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PL-017

Names

[ CAS No. ]:
83397-56-2

[ Name ]:
PL-017

[Synonym ]:
H-TYR-PRO-N-ME-PHE-D-PRO-NH2
Cardiogenol C hydrochloride
D-Prolinamide, L-tyrosyl-L-prolyl-N-methyl-L-phenylalanyl-
L-Prolinamide, L-tyrosyl-L-prolyl-N-methyl-L-phenylalanyl-
L-Tyrosyl-L-prolyl-N-methyl-L-phenylalanyl-L-prolinamide
L-Tyrosyl-L-prolyl-N-methyl-L-phenylalanyl-D-prolinamide
L-Tyr-L-Pro-N-Methyl-L-Phe-D-Pro-NH2
[NMePhe3, DPro4] b-Casomorphin: 1-4, amide, bovine

Biological Activity

[Description]:

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].

[Related Catalog]:

Signaling Pathways >> GPCR/G Protein >> Opioid Receptor
Signaling Pathways >> Neuronal Signaling >> Opioid Receptor
Research Areas >> Neurological Disease

[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].

[References]

[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.

Chemical & Physical Properties

[ Density]:
1.3±0.1 g/cm3

[ Boiling Point ]:
878.5±65.0 °C at 760 mmHg

[ Molecular Formula ]:
C29H37N5O5

[ Molecular Weight ]:
535.635

[ Flash Point ]:
485.1±34.3 °C

[ Exact Mass ]:
535.279480

[ PSA ]:
150.27000

[ LogP ]:
0.93

[ Vapour Pressure ]:
0.0±0.3 mmHg at 25°C

[ Index of Refraction ]:
1.630

[ Storage condition ]:
-20°C

Safety Information

[ Safety Phrases ]:
22-24/25

Related Compounds