CAS 188196-22-7|frakefamide

Introduction:Basic information about CAS 188196-22-7|frakefamide, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.
Common Namefrakefamide
CAS Number188196-22-7Molecular Weight563.620
Density1.3±0.1 g/cm3Boiling Point897.9±65.0 °C at 760 mmHg
Molecular FormulaC30H34FN5O5Melting Point/
MSDS/Flash Point496.8±34.3 °C

Names

Namefrakefamide
SynonymMore Synonyms

frakefamide BiologicalActivity

DescriptionFrakefamide 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 CatalogSignaling Pathways >>GPCR/G Protein >>Opioid ReceptorSignaling Pathways >>Neuronal Signaling >>Opioid ReceptorResearch Areas >>Neurological Disease
In VivoFrakefamide (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.

Chemical & Physical Properties

Density1.3±0.1 g/cm3
Boiling Point897.9±65.0 °C at 760 mmHg
Molecular FormulaC30H34FN5O5
Molecular Weight563.620
Flash Point496.8±34.3 °C
Exact Mass563.254395
LogP1.45
Vapour Pressure0.0±0.3 mmHg at 25°C
Index of Refraction1.610
InChIKeyGTPHQORJKFJIRB-JTQLPTLWSA-N
SMILESCC(NC(=O)C(N)Cc1ccc(O)cc1)C(=O)NC(Cc1ccc(F)cc1)C(=O)NC(Cc1ccccc1)C(N)=O

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
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