Potent and selective nociceptin receptor antagonist.

UFP 101 is a potent, selective and competitive antagonist at the nociceptin receptor. UFP 101 binds to nociceptin receptors with high affinity (pKi 10.24) and possesses ~3000 fold selectivity over the classical opioid receptors. UFP 101 is antinociceptive and opposes the action of nociceptin in vivo, with an antinociceptive effect when given i.c.v. while being inactive following spinal administration in mice. UFP 101 also shows antidepressant effects in distinct species and can reduce microvascular inflammation to lipopolysaccharide in vivo.

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