PL-017

PL-017 is a potent and selective μ opioid receptor agonist with an IC₅₀ of 5.5 nM for ¹²⁵I-FK 33,824 binding to μ site. PL-017 produces long-lasting, reversible analgesia in rats^[1]. IC50 & Target: IC50: 5.5 nM (¹²⁵I-FK 33,824 binding to μ site)^[1] In Vitro: PL-017 has an IC₅₀ of 10000 nM for ¹²⁵I-DADLE binding to δ site^[1]. In Vivo: PL-017 (0.22, 0.45, 0.9 nmol/rat; i.c.v.) has the time of maximum effect of approximately 15 to 30 mm after injection at lower doses and produces analgesia lasting as long as 4 hours with larger doses in male Sprague-Dawley rats weighing 250 to 375 g^[1].