Journal of Medicinal Chemistry p. 674 - 676 (1980)
Update date:2022-08-02
Topics:
Pasternak, Gavril W.
Hahn, Elliot F.
Two new long-acting hydrazone derivatives of 14-hydroxydihydromorphinones have been synthesized, oxymorphazone and naltrexazone.Both derivatives show high affinity for opiate binding sites in vitro, similar to naloxazone, the hydrazone analogue of naloxone.Sodium and manganese shifts imply that naltrexazone, like naloxazone, is a pure antagonist.By contrast, oxymorphazone inhibition of receptor binding is dramatically reduced by sodium and potentiated by manganese, suggesting it is an agonist.When given in vivo, all agents produce a significant inhibition of receptor binding for over 24 h despite extensive washing of the brain homogenates.Oxymorphone, naltrexone, and naloxone are without effect.Twenty-four hours after in vivo administration of oxymorphazone, 82percent of mice are still analgetic compared to only 17percent of oxymorphone-treated mice (p < 0.005).Twenty-four hours after naltrexazone or naloxazone treatment all mice were protected from morphine analgesia (12 mg/kg; p < 0.005), while naltrexone- and naloxone-treated animals did not differ significantly from saline-treated controls.
View Morelianyungang jinkang pharmaceutical technology co., ltd.
Contact:008651885445517
Address:Jinshan industrial park, Ganyu county, Lianyungang, Jiangsu Province, 222115, China
website:http://www.vanzpharm.com/en/index.html
Contact:86-27-84492310
Address:FANHU INDUSTRY PARK
Contact:+86-512-69561895
Address:No.111, Building A4, 218 Xinghu Street, Suzhou Industrial Park, P. R. China
Guangzhou Swan Chemical Co., Ltd.
Contact:+86-20-31075659
Address:NO.301, Hong ba fang investment BLDG 1,Guan chong village,Shiqi town,Panyu district,Guangzhou
Nantong Baokai Chemical Co., Ltd (Hangzhou Baokai Bio-Chemicals Co.,Ltd.)
Contact:+86-513-83886111
Address:No. 68 Suzhou road ,Binjiang Fine Chemical Industrial Park , Beixin town, Qidong city ,Jiangsu province
Doi:10.1039/jr9500000188
(1950)Doi:10.1016/j.tetlet.2011.03.117
(2011)Doi:10.1007/BF00696962
(1995)Doi:10.7164/antibiotics.53.1257
(2000)Doi:10.1021/jm501241g
(2014)Doi:10.1021/jo01305a037
(1980)