Ro 25-6981|NMDA receptors NR1C & NR2B blocker

Cas No.:	169274-78-6
SMILES:	OC1=CC=C([C@H](O)[C@@H](C)CN2CCC(CC3=CC=CC=C3)CC2)C=C1
Formula:	C₂₂H₂₉NO₂
M.Wt:	339.47
Purity:	>98%
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

Ro 25-6981 is a potent and selective activity-dependent blocker of NMDA receptors containing the NR2B subunit. IC50 values are 0.009 and 52 μM for cloned receptor subunit combinations NR1C/NR2B and NR1C/NR2A respectively. in vitro: Ro 25-6981 inhibited 3H-MK-801 binding to rat forebrain membranes in a biphasic manner with IC50 values of 0.003 microM and 149 microM for high- (about 60%) and low-affinity sites, respectively. NMDA receptor subtypes expressed in Xenopus oocytes were blocked with IC50 values of 0.009 microM and 52 microM for the subunit combinations NR1C & NR2B and NR1C & NR2A, respectively, which indicated a >5000-fold selectivity . Increasing the concentration of spermidine did not change the efficacy of RO 25-6981 and minimally changed the IC(50) value. Epsilon1Q336R receptors were more inhibited by ifenprodil and RO 25-9681 than wildtype epsilon1 receptors in ligand binding assays but not in functional assays. in vivo: Intrathecal injection of Ro 25-6981 significantly enhanced the paw withdrawal mechanical threshold and paw withdrawal thermal latency after the operation. Significant change has been observed after intrathecal injection of 800.0 μg of Ro 25-6981 and at 2h after operation in the oblique pull test degree and BBB rating score. Pretreatment of Ro 25-6981 decreased the high level expression of NR2B with tyrosine phosphorylation in spinal dorsal horn of the rat model after the operation.

Cat. No.	Product name	Field of application
DC47600	NMDA receptor antagonist-3	NMDA receptor antagonist-3, a NMDA receptor antagonist, stands out with a remarkable percentage of recovery (40.0%, at 100 μM) and safe toxicological profile in SH-SY5Y and human adipose mesenchymal stem cells.
DC47255	Co 101244 hydrochloride	Co 101244 (PD 174494) hydrochloride is a NR2B-containing NMDA receptor antagonist.
DC47241	CGP 39551	CGP 39551 is a potent, orally active, competitive N-methyl-D-aspartate (NMDA) receptor antagonist with potent anticonvulsant activity. CGP 39551 shows measurable inhibitory activity at both L-[3H]-glutamate (Ki=8.4 μM).
DC47082	Zelquistinel	Zelquistinel is a N-methyl-D-aspartate (NMDA) receptor partial agonist used for the research of depression, anxiety and other related psychiatric disorders.
DC47045	Plazinemdor	Plazinemdor is a N-methyl-D-aspartate(NMDA) receptor positive allosteric modulator. Plazinemdor can be uses in the research of psychiatric, neurological, and neurodevelopmental disorders, as well as diseases of the nervous system..
DC46862	D-AP4	D-AP4 (D-APB; D-2-Amino-4-phosphonobutyric acid), a phosphono analogue of glutamate, is an NMDA broad spectrum excitatory amino acid receptor antagonist. D-AP4 also is an agonist for a quisqualate-sensitized AP6 site in hippocampus. D-AP4 inhibits AMPA receptor-stimulated 57Co2+ influx in cultured cerebellar granule cells (IC50 ≥ 100 μM).
DC46424	Cl-HIBO	Cl-HIBO is a highly subtype-selective GluR1/2 agonist (EC50=4.7 and 1.7 μM, respectively). Cl-HIBO is a potent AMPA receptor agonist (IC50=0.22 μM). Cl-HIBO has desensitizing properties.
DC45927	(RS)-AMPA monohydrate	(RS)-AMPA ((±)-AMPA) monohydrate is a glutamate analogue and a potent and selective excitatory neurotransmitter L-glutamic acid agonist. (RS)-AMPA monohydrate does not interfere with binding sites for kainic acid or NMDA receptors.
DC45878	NS-102	NS-102 is a selective kainate (GluK2) receptors antagonist. NS-102 is a potent GluR6/7 receptor antagonist.
DC45310	UBP316	UBP316 (ACET) is a highly potent and selective kainate receptor GluK1 (GluR5) antagonist, with a Kb value of 1.4 nM. UBP316 is effective at blocking the depression of both field excitatory postsynaptic potentials (fEPSPs) and monosynaptically-evoked GABAergic transmission induced by ATPA, a GluK1 selective agonist.