- Inhibitory Selectivity
|Catalog No.||Product Name||Solubility(25°C)|
|S2857||(-)-MK 801 maleate||<1 mg/mL||67 mg/mL||7 mg/mL|
|S2876||(+)-MK 801 maleate||<1 mg/mL||68 mg/mL||<1 mg/mL|
|S4091||Ifenprodil Tartrate||9 mg/mL||95 mg/mL||62 mg/mL|
|S7072||NMDA (N-Methyl-D-aspartic acid)||30 mg/mL||5 mg/mL||<1 mg/mL|
|S3624||Quinolinic acid||3 mg/mL||25 mg/mL||<1 mg/mL|
|S4023||Procaine HCl||55 mg/mL||55 mg/mL||<1 mg/mL|
|S1330||Felbamate||<1 mg/mL||48 mg/mL||3 mg/mL|
|S4702||Sarcosine||17 mg/mL||<1 mg/mL||<1 mg/mL|
|S4719||Kynurenic acid||<1 mg/mL||10 mg/mL||<1 mg/mL|
- NMDAR Inhibitors (9)
- New NMDAR Products
|Catalog No.||Information||Product Use Citations||Product Validations|
(-)-MK-801 (Dizocilpine) is a potent N-methyl-D-aspartate (NMDA) receptor antagonist with Ki of 30.5 nM.
The NMDA receptor is involved in the neuroprotective effect of Res. MK 801 (2 mg/kg) was injected respectively at 30 min prior to cerebral ischemia or at 30 min prior to the administration of Res at 1 or 24 h pre-MCAO. (A) The effects of MK801 on ischemia-induced neuronal death when Res was administrated at 1 h pre-MCAO. (B) The effects of MK801 on ischemia-induced neuronal death when Res was administrated at 24 h pre-MCAO. n = 5 rats at each group.
(+)-MK-801 is a potent, selective and non-competitive NMDA receptor antagonist with Kd of 37.2 nM in rat brain membranes.
Ifenprodil is an atypical noncompetitive antagonist at the NMDA receptor, it interacts with high affinity at a homogeneous population of NMDA receptors in neonatal rat forebrain with IC50 of 0.3 μM.
(B) Vehicle-treated rats, BDNF-treated rats, rats pre-treated with CTX-B and rats pre-treated with Ifenprodil showed equivalenttime in the pairing chambers prior to the conditioning day. There were no differences in these groups;thus,the preconditioning values were pooled for graphical representation. Only BDNF-treated rats showed a clear preference for the chamber paired with spinal clonidine (10 g). *P < 0.05, compared with pre-conditioning, two-way ANOVA, F(1,1,1/20) = (23.25, 16.89, 10.97), n = 6/group. (C) Difference score, indicates that application of BDNF in intact rats increased the time spent in the clonidine-paired chamber, while pre-injection of CTX-B or Ifenprodil into the rACC attenuated the difference score. #P < 0.05, one-way ANOVA, F(3,20) = 15.38, n = 6/group. Data are expressed as the mean ± SEM.
NMDA（N-Methyl-D-aspartic acid）is a specific agonist for NMDA receptor mimicking the action of glutamate, the neurotransmitter which normally acts at that receptor. Phase 4.
Quinolinic Acid, a neuroactive metabolite of the kynurenine pathway, is an agonist of N-methyl-D-aspartate (NMDA) receptor.
Procaine is an inhibitor of sodium channel, NMDA receptor and nAChR with IC50 of 60 μM, 0.296 mM and 45.5 μM, which is also an inhibitor of 5-HT3 with KD of 1.7 μM.
Procaine pretreatment inhibits JAK2 and STAT3 expression. (A) Relative Jak2 mRNA level detected by qRT-PCR. (B) Relative Stat3 mRNA level detected by qRT-PCR. (C) JAK2 and STAT3 protein expression detected by western blot. (D) Relative protein levels of JAK2 and STAT3 based on Western blot results. sham, rats undergone sham surgery. CCI, rats undergone sciatic nerve chronic compression injury (CCI) as the neuropathic pain (NPP) model. CCI+procaine, NPP model rats pretreated with procaine. The detection is performed on the 20th day post surgery (n=3). GAPDH is used as an internal reference. *p<0.05, **p<0.01. JAK2, Janus kinase 2. STAT3, signal transducer and activator of transcription 3.
Felbamate (Felbatol) is an anticonvulsant drug used in the treatment of epilepsy; NMDAR antagonist.
Sarcosine is a competitive inhibitor of the type I glycine transporter (GlyT1) and an N-methyl-D-aspartate receptor (NMDAR) co-agonist.
Kynurenic acid, a natural metabolite of tryptophan via the kynurenine pathway, is a broad-spectrum excitatory amino acid antagonist; It proved to be an antagonist at NMDA, kainate and AMPA receptors.