| Bioactivity | 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]. | ||||||||||||
| Invitro | 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]. | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | R-PSOP | ||||||||||||
| CAS | 1185189-97-2 | ||||||||||||
| Formula | C20H22N4O2 | ||||||||||||
| Molar Mass | 350.41 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |