title: [Experimental study of the anti-inflammatory and analgesic effects of diethyl 1,3-dicyclohexyl- 1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate].
abstract: OBJECTIVE
  To study the anti-inflammatory and analgesic activities of diethyl 1,3-dicyclohexyl-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate (ZL-5010) in vivo and in vitro.
  
  
  METHODS
  The analgesic effect of ZL-5010 was evaluated by acetic acid-induced writhing response in mice, and the anti-inflammatory effects was assessed in mice with xylene-induced ear edema and in rats with carrageenan-induced paw edema. Mouse peritoneal exudate cells activated by bacterial lipopolysaccharides (LPS) were used to evaluate the anti-inflammatory effect of ZL-5010 in vitro. The levels of interleukin-1β (IL -1β) and tumor necrosis factor-α (TNF-α) in the cell culture supernatant were measured using enzyme-linked immunosorbent assay (ELISA).
  
  
  RESULTS
  At the doses of 0.25 and 0.5 mmol/kg, ZL-5010 administered by gavage once daily for 3 days significantly reduced acetic acid-induced writhing frequency and suppressed xylene-induced ear edema in mice, and alleviated paw edema induced by carrageenan in rats (P<0.05). The agent also inhibited the production of the pro-inflammatory cytokines IL-1β and TNF-α by LPS-induced mouse peritoneal exudate cells in vitro, with the statistically significant minimum effective concentrations of 10 and 20 µmol/L, respectively (P<0.05).
  
  
  CONCLUSIONS
  ZL-5010 administered by gavage has anti-inflammatory and analgesic effects in mice and rats, and in mouse peritoneal exudate cell cultures, the agent also inhibits the production of the pro-inflammatory cytokines IL-1β and TNF-α.
authors.affiliation: School of Pharmaceutical Sciences, Southern Medical University, Guangzhou 510515, China. zhangqun123456@126.com
authors.forename: Qun
authors.initials: Q
authors.lastname: Zhang
authors.forename: Guibao
authors.initials: G
authors.lastname: Zhou
authors.forename: Linsheng
authors.initials: L
authors.lastname: Lei
authors.forename: Chuanlin
authors.initials: C
authors.lastname: Yu
authors.forename: Nana
authors.initials: N
authors.lastname: Chen
mesh_terms: D000599:Amino Acids, Diamino / Q000494:pharmacology* / Q000627:therapeutic use; D000700:Analgesics / Q000494:pharmacology* / Q000627:therapeutic use; D000818:Animals; D000893:Anti-Inflammatory Agents / Q000494:pharmacology* / Q000627:therapeutic use; D003510:Cyclohexanes / Q000494:pharmacology* / Q000627:therapeutic use; D005260:Female; D053583:Interleukin-1beta / Q000378:metabolism; D008297:Male; D051379:Mice; D008815:Mice, Inbred Strains; D011743:Pyrimidines / Q000494:pharmacology* / Q000627:therapeutic use; D051381:Rats; D017207:Rats, Sprague-Dawley; D014409:Tumor Necrosis Factor-alpha / Q000378:metabolism
chemical_list: D000599:Amino Acids, Diamino; D000700:Analgesics; D000893:Anti-Inflammatory Agents; D003510:Cyclohexanes; D053583:Interleukin-1beta; D011743:Pyrimidines; D014409:Tumor Necrosis Factor-alpha; C581226:diethyl 1,3-dicyclohexyl-1,2,3,6-tetrahydropyrimidine-4,5-dicarboxylate