R-PSOP 

R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the K_is of 52 and 32 nM for the human and rat NMUR2, respectively. R-PSOP shows moderate CNS penetration. R-PSOP can be used for the research of the eating disorders, obesity, pain, and stress-related disorders^[1].

From Schild analyses, the functional K_b values for R-PSOP are 92 and 155 nM at human and rat NMUR2, respectively (the effects of R-PSOP on the intracellular calcium mobilization response induced by NMU-25 in HEK293 cells expressing human or rat NMUR2)^[1].
R-PSOP strongly inhibits the responses stimulated by peptide agonists NMU-25, NMU-23, and NMU-8 in human embryonic kidney 293 cells expressing NMUR2^[1].
In functional assays measuring phosphoinositide turnover or intracellular calcium mobilization, R-PSOP strongly inhibits the responses stimulated by peptide agonists NMU-25, NMU-23, and NMU-8 in human embryonic kidney 293 cells expressing NMUR2^[1].
R-PSOP concentration-dependently inhibits the phosphoinositide (PI) turnover turnover response in human NMUR2-expressing cells stimulated by 10 nM NMU-25 (EC₅₀ of 5 nM). The IC₅₀ value is determined to be 86 nM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

R-PSOP (10 μL 50 nmol; intrathecal injection; male Sprague-Dawley rats) attenuates NMU-23-evoked nociceptive responses in a rat spinal reflex preparation^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

350.41

C₂₀H₂₂N₄O₂

1185189-97-2

Solid

White to off-white

O=C(NC1=CC=CC=C1)NC2=CN=C3O[C@]4(CC3=C2)C(CC5)CCN5C4

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• [1]. Liu JJ, et al. Discovery and pharmacological characterization of a small-molecule antagonist at neuromedin U receptor NMUR2. J Pharmacol Exp Ther. 2009;330(1):268-275.  [Content Brief]