188196-22-7

188196-22-7 structure

Name: frakefamide
Chemical Name: frakefamide
CAS Number: 188196-22-7
Molecular Formula: C₃₀H₃₄FN₅O₅
Molecular Weight: 563.620
Catalog: Signaling Pathways GPCR/G Protein Opioid Receptor
Create Date: 2018-10-06 16:14:18
Modify Date: 2024-01-03 13:13:24
Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system[1][2].

Name	frakefamide
Synonyms	L-Phenylalaninamide, 4-fluoro-L-phenylalanyl-N-[(2R)-2-[[(2S)-2-amino-3-(4-hydroxyphenyl)-1-oxopropyl]amino]-1-oxopropyl]- 4-Fluoro-L-phenylalanyl-N-[(2R)-2-(L-tyrosylamino)propanoyl]-L-phenylalaninamide frakefamide

Description	Frakefamide is a potent analgesic that acts as a peripheral active μ-selective receptor agonist. Frakefamide is unable to penetrate the blood-brain-barrier and enter the central nervous system[1][2].
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Opioid Receptor Signaling Pathways >> Neuronal Signaling >> Opioid Receptor Research Areas >> Neurological Disease
In Vivo	Frakefamide (LEF576) yields a dose dependent increase in morphine appropriate responding to 50% at the highest dose tested (10 μmol/kg) after infusion durations of 2 min, whereas after 15 min infusions a maximum of 25% morphine appropriate responding was occasioned at 17.5 μmol/kg[1][2].
References	[1]. Modalen AO, et al. A novel molecule (frakefamide) with peripheral opioid properties: the effects on resting ventilation compared with morphine and placebo. Anesth Analg. 2005 Mar;100(3):713-7. [2]. Swedberg MD, et al. Drug discrimination: A versatile tool for characterization of CNS safety pharmacology and potential for drug abuse. J Pharmacol Toxicol Methods. 2016 Sep-Oct;81:295-305.