| 词条 | Cyclorphan |
| 释义 |
| IUPAC_name = (−)-3-Hydroxy-N-cyclopropylmethylmorphinan | image = cyclorphan_structure.svg | tradename = | pregnancy_AU = | pregnancy_US = | pregnancy_category = | legal_AU = | legal_CA = | legal_UK = | legal_US = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | excretion = | CAS_number = 4163-15-9 | ATC_prefix = | ATC_suffix = | PubChem = 5359966 | DrugBank = | ChemSpiderID = 4514407 | ChEMBL = 49269 | C=20 | H=27 | N=1 | O=1 | molecular_weight = 297.434 g/mol | smiles = Oc1ccc4c(c1)[C@@]25[C@H]([C@H](N(CC2)CC3CC3)C4)CCCC5 | melting_point = 188 | boiling_point = 458.4 | density = 1.19 }} 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]{{rp|232}} 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]{{rp|232, 237}} See also
References1. ^1 {{cite book|author=Maxwell Gordon|title=Psychopharmacological Agents|url=https://books.google.com/books?id=yt2KcKcJROgC&pg=PA19|date=2 December 2012|publisher=Elsevier Science|isbn=978-0-323-15963-0|pages=19–}} {{Analgesics}}{{Hallucinogens}}{{Opioidergics}}{{analgesic-stub}}2. ^{{cite book|author=Linda P. Dwoskin|title=Emerging Targets & Therapeutics in the Treatment of Psychostimulant Abuse|url=https://books.google.com/books?id=b3UpAgAAQBAJ&pg=PA403|date=29 January 2014|publisher=Elsevier Science|isbn=978-0-12-420177-4|pages=403–}} 3. ^{{cite book |vauthors=Aldrich JV, Vigil-Cruz SC| chapter = Narcotic Analgesics | doi = 10.1002/0471266949.bmc100 | pages = 331–482 | title = Burger's Medicinal Chemistry and Drug Discovery | edition = 7th | date = 2003 | isbn = 9780471266945}} 4. ^US Patent 3,285,922 5. ^1 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. {{ISBN|9783527676552}} 7 : Synthetic opioids|Kappa agonists|Delta-opioid agonists|Dissociative drugs|Morphinans|Phenols|Cyclopropanes |
| 随便看 |
|
开放百科全书收录14589846条英语、德语、日语等多语种百科知识，基本涵盖了大多数领域的百科知识，是一部内容自由、开放的电子版国际百科全书。