuroprotective and vasodilatory NMDA receptor inhibitor.MN-05 blocks calcium influx, reduces free radical production, and maintains mitochondrial membrane potential in cortical neurons exposed to glutamate.MN-05 dilates aortic rings against phenylephrine-induced contraction.MN-05 protects neurons against glutamate-induced injury in vitro.MN-05 can be used for the research of neurodegenerative diseases.

Indole-2-carboxylic acid-¹³C is the ¹³C-labeled Indole-2-carboxylic acid. Indole-2-carboxylic acid is a strong inhibitor of lipid peroxidation. Indole-2-carboxylic acid (I2CA) specifically and competitively inhibits the potentiation by glycine of NMDA-gated current.

Bupivacaine hydrochloride monohydrate is a NMDA receptor inhibitor. Bupivacaine hydrochloride monohydrate can block sodium, L-calcium, and potassium channels. Bupivacaine hydrochloride monohydrate potently blocks SCN5A channels with the IC₅₀ of 69.5 μM. Bupivacaine hydrochloride monohydrate can be used for the research of chronic pain.

Dynorphin A (1-10) an endogenous opioid neuropeptide, binds to extracellular loop 2 of the κ-opioid receptor. Dynorphin A (1-10) also blocks NMDA-activated current with an IC₅₀ of 42.0 μM.

WMS-1410 is a selective GluN2B-containing NMDA receptor inhibitor with an IC₅₀ of 18.4 nM. WMS-1410 regulates intracellular calcium levels and protects cells from Apoptosis. WMS-1410 inhibits glutamate-induced excitotoxicity. WMS-1410 reverses NMDA/glycine-induced reduction in glucose-stimulated insulin secretion without altering physiological insulin secretion or baseline redox status, but fails to counteract insulin content loss induced by glucolipotoxicity. WMS-1410 exhibits analgesic activity against advanced neuropathic pain. WMS-1410 can be used in studies related to stroke, brain injury, Alzheimer's disease, Parkinson's disease, type 2 diabetes, and neuropathic pain.