RP-67580

RP-67580 is a potent and selective non-peptide antagonist of the neurokinin 1 receptor (NK1R), which is the primary receptor for substance P. It exhibits high affinity for rat and mouse NK1 receptors (Ki ≈ 2.9 nM) and much lower affinity for human NK1 receptors. The compound does not show significant antagonistic activity against NK2 or NK3 receptors. In preclinical studies, RP‑67580 demonstrated antinociceptive effects in vivo—likely through inhibition of substance P-mediated signaling—and was shown to reduce plasma extravasation and inflammation in animal models. Its mechanism involves competitive inhibition at the orthosteric binding site of the neurokinin 1 receptor, blocking substance P-induced responses such as pain transmission and inflammatory processes. Developed originally by Rhône-Poulenc Rorer (now part of Sanofi), it was investigated as a potential treatment for pain and inflammation but did not advance beyond preclinical development[2][3][4][5][6][9].

Other names

(3aR,7aR)-Octahydro-2-[1-imino-2-(2-methoxyphenyl)ethyl]-7,7-diphenyl-4H-isoindolCAS 135911-02-3CAS135911-02-3CAS-135911-02-3