|Description||(-)-MK-801 maleate is a potent, selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM that acts at the NMDA receptor-operated ion channel as an open channel blocker. It blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. It anti-convulsant and likely has dissociative anesthetic properties, but it is not used clinically for this purpose due to the discovery of brain lesions, called Olney's lesions in test rats. It were used to treat hyperalgesia in the diabetic neuropathic pain (DNP). It is used in various ischemia treatments. It has been shown to be protective in various models of ischemia as well as to inhibit behavioral sensitization to certain psychostimulants.|
|Synonyms||(+)-10,11-Dihydro-5-methyl-5H-dibenzo[a,d]cyclohepten-5,10-diyldiammonium maleate;Dizocilpine maleate;(5R,10S)-(+)-5-Methyl-10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5,10-imine hydrogen maleate;Dizocilpine maleate;Dizocilpine hydrogen maleate;(+)-MK-801 hydrogen maleate|
|Solubility||DMSO: ＞ 20 mg/mL, H2O: 6 mg/mL|
|Application||(-)-MK-801 maleate blocks NMDA receptors in a use- and voltage-dependent manner, since the channel must open for the drug to bind inside it. It were used to treat hyperalgesia in the diabetic neuropathic pain (DNP). It is used in various ischemia treatments. It has been shown to be protective in various models of ischemia as well as to inhibit behavioral sensitization to certain psychostimulants.|
|Quality Standard||In-house standard|
|Shelf Life||2 month in rt, long time|
|Quantity||Grams to Kilograms|
|Boiling Point||541°C at 760 mmHg|
Apimostinel is a selective partial agonist of an allosteric site of the glycine site of the NMDA receptor complex under investigation by Naurex. Its mechanism o...
Eliprodil, a NR2B-NMDA receptor antagonist, was found to have neuroprotective activity in study of ischemia.
Cgp 39551 is a selective and competitive N-methyl-D-aspartate (NMDA) receptor antagonist originated by Novartis. Ki is 310 nM for inhibition of [3H]-CPP binding...
The hydrate of Felbamate which is an effective anticonvulsant agent. It was found to be clinically active for probably restraining the effectivity of NMDA.
CP-283097 is NR2B N-Methyl-D-Aspartate receptor antagonist originated by Pfizer. Preclinical trials for the treatment of Migraine and Neurodegenerative disorder...
Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neona...
PEAQX(NVP-AAM 077) is a potent and orally active NMDA antagonist with a 15-fold preference for human NMDA receptors with the 1A/2A(IC50=270 nM), rather than 1A/...
LY 235959 is a competitive N-Methyl-D-Aspartate Receptor antagonist originated by Eli Lilly. No development was reported for treatment of Movement disorders in ...
TCN 237 dihydrochloride
TCN 237 dihydrochloride is a potent and NR2B-selective NMDA antagonist (Ki = 0.8 nM), blocks NR2B-mediated calcium influx in Ltk cells (Ki = 9.7 nM).
Besonprodil, a benzimidazolone bioisostere, is an NMDA antagonist that selective for the NR2B subunit.
Radiprodil is a orally active and selective NMDA NR2B antagonist with a potential therapeutic agent in treatment of neuropathic pain and possibly other chronic ...
Felbamate (Felbatol) is an anticonvulsant drug used in the treatment of epilepsy.
Memantine is the first in a novel class of Alzheimer's disease medications acting on the glutamatergic system by blocking NMDA receptors.It is also a CYP2B6 and...
Mephenesin is an NMDA receptor antagonist, is a centrally acting muscle relaxant.
LY 257883, also known as PPPA, is a competitive NMDA receptor antagonist which displays moderate selectivity for NR2A-containing receptors. Ki values are 0.13μM...
(-)-MK-801 maleate is a potent, selective and non-competitive N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM that acts at the NMDA receptor-...
Rapastinel, a brain penetrable tetrapeptide, could be a partial agonist of NMDA receptor. It was already finished the Phase II trial for acting as an antidepres...
AM-36 is a potent blocker of batrachotoxinin (BTX)-sensitive Na+ channel binding in rat brain homogenates with an IC50 of 0.28 microM. As a unique neuroprotecti...
Dioxadrol hydrochloride has been found to be an NMDA antagonist and is used as a dissociative anaesthetic drug. It produces similar effects to PCP in animals. I...