NMDAR

抑制剂选择性比较

特异性亚型抑制剂

NMDA receptor Selective

NMDAR产品

所有产品 NMDAR抑制剂(1) NMDAR拮抗剂(13) NMDAR激动剂(4) NMDAR调节剂(3)

目录号	产品描述	文献引用	实验数据
S4023	Procaine HCl Procaine HCl是一种钠离子通道的，NMDA受体以及乙酰胆碱受体抑制剂， IC50分别为60 μM， 0.296 mM何45.5 μM，也是一种，5-HT3抑制剂，K_D为1.7 μM。	Biomol Ther (Seoul), 2016, 24(5):489-94 Biomol Ther (Seoul), 2016, 24(5):489-94	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.
S2857	(-)-MK 801 maleate MK-801 (Dizocilpine)是一种有效的N-methyl-D-aspartate(NMDA)受体拮抗剂，K_i为30.5 nM。	Clin Exp Pharmacol Physiol, 2020, 47(5):848-856 J Burn Care Res, 2017, 38(5):e842-e850 Pharmacol Biochem Behav, 2016, 146-147:21-27	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.
S2876	(+)-MK 801 maleate (+)-MK 801 Maleate作用于大鼠脑组织膜，是一种有效的，选择性的，非竞争性NMDA受体拮抗剂，K_d为37.2 nM。	Acta Biochim Biophys Sin (Shanghai), 2019, 51(11):1114-1122 J Burn Care Res, 2017, 38(5):e842-e850
S4091	Ifenprodil Tartrate Ifenprodil是一种非典型非竞争性的NMDA受体拮抗剂，在新生大鼠前脑中，高亲和力结合于NMDA受体，IC50为0.3 μM。	Brain Res Bull, 2016, 127:56-65	(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.
S6644^New	Radiprodil (RGH-896) Radiprodil (RGH-896)是对NR2B具有选择性的NMDAR拮抗剂，用于治疗神经性疼痛。
S6731^New	Eliprodil (SL-820715) Eliprodil (SL-820715)是一种非竞争性的、对NR2B具有选择性的NMDA拮抗剂，IC50为1 μM。它对含NR2A和NR2C的受体的IC50大于100 μM。
S2043	Memantine HCl Memantine HCl是NMDAR拮抗剂。它还是CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，K_i分别为0.51 nM和94.9 μM。
S1330	Felbamate Felbamate 是一种抗惊厥药，用于治疗癫痫。是NMDAR拮抗剂。
S4957	Linalool Linalool是一些芳香剂中的香精油的主要成分。它是NMDA receptors的竞争性拮抗剂。
S5287	Tiletamine Hydrochloride Tiletamine is a lipophilc and potent vetrinary anesthetic. It is also a NMDA receptor antagonist.
S3653	Spermidine trihydrochloride Spermidine是一种从腐胺和dcSAM中，通过亚精胺合成酶合成的天然聚胺。它是新型的自噬诱导剂，负向调控N-methyl-d-aspartate (NMDA)。
S5032	Mephenesin Mephenesin是一种作用于中枢的肌肉松弛剂、局部镇痛剂，也是NMDA receptor的拮抗剂。
S5664	Orphenadrine Hydrochloride Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity.
S4719	Kynurenic acid Kynurenic acid是色氨酸通过犬尿氨酸途径代谢的天然代谢物，是一种广谱的兴奋性氨基酸拮抗剂。它是NMDAR, kainate receptor和AMPA receptor的拮抗剂。	Gene, 2020, 737:144434
S7072	NMDA (N-Methyl-D-aspartic acid) NMDA (N-Methyl-D-aspartic acid)是一种特异性NMDA受体激动剂，通常作为受体，模拟神经递质谷氨酸的活性。Phase 4。	Mol Brain, 2018, 11(1):35
S3624	Quinolinic acid Quinolinic Acid是犬尿氨酸途径中的具有神经活性的代谢物，是N-methyl-D-aspartate (NMDA)受体的激动剂。
S6224	(R)-Serine (R)-Serine是丝氨酸的R-对映体。丝氨酸被用于蛋白质的生物合成。
S4702	Sarcosine Sarcosine是GlyT1的竞争性抑制剂以及天冬氨酸受体（NMDAR）的协同激动剂。
S5129	D-Aspartic acid D-Aspartic acid (D-Asp) is an endogenous amino acid occurring in several tissues and cells of both invertebrates and vertebrates. It can regulate testosterone synthesis and may act on a stimulatory receptor (NMDA).
S9271	Pulchinenoside A Pulchinenoside A, a natural triterpenoid saponin, is a AMPARs and NMDAR modulator.
S5302	6-Methoxy-2-naphthoic acid 6-Methoxy-2-naphthoic acid是NMDAR的调节剂。

目录号	产品描述	文献引用	实验数据
S4023	Procaine HCl Procaine HCl是一种钠离子通道的，NMDA受体以及乙酰胆碱受体抑制剂， IC50分别为60 μM， 0.296 mM何45.5 μM，也是一种，5-HT3抑制剂，K_D为1.7 μM。	Biomol Ther (Seoul),2016, 24(5):489-94 Biomol Ther (Seoul),2016, 24(5):489-94	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.

目录号

产品描述

文献引用

实验数据

S4023

目录号	产品描述	文献引用	实验数据
S2857	(-)-MK 801 maleate MK-801 (Dizocilpine)是一种有效的N-methyl-D-aspartate(NMDA)受体拮抗剂，K_i为30.5 nM。	Clin Exp Pharmacol Physiol, 2020, 47(5):848-856 J Burn Care Res, 2017, 38(5):e842-e850 Pharmacol Biochem Behav, 2016, 146-147:21-27	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.
S2876	(+)-MK 801 maleate (+)-MK 801 Maleate作用于大鼠脑组织膜，是一种有效的，选择性的，非竞争性NMDA受体拮抗剂，K_d为37.2 nM。	Acta Biochim Biophys Sin (Shanghai), 2019, 51(11):1114-1122 J Burn Care Res, 2017, 38(5):e842-e850
S4091	Ifenprodil Tartrate Ifenprodil是一种非典型非竞争性的NMDA受体拮抗剂，在新生大鼠前脑中，高亲和力结合于NMDA受体，IC50为0.3 μM。	Brain Res Bull, 2016, 127:56-65	(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.
S6644^New	Radiprodil (RGH-896) Radiprodil (RGH-896)是对NR2B具有选择性的NMDAR拮抗剂，用于治疗神经性疼痛。
S6731^New	Eliprodil (SL-820715) Eliprodil (SL-820715)是一种非竞争性的、对NR2B具有选择性的NMDA拮抗剂，IC50为1 μM。它对含NR2A和NR2C的受体的IC50大于100 μM。
S2043	Memantine HCl Memantine HCl是NMDAR拮抗剂。它还是CYP2B6和CYP2D6抑制剂，作用于重组CYP2B6和CYP2D6，K_i分别为0.51 nM和94.9 μM。
S1330	Felbamate Felbamate 是一种抗惊厥药，用于治疗癫痫。是NMDAR拮抗剂。
S4957	Linalool Linalool是一些芳香剂中的香精油的主要成分。它是NMDA receptors的竞争性拮抗剂。
S5287	Tiletamine Hydrochloride Tiletamine is a lipophilc and potent vetrinary anesthetic. It is also a NMDA receptor antagonist.
S3653	Spermidine trihydrochloride Spermidine是一种从腐胺和dcSAM中，通过亚精胺合成酶合成的天然聚胺。它是新型的自噬诱导剂，负向调控N-methyl-d-aspartate (NMDA)。
S5032	Mephenesin Mephenesin是一种作用于中枢的肌肉松弛剂、局部镇痛剂，也是NMDA receptor的拮抗剂。
S5664	Orphenadrine Hydrochloride Orphenadrine Hydrochloride is an uncompetitive NMDAR antagonist, H1 receptor antagonist and nonselective mAChR antagonist with muscle relaxant activity.
S4719	Kynurenic acid Kynurenic acid是色氨酸通过犬尿氨酸途径代谢的天然代谢物，是一种广谱的兴奋性氨基酸拮抗剂。它是NMDAR, kainate receptor和AMPA receptor的拮抗剂。	Gene, 2020, 737:144434

目录号	产品描述	文献引用
S7072	NMDA (N-Methyl-D-aspartic acid) NMDA (N-Methyl-D-aspartic acid)是一种特异性NMDA受体激动剂，通常作为受体，模拟神经递质谷氨酸的活性。Phase 4。	Mol Brain, 2018, 11(1):35
S3624	Quinolinic acid Quinolinic Acid是犬尿氨酸途径中的具有神经活性的代谢物，是N-methyl-D-aspartate (NMDA)受体的激动剂。
S6224	(R)-Serine (R)-Serine是丝氨酸的R-对映体。丝氨酸被用于蛋白质的生物合成。
S4702	Sarcosine Sarcosine是GlyT1的竞争性抑制剂以及天冬氨酸受体（NMDAR）的协同激动剂。

目录号	产品描述	文献引用	实验数据
S5129	D-Aspartic acid D-Aspartic acid (D-Asp) is an endogenous amino acid occurring in several tissues and cells of both invertebrates and vertebrates. It can regulate testosterone synthesis and may act on a stimulatory receptor (NMDA).
S9271	Pulchinenoside A Pulchinenoside A, a natural triterpenoid saponin, is a AMPARs and NMDAR modulator.
S5302	6-Methoxy-2-naphthoic acid 6-Methoxy-2-naphthoic acid是NMDAR的调节剂。

D-Aspartic acid (D-Asp) is an endogenous amino acid occurring in several tissues and cells of both invertebrates and vertebrates. It can regulate testosterone synthesis and may act on a stimulatory receptor (NMDA).

S9271

Pulchinenoside A

Pulchinenoside A, a natural triterpenoid saponin, is a AMPARs and NMDAR modulator.

S5302

6-Methoxy-2-naphthoic acid

6-Methoxy-2-naphthoic acid是NMDAR的调节剂。

研究领域

产品类型

NMDAR

抑制剂选择性比较

特异性亚型抑制剂

NMDAR产品