UBP 302

Names

[ Name ]:
UBP 302

[Synonym ]:
Tocris-2079
UBC
(S)-1-(2-AMINO-2-CARBOXYETHYL)-3-(2-CARBOXYBENZYL)PYRIMIDINE-2,4-DIONE
UBP-302
2f35

Biological Activity

[Description]:

UBP 302, the S enantiomer, is a potent and selective GluK1 (GluR5)-subunit containing kainate receptor antagonist (apparent Kd=402 nM), and displays very little affinity on GluK2 (GluR6) kainate receptors. Anxiolytic effects[1][2][3].

[Related Catalog]:

Signaling Pathways >> Neuronal Signaling >> iGluR

Signaling Pathways >> Membrane Transporter/Ion Channel >> iGluR

[Target]

Apparent Kd: 402 nM (GluK1)[2] IC50: 106 μM (AMPA receptors)[2]

[References]

[1]. More JC, et al. Characterisation of UBP296: a novel, potent and selective kainate receptor antagonist. Neuropharmacology. 2004 Jul;47(1):46-64.

[2]. Dolman NP, et al. Synthesis and pharmacology of willardiine derivatives acting as antagonists of kainate receptors. J Med Chem. 2005 Dec 1;48(24):7867-81.

[3]. Apland JP, et al. The limitations of diazepam as a treatment for nerve agent-induced seizures and neuropathology in rats: comparison with UBP302. J Pharmacol Exp Ther. 2014 Nov;351(2):359-72.

Chemical & Physical Properties

[ Molecular Formula ]:
C₁₅H₁₅N₃O₆

[ Molecular Weight ]:
333.29600

[ Exact Mass ]:
333.09600

[ PSA ]:
144.62000

MSDS

Click to get detail MSDS

Safety Information

[ Symbol ]:

GHS07

[ Signal Word ]:
Warning

[ Hazard Statements ]:
H302

[ RIDADR ]:
NONH for all modes of transport

Articles

The limitations of diazepam as a treatment for nerve agent-induced seizures and neuropathology in rats: comparison with UBP302.

J. Pharmacol. Exp. Ther. 351(2) , 359-72, (2014)

Exposure to nerve agents induces prolonged status epilepticus (SE), causing brain damage or death. Diazepam (DZP) is the current US Food and Drug Administration-approved drug for the cessation of nerv...

High-Throughput Screen of GluK1 Receptor Identifies Selective Inhibitors with a Variety of Kinetic Profiles Using Fluorescence and Electrophysiology Assays.

J. Biomol. Screen. 20 , 708-19, (2015)

GluK1, a kainate subtype of ionotropic glutamate receptors, exhibits an expression pattern in the CNS consistent with involvement in pain processing and migraine. Antagonists of GluK1 have been shown ...

A rat model of nerve agent exposure applicable to the pediatric population: The anticonvulsant efficacies of atropine and GluK1 antagonists.

Toxicol. Appl. Pharmacol. 284 , 204-16, (2015)

Inhibition of acetylcholinesterase (AChE) after nerve agent exposure induces status epilepticus (SE), which causes brain damage or death. The development of countermeasures appropriate for the pediatr...