Journal of Medicinal Chemistry p. 3310 - 3316 (1991)
Update date:2022-09-26
Topics:
Compton
Prescott Jr.
Martin
Siegel
Gordon
Razdan
The primary goal of this research was to synthesize a series of ether analogues of the cannabinoid drug class and to evaluate their agonist and antagonist pharmacological properties in either the mouse or the rat. Agonist and antagonist activity was evaluated in mice using a multiple-evaluation procedure (locomotor activity, tail-flick latency, hypothermia, ring immobility) and activity in rats determined in a discriminative stimulus paradigm. Additionally, novel analogues were evaluated for their ability to bind to the THC receptor site labeled by 3H-CP-55,940. None of the cannabinoid analogues were capable of attenuating the effects of Δ9-THC (3 mg/kg) in either the rat (doses up to 10 mg/kg) or in the mouse (doses up to 30 mg/kg). It also appears that the compounds with minimal in vivo activity are not mixed agonist/antagonists. These data would suggest that the phenolic hydroxyl is important for receptor recognition (binding) and in vivo potency. Additionally, cannabinoid methyl ethers previously considered inactive have been found to produce limited activity. Lastly, data suggest that Δ9,11- THC is more potent than previous reports indicated, and does possess pharmacological activity.
View MoreContact:+86-511-88790000
Address:338 North Yushan Rd, Zhenjiang, Jiangsu 212016
Suzhou Wedo Chemicals Co., Ltd.
Contact:86 512 58100425
Address:Zonger Road, DongSha Industry Park , Zhangjiagang, Jiangsu, China
Shandong Hongxiang Zinc Co., Ltd
Contact:086-0311-66187879
Address:DaWang developing zone
Nanjing Chemlin Chemical Co., Ltd.
website:http://www.echemlin.cn
Contact:+86-25-83697070
Address:Rm.902 Longyin Plaza, No. 217 Zhongshan Rd.(N) Nanjing 210009,China
shijiazhuang baisheng chem co.; ltd
Contact:86-0311-80790826
Address:shijiazhuang hebei
Doi:10.1016/j.bbamem.2011.04.020
(2011)Doi:10.1021/ja00006a054
(1991)Doi:10.1039/c29700000650
(1970)Doi:10.1021/jacs.8b09851
(2018)Doi:10.1039/P19900002745
(1990)Doi:10.1016/s0020-1693(99)00133-4
(1999)