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U-77891 is an opioid analgesic drug that w … U-77891 is an opioid analgesic drug that was first synthesized in 1983 by the Upjohn company. It was originally synthesized to prove that the removal of a single methylene of the benzamide would alter a κ-opioid receptor agonist such as U-50488 into an μ-opioid receptor agonist, as well as producing a semi-rigid derivative of U-47700. This would help elucidate the relative positions of the hydrogen-bond acceptors and substituted aromatic system to find the compound with the lowest Ki value in a series of benzamide opioids dating back to the 1970s. The original work found a mixture of agonists and antagonists. U-77891 acts as an agonist of the μ-opioid, δ-opioid and κ-opioid receptors with Ki values of 2, 105 and 2300 nM, respectively. The compound has ED50 values of 0.02 mg/kg and 0.21 mg/kg in mouse phenylquinone writhing and tail-flick assays. One reason for the high potency is the LogP of 4.57, allowing it to accumulate in fatty tissue such as the brain.umulate in fatty tissue such as the brain.
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| rdfs:comment |
U-77891 is an opioid analgesic drug that w … U-77891 is an opioid analgesic drug that was first synthesized in 1983 by the Upjohn company. It was originally synthesized to prove that the removal of a single methylene of the benzamide would alter a κ-opioid receptor agonist such as U-50488 into an μ-opioid receptor agonist, as well as producing a semi-rigid derivative of U-47700. This would help elucidate the relative positions of the hydrogen-bond acceptors and substituted aromatic system to find the compound with the lowest Ki value in a series of benzamide opioids dating back to the 1970s. The original work found a mixture of agonists and antagonists.und a mixture of agonists and antagonists.
|
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U-77891
|
