Synthesis and analgesic activity evaluation of some agmatine derivatives.
A series of N,N'-disubstituted-2-nitroethene-1,1-diamine and N,N'-disubstituted- N''-cyanoguanidine derivatives were prepared and evaluated for in vivo analgesic activity. The blood brain barrier (BBB) VolSurf model was used to predict the BBB permeation profiles of our synthesized compounds. Some compounds show both remarkable analgesic activity and good BBB permeation profiles, and these compounds might be developed for treatment of opioid tolerance and dependence.
He
Hongxia
H
School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, 110016, P.R. China. zbzheng@nic.bmi.ac.cn.
Liu
Mengjia
M
Zheng
Zhibing
Z
Liu
Ying
Y
Xiao
Junhai
J
Su
Ruibin
R
Hu
Chun
C
Li
Jin
J
Li
Song
S
D000376:Agmatine / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D000700:Analgesics / Q000138:chemical synthesis* / Q000493:pharmacokinetics / Q000494:pharmacology*; D000701:Analgesics, Opioid / Q000493:pharmacokinetics; D000818:Animals; D001693:Biological Transport, Active; D001812:Blood-Brain Barrier / Q000378:metabolism; D005260:Female; D008297:Male; D051379:Mice; D010539:Permeability
D000700:Analgesics; D000701:Analgesics, Opioid; D000376:Agmatine