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].
PL-017 is a potent and selective μ opioid receptor agonist with IC50 of 5.5 nM for 125I-FK 33,824 binding to the μ site. PL-017 produces durable and reversible analgesia in rats.
PL-017 has an IC 50 of 10000 nM for 125 I-DADLE binding to δ site.
PL-017 (0.22, 0.45, 0.9 nmol/rat; icv) 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.
IC50: 5.5 nM ( 125 I-FK 33,824 binding to μ site)
[1] K J Chang, et al. Potent morphiceptin analogs: structure activity relationships and morphine-like activities. J Pharmacol Exp Ther. 1983 Nov;227(2):403-8. PMID:6313901