R-PSOP

• CAT Number: I045184
• CAS Number: 1185189-97-2
• Molecular Formula: C20H22N4O2
• Molecular Weight: 350.41
• Purity: ≥95%
• Synonyms: 1-phenyl-3-[(3R)-spiro[1-azabicyclo[2.2.2]octane-3,2′-3H-furo[2,3-b]pyridine]-5′-yl]urea
• InChI: InChI=1S/C20H22N4O2/c25-19(22-16-4-2-1-3-5-16)23-17-10-14-11-20(26-18(14)21-12-17)13-24-8-6-15(20)7-9-24/h1-5,10,12,15H,6-9,11,13H2,(H2,22,23,25)/t20-/m0/s1
• InChIKey: BUOWEYLLAFLKCW-FQEVSTJZSA-N
• SMILES: C1CN2CCC1C3(C2)CC4=C(O3)N=CC(=C4)NC(=O)NC5=CC=CC=C5

R-PSOP is highly potent and selective nonpeptidic NMUR2 antagonist. R-PSOP binds to NMUR2 with the Kis 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 Kb 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].
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].

Reference

[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.
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