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Cara possesses best-in-class peripherally-selective
molecules that interact with kappa opioid receptors present on peripheral,
pain-sensing nerves. These compounds exhibit potent analgesic and anti-inflammatory
properties in animals. Unlike currently marketed opioids, these new
compounds do not produce inhibition of intestinal transit (ileus),
do not induce life-threatening respiratory depression, nor do they
elicit signs of addiction or euphoria in animal models.
The degree of kappa receptor selectivity displayed by CR665 (also seen
with analogs such as CR666) ranks as best-in-class compared to all other
previously developed compounds for this therapeutic target. Moreover,
CR665 displayed no significant affinity for any other non-opioid known
receptors. |