In vitro: [3H]MK-801 binds with NMDA receptor with a Kd of 37.2 ±2.7 nM in rat cerebral cortical membranes. MK-801 shows an inhibitory activity against N-methyl-D-aspartate-induced [3H]norepinephrine (NE) release and [3H]TCP binding in the hippocampus with IC50s of 20 nM and 9 nM, respectively. MK-801 progressively suppresses of current induced by NMDA. Mg2+ (10 mM) prevents MK-801 from blocking the N-Me-D-Asp-induced current, even when MK-801 is applied for a long time in the presence of NMDA. MK-801 blocks NMDA-activated single-channel activity in outside-out patches. MK-801 (< 500 μM) inhibits activation of microglia induced by LPS with increased Cox-2 protein expression in BV-2 cells. MK-801 (< 500 μM) reduces microglial TNF-α output with an EC50 of 400 μM in BV-2 cells.
In vivo: MK-801 (1 mg/kg) treatment before each METH injection reduces the extent of DA depletion by 55% in striatal of mice. MK-801 (1 mg/kg) also attenuates the effects of METH on microglial activation in striatal of mice. MK-801 (0.05, 0.2 mg/kg, i.p.) attenuates subsequent cocaine-primed reinstatement without disruption in rats. MK-801 (0.2 mg/kg, i.p.) prior to two reactivation sessions in the home cage shows no suppression on subsequent cocaine-primed reinstatement.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.
|Solubility||10 mM in DMSO|
Neonatal immune activation by lipopolysaccharide causes inadequate emotional responses to novel situations but no changes in anxiety or cognitive behavior in Wistar rats.
Vojtechova I, et al. Behav Brain Res. 2018 May 2;349:42-53. PMID: 29729302.
In Vitro and In Vivo Characterization of PCC0104005, a Novel Modulator of Serotonin-Dopamine Activity, as an Atypical Antipsychotic Drug.
Xu Y, et al. Sci Rep. 2018 May 2;8(1):6892. PMID: 29720711.
|Related GluR Products|
JNJ-42153605 is a positive allosteric modulator of the metabotropic glutamate 2 (mGlu2) receptor with an EC50 of 17 nM.
Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an IC50 of 500 nM for human mGlu4.
Beclomethasone dipropionate is a potent glucocorticoid steroid used for the treatment of rhinitis and sinusitis.
Topiramate is an anticonvulsant that antagonizes GluR5 receptors and acts as a positive allosteric modulator of GABA receptor-mediated currents.
ADX47273 is a potent and specific mGlu5 positive allosteric modulator(PAM) with EC50 of 0.17 μM, showing no activity at other mGlu subtypes.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2017 AbMole BioScience. All Rights Reserved.