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PF-4455242
PF-4455242 is a selective, short-acting (non-"inactivating") antagonist of the κ-opioid receptor. Discovered by Pfizer Pfizer Inc. ( ) is an American multinational pharmaceutical and biotechnology corporation headquartered on 42nd Street in Manhattan, New York City. The company was established in 1849 in New York by two German entrepreneurs, Charles Pfizer ... in 2009, it was pursued in a Phases of clinical research#Phase I, phase I clinical trial for the treatment of bipolar disorder, and was also investigated as a treatment for depression (mood), depression and substance abuse. However, development was stopped in September 2010 due to toxicology findings in animals that had been exposed to the drug for three months. See also * κ-Opioid receptor#Antagonists, κ-Opioid receptor § Antagonists * List of investigational antidepressants References External links PF-4455242 - AdisInsight Amines Kappa-opioid receptor antagonists 1-Pyrrolidinyl compounds Sulfonamid ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
κ-Opioid Receptor
The κ-opioid receptor or kappa opioid receptor, abbreviated KOR or KOP, is a G protein-coupled receptor that in humans is encoded by the ''OPRK1'' gene. The KOR is coupled to the G protein Gi/G0 and is one of four related receptors that bind opioid-like compounds in the brain and are responsible for mediating the effects of these compounds. These effects include altering nociception, consciousness, motor control, and mood. Dysregulation of this receptor system has been implicated in alcohol and drug addiction. The KOR is a type of opioid receptor that binds the opioid peptide dynorphin as the primary endogenous ligand (substrate naturally occurring in the body). In addition to dynorphin, a variety of natural alkaloids, terpenes and synthetic ligands bind to the receptor. The KOR may provide a natural addiction control mechanism, and therefore, drugs that target this receptor may have therapeutic potential in the treatment of addiction. There is evidence that distribution ... [...More Info...] [...Related Items...] OR: [Wikipedia] [Google] [Baidu] |
