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Wikipedia

Ro4-1539

Ro4-1539 (furethylnorlevorphanol) is an opioid analgesic drug from the morphinan series that was discovered by the pharmaceutical company Hoffmann–La Roche in the 1950s.[1] It acts as a potent μ-opioid agonist, and was found to be around 30-60 times more potent than the related drug levorphanol in animal experiments.[2][3] Although it has high potency, long duration, and good therapeutic index (1100 in animal studies),[4] Ro4-1539 had no particular clinical advantages over other available opioid drugs, and was never commercially marketed.

Ro4-1539
Legal status
Legal status
  • US: Never FDA approved
  • In general: legal
Pharmacokinetic data
Bioavailability70% oral IV 100%
Elimination half-life11-16h
Identifiers
  • 17-(2-(Furan-2-yl)ethyl)-3-hydroxymorphinan
CAS Number
  • 27767-85-7 Y
PubChem CID
  • 20834001
CompTox Dashboard (EPA)
  • DTXSID20950452
Chemical and physical data
FormulaC22H27NO2
Molar mass337.463 g·mol−1
3D model (JSmol)
  • Interactive image
  • C3CCCC1C35c2cc(O)ccc2CC1N(CC5)CCc4ccco4
  (verify)

Ro4-1539 has never formally undergone clinical trials in humans, but based on its effects in animals it would be expected to produce effects similar to those of other potent opioid agonists, including strong analgesia, sedation, euphoria, constipation, itching, tachyphylaxis and respiratory depression, which could be harmful or fatal.

See also

References

  1. ^ US 2970147, "3-hydroxy-N-(heterocyclic-ethyl)-morphinans", published 1961-01-31 
  2. ^ Nathan B. Eddy, Hedwig Besendorf and Béla Pellmont. Synthetic analgesics - Aralkyl substitution on nitrogen of morphinan. UNODC Bulletin on Narcotics 1958 p 23-42.
  3. ^ Hellerbach J, Schnider O, Besendorf H, Pellmont B (1966). "Morphinans". Synthetic Analgesics. Part IIA. Pergamon Press.
  4. ^ Bulletin on Narcotics October–December 1956 page 37

1539, furethylnorlevorphanol, opioid, analgesic, drug, from, morphinan, series, that, discovered, pharmaceutical, company, hoffmann, roche, 1950s, acts, potent, opioid, agonist, found, around, times, more, potent, than, related, drug, levorphanol, animal, expe. Ro4 1539 furethylnorlevorphanol is an opioid analgesic drug from the morphinan series that was discovered by the pharmaceutical company Hoffmann La Roche in the 1950s 1 It acts as a potent m opioid agonist and was found to be around 30 60 times more potent than the related drug levorphanol in animal experiments 2 3 Although it has high potency long duration and good therapeutic index 1100 in animal studies 4 Ro4 1539 had no particular clinical advantages over other available opioid drugs and was never commercially marketed Ro4 1539Legal statusLegal statusUS Never FDA approved In general legalPharmacokinetic dataBioavailability70 oral IV 100 Elimination half life11 16hIdentifiersIUPAC name 17 2 Furan 2 yl ethyl 3 hydroxymorphinanCAS Number27767 85 7 YPubChem CID20834001CompTox Dashboard EPA DTXSID20950452Chemical and physical dataFormulaC 22H 27N O 2Molar mass337 463 g mol 13D model JSmol Interactive imageSMILES C3CCCC1C35c2cc O ccc2CC1N CC5 CCc4ccco4 verify Ro4 1539 has never formally undergone clinical trials in humans but based on its effects in animals it would be expected to produce effects similar to those of other potent opioid agonists including strong analgesia sedation euphoria constipation itching tachyphylaxis and respiratory depression which could be harmful or fatal See also Edit14 Cinnamoyloxycodeinone 14 Phenylpropoxymetopon 7 PET N Phenethylnormorphine N Phenethyl 14 ethoxymetopon Phenomorphan RAM 378References Edit US 2970147 3 hydroxy N heterocyclic ethyl morphinans published 1961 01 31 Nathan B Eddy Hedwig Besendorf and Bela Pellmont Synthetic analgesics Aralkyl substitution on nitrogen of morphinan UNODC Bulletin on Narcotics 1958 p 23 42 Hellerbach J Schnider O Besendorf H Pellmont B 1966 Morphinans Synthetic Analgesics Part IIA Pergamon Press Bulletin on Narcotics October December 1956 page 37 This analgesic related article is a stub You can help Wikipedia by expanding it vte Retrieved from https en wikipedia org w index php title Ro4 1539 amp oldid 1121502390, wikipedia, wiki, book, books, library,

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