Bromadoline
Opioid analgesic drug
- none
- 4-bromo-N-[(1R,2R)-2-(dimethylamino)cyclohexyl]benzamide
2418521-61-4
Y 67579-24-2 (mixture of trans isomers)
- 6328449
- R8DWN01P1M
- DTXSID40217897
- Interactive image
- CN(C)[C@@H]1CCCC[C@H]1NC(=O)C2=CC=C(C=C2)Br
InChI
- InChI=1S/C15H21BrN2O/c1-18(2)14-6-4-3-5-13(14)17-15(19)11-7-9-12(16)10-8-11/h7-10,13-14H,3-6H2,1-2H3,(H,17,19)/t13-,14-/m1/s1
- Key:UFDJFJYMMIZKLG-ZIAGYGMSSA-N
Bromadoline (U-47931E)[1] is an opioid analgesic selective for the μ-opioid receptor[2] developed by the Upjohn company in the 1970s.[3] The drug has a potency lying between that of codeine and morphine, being slightly stronger than pentazocine.[4] Bromadoline is related to AH-7921 and U-47700.[5]
See also
- AH-7921
- U-47700
- Spiradoline
- U-50488
References
- ^ Unlisted Drugs. Vol. 34–35. Chatham: Pharmaceutical Section, Special Libraries Association. 1982. p. 392. ISBN 978-0-913210-13-0.
- ^ Hayes AG, Skingle M, Tyers MB (March 1987). "Evaluation of the receptor selectivities of opioid drugs by investigating the block of their effect on urine output by beta-funaltrexamine". The Journal of Pharmacology and Experimental Therapeutics. 240 (3): 984–8. PMID 3559988.
- ^ Jacob Szmuszkovicz (4 July 1978). "Patent US4098904 - Analgesic N-(2-aminocycloaliphatic)benzamides". The Upjohn Company.
- ^ Hayes AG, Sheehan MJ, Tyers MB (August 1987). "Differential sensitivity of models of antinociception in the rat, mouse and guinea-pig to mu- and kappa-opioid receptor agonists". British Journal of Pharmacology. 91 (4): 823–32. doi:10.1111/j.1476-5381.1987.tb11281.x. PMC 1853585. PMID 2822190.
- ^ Cheney BV, Szmuszkovicz J, Lahti RA, Zichi DA (December 1985). "Factors affecting binding of trans-N-[2-(methylamino)cyclohexyl]benzamides at the primary morphine receptor". Journal of Medicinal Chemistry. 28 (12): 1853–64. doi:10.1021/jm00150a017. PMID 2999404.
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Antagonists |
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- Enkephalinase inhibitors: Amastatin
- BL-2401
- Candoxatril
- D -Phenylalanine
- Dexecadotril (retorphan)
- Ecadotril (sinorphan)
- Kelatorphan
- Racecadotril (acetorphan)
- RB-101
- RB-120
- RB-3007
- Opiorphan
- Selank
- Semax
- Spinorphin
- Thiorphan
- Tynorphin
- Ubenimex (bestatin)
- Propeptides: β-Lipotropin (proendorphin)
- Prodynorphin
- Proenkephalin
- Pronociceptin
- Proopiomelanocortin (POMC)
- Others: Kyotorphin (met-enkephalin releaser/degradation stabilizer)
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