GRK2 Inhibitor 1

GRK2 Inhibitor 1 (methyl 5-[2- (5-nitro-2-furyl) vinyl]-2-furoate) is a dual GRK2/β-ARK1 inhibitor that induces dopamine (DA) inhibition reversal (DIR) . GRK2 Inhibitor 1 can also block serotonin-induced or neurotensin-induced DIR reversal. Note: DIR refers to the phenomenon in which neurons in addiction-related brain pathways become less sensitive to DA inhibition when exposed to moderate concentrations of DA for a long time[1].

Product Specifications

CAS Number

[24269-96-3]

UNSPSC

12352005

Hazard Statement

H302, H315, H319

Target

Dopamine Receptor; G Protein-coupled Receptor Kinase (GRK)

Type

Reference compound

Related Pathways

GPCR/G Protein; Neuronal Signaling

Applications

Neuroscience-Neuromodulation

Field of Research

Cardiovascular Disease

Assay Protocol

https://www.medchemexpress.com/grk2-inhibitor-1.html

Purity

98.06

Solubility

DMSO : 41.67 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C(OC)C1=CC=C(O1)/C=C/C2=CC=C(O2)[N+]([O-])=O

Molecular Formula

C12H9NO6

Molecular Weight

263.20

Precautions

H302, H315, H319

References & Citations

[1]Nimitvilai S, et al. Reversal of dopamine D2 agonist-induced inhibition of ventral tegmental area neurons by Gq-linked neurotransmitters is dependent on protein kinase C, G protein-coupled receptor kinase, and dynamin. J Pharmacol Exp Ther. 2013 Jan;344 (1) :253-63.