Syntheses of novel high affinity ligands for opioid receptors
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چکیده
منابع مشابه
Selectively Promiscuous Opioid Ligands: Discovery of High Affinity/Low Efficacy Opioid Ligands with Substantial Nociceptin Opioid Peptide Receptor Affinity
Emerging clinical and preclinical evidence suggests that a compound displaying high affinity for μ, κ, and δ opioid (MOP, KOP, and DOP) receptors and antagonist activity at each, coupled with moderate affinity and efficacy at nociceptin opioid peptide (NOP) receptors will have utility as a relapse prevention agent for multiple types of drug abuse. Members of the orvinol family of opioid ligands...
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Background The opioid (KOP) receptor belongs to the family of seven transmembrane G protein-coupled receptors (GPCRs) and it plays a significant role in a broad range of physiological functions. Stimulation of the KOP receptor results in analgesic actions, and KOP agonists appear to have some advantages over the μ opioid (MOP) receptor agonists. Inhibiting KOP receptors is proposed to be useful...
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ژورنال
عنوان ژورنال: Bioorganic & Medicinal Chemistry Letters
سال: 2009
ISSN: 0960-894X
DOI: 10.1016/j.bmcl.2009.02.078