title: [Synthesis and analgesic activities of phenyl piperazinyl aralkyl ketone derivatives].
abstract: To explore novel non-opioid analgesic agents, 16 compounds were synthesized and their structures were confirmed by 1H NMR and HR-MS. YX0611-1 was treated as the leading compound. The results of mice writhing model and hot plate model showed that compounds 2, 7, 8, 9, 11 and 15 had obvious analgesic activities in vivo. The test of affinity to mu, delta, kappa receptor displayed that active compounds didn't act on opioid receptor. The results of preliminary toxicity and pharmacokinetic tests showed that compound 7 had better safety and pharmacokinetic properties than that of YX0611-1, and it deserved further development.
authors: Novel Technology Center of Pharmaceutical Chemistry, Shanghai Institute of Pharmaceutical Industry, Shanghai 200437, China.
authors: Peng
authors: P
authors: Xie
authors: Guan
authors: G
authors: Wang
authors: Gui-Sen
authors: GS
authors: Zhang
authors: Li
authors: L
authors: Zhang
authors: Xiang-Qing
authors: XQ
authors: Xu
authors: Lin
authors: L
authors: Guo
authors: Jian-Qi
authors: JQ
authors: Li
mesh_terms: D018712:Analgesics, Non-Narcotic / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D000818:Animals; D005260:Female; D008297:Male; D051379:Mice; D010147:Pain Measurement; D010879:Piperazines / Q000138:chemical synthesis* / Q000737:chemistry / Q000493:pharmacokinetics / Q000494:pharmacology / Q000633:toxicity; D011897:Random Allocation; D011957:Receptors, Opioid / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D018712:Analgesics, Non-Narcotic; D010879:Piperazines; D011957:Receptors, Opioid