NVP CXCR2 20

NVP CXCR2 20 is a selective CXCR2 inhibitor with analgesic and antinociceptive activities. NVP CXCR2 20 selectively blocks CXCR2 signaling and attenuates mechanical and thermal hypersensitivity in rat chronic constriction injury (CCI) models. NVP CXCR2 20 inhibits CXCL3-induced hypersensitivity in naive mice and reduces elevated CXCL3 protein levels in the spinal cord and dorsal root ganglia (DRG) of CCI-exposed rats. NVP CXCR2 20 can be used for the research of neuropathic pain and chronic obstructive pulmonary disease (COPD)^[1][2][3]. In Vitro:NVP CXCR2 20 (100 nM; 30 min pre-incubation, 24 h with LPS) reduces LPS-induced CXCL1, CXCL2, and CXCL3 protein expression in primary rat microglial cell cultures and astroglial cell cultures^[1].
NVP CXCR2 20 (0.0005–10 μM) binds to human recombinant CXCR2 in CHO membranes with an IC₅₀ of 0.04 μM and acts as a functional CXCR2 antagonist with an [³⁵S]-GTPγS IC₅₀ of 0.14 μM; it shows a cLogP of 3.9 and a functional ligand-lipophilicity efficiency (LLE) of 3.0^[3].
NVP CXCR2 20 (10 μM) is selective for CXCR2, with no significant inhibitory activity (IC₅₀ > 10 μM) against a panel of 49 other GPCRs^[3]. In Vivo:NVP CXCR2 20 (10-30 μg/5 μL; intrathecal; single dose or 16 h and 1 h post-CCI, then once daily for 7 days) dose-dependently attenuates mechanical and thermal hypersensitivity in CCI-induced neuropathic pain in rats, with repeated 10 μg/5 μL doses reducing hypersensitivity on days 2 and 7 post-CCI and normalizing CXCL3 protein levels in the spinal cord and DRG without affecting glial activation^[1].
NVP CXCR2 20 (10 μg/5 μL; intrathecal; single dose on day 7 post-CCI, 4 hours prior to opioid co-administration) produces analgesic effects^[1].
NVP CXCR2 20 (60 μg/5 μL; intrathecal; single dose, 2 hours prior to intrathecal CXCL3) prevents CXCL3-induced mechanical and thermal hypersensitivity in naive mice^[1].