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| Names | |
|---|---|
| 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) | |
| ChemSpider | |
| UNII | |
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| Properties | |
| C36H49N9O4 | |
| Molar mass | 671.847 g·mol−1 |
Except where otherwise noted, data are given for materials in theirstandard state (at 25 °C [77 °F], 100 kPa). | |
CR665 (H-D-Phe-D-Phe-D-Nle-D-Arg-NH-4-Picolyl), also known by the previous developmental code namesFE-200665 andJNJ-38488502, is an allD-amino acidpeptide that acts as a peripherally restrictedκ-opioid receptor agonist. The selectivity for FE 200665 is 1/16,900/84,600 for the human κ,μ, andδ opioid receptors, respectively. The dose of FE 200665 required to produce motor impairment (measure ofCNS penetration) was 548 times higher than the dose required forantinociceptive activity.[1] It is being developed for use byCara 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/kgI.V., and was compared to 15 mgoxycodone orally. CR665 had analgesic effects on visceral pain, but produced ahyperalgesic response in a skin pinch test.[2]
