Cyclorphan
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Cyclorphan is an opioid analgesic of the morphinan family that was never marketed.[1] It acts as a μ-opioid receptor (MOR) weak partial agonist or antagonist, κ-opioid receptor (KOR) full agonist, and, to a much lesser extent, δ-opioid receptor (DOR) agonist (75-fold lower affinity relative to the KOR).[2][3] The drug was first synthesized in 1964 by scientists at Research Corporation.[4][5]Template:Rp In clinical trials, it had relatively long duration, good absorption, and provided strong pain relief but produced psychotomimetic effects via KOR activation, so its development was not continued.[1][5]Template:Rp
See also
References
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- ↑ US Patent 3,285,922
- ↑ a b Varghese V & Hudlicky T. A Short History of the Discovery and Development of Naltrexone and Other Morphine Derivatives. Chapter 6 in Natural Products in Medicinal Chemistry, Volume 60 of Methods and Principles in Medicinal Chemistry. Ed. Stephen Hanessian. John Wiley & Sons, 2013. Template:ISBN
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