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Names | |
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IUPAC name
(R)-2-((R)-2-((R)-2-amino-3-phenylpropanamido)-3-phenylpropanamido)-N-((R)-5-guanidino-1-oxo-1-((pyridin-4-ylmethyl)amino)pentan-2-yl)hexanamide | |
Other names
CR 665; JNJ 38488502 | |
Identifiers | |
3D model (JSmol) |
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ChemSpider | |
PubChem CID |
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UNII | |
CompTox Dashboard (EPA) |
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Properties | |
C36H49N9O4 | |
Molar mass | 671.847 g·mol−1 |
Except where otherwise noted, data are given for materials in their standard state (at 25 °C [77 °F], 100 kPa).
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CR665 (H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-Picolyl), also known by the previous developmental code names FE-200665 and JNJ-38488502, is an all D-amino acid peptide that acts as a peripherally restricted κ-opioid receptor agonist. The selectivity for FE 200665 is 1/16,900/84,600 for the human κ, μ, and δ opioid receptors, respectively. The dose of FE 200665 required to produce motor impairment (measure of CNS penetration) was 548 times higher than the dose required for antinociceptive activity.[1] It is being developed for use by Cara Therapeutics under the code name CR665.
A small, blinded study was done in healthy humans to determine the analgesic effects. CR665 was dosed at 0.36 mg/kg I.V., and was compared to 15 mgoxycodone orally. CR665 had analgesic effects on visceral pain, but produced a hyperalgesic response in a skin pinch test.[2]
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μ-opioid (MOR) |
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δ-opioid (DOR) |
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κ-opioid (KOR) |
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Nociceptin (NOP) |
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Others |
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