SYM 2081

SYM 2081 is a kainate receptor agonist. SYM 2081 is a substrate of EAAT1 (Km of 54 μM) . SYM 2081 inhibits EAAT2-mediated glutamate transport (Kb is 3.4 μM in Xenopus oocytes), modulates Apoptotic signaling pathways (increases Bcl-2 and decreases Bax/caspase-3 expression) . SYM 2081 exhibits neuroprotective activity. SYM 2081 can be used in the study of hypoxic-ischemic brain damage and inflammatory or neuropathic pain[1][2][3][4].

Product Specifications

CAS Number

[31137-74-3]

UNSPSC

12352211

Hazard Statement

H302, H315, H319, H335

Target

Bcl-2 Family; Caspase; EAAT; iGluR

Type

Reference compound

Related Pathways

Apoptosis; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

Neuroscience-Neurodegeneration

Field of Research

Inflammation/Immunology; Neurological Disease; Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/sym-2081.html

Purity

98.0

Solubility

H2O : 50 mg/mL (ultrasonic)

Smiles

N[C@@H](C[C@@H](C)C(O)=O)C(O)=O

Molecular Formula

C6H11NO4

Molecular Weight

161.16

Precautions

H302, H315, H319, H335

References & Citations

[1]Lee JY, et al. Furthering pharmacological and physiological assessment of the glutamatergic receptors at the Drosophila neuromuscular junction. Comp Biochem Physiol C Toxicol Pharmacol. 2009 Nov;150 (4) :546-57.|[2]Vandenberg RJ, et al. Contrasting modes of action of methylglutamate derivatives on the excitatory amino acid transporters, EAAT1 and EAAT2. Mol Pharmacol. 1997 May;51 (5) :809-15.|[3]Turner MS, et al. SYM 2081, an agonist that desensitizes kainate receptors, attenuates capsaicin and inflammatory hyperalgesia. Brain Res. 2003 May 30;973 (2) :252-64.|[4]Park J K, et al. SYM 2081 Exerts Neuroprotective Effect Modulating Anti-Apoptosis in the Hypoxic-Ischemic Brain Injury of Neonatal Rats[J]. Perinatology, 2019, 30 (3) : 117-125.