Turkish Journal of Medical Sciences

Abstract: The aim of this study was to investigate the effects of 3-benzoyl-1-methyl-4-phenyl-4-piperidinol-hydrochloride (C1), which is a structural and also non-classical isomer of bis Mannich base, bis (3-aryl-3-oxo-propyl) methylamine hydrochlorides (B1), on cyclooxygenase (COX) activities in 48 rats with inflammation by using carrageenan-induced paw edema, and to compare its effect with other non-steroidal anti-inflammatory drugs (NSAIDs). Materials and methods: Experimental animals were supplied by the Center of Experimental Research and Practice in Ataturk University. The animals were housed and fed in the laboratory (normal room temparature, food and water) under standard conditions. Rats were randomly assigned to eight groups (n = 6); control, intact, indomethacin, nimesulide, rofecoxib, C1 (50 mg), C1 (100 mg), and C1(200 mg). Results: C1 significantly inhibited COX-1 (P < 0.01 for all) and COX-2 (P < 0.01 for all) activities at the doses of 50, 100, and 200 mg kg^-1 when compared to control group. The inhibitory effect of C1 on COX-1 and COX-2 activities at all doses was similar to those of nimesulide. While C1 at 200 mg kg^-1 significantly inhibited COX-1 and COX-2 activities (P < 0.01 for both), at C1 100 mg kg^-1 significantly inhibited only COX-1 activity in comparison to rofecoxib (P < 0.05). Inhibitory effects of C1 on COX-1 activity at the doses of 50 and 100 mg kg^-1 were significantly weaker when compared to indomethacin (P < 0.01 and P < 0.05, respectively). Conclusion: It may be claimed that C1 has an anti-inflammatory effect, and its COX-2 selectivity is stronger than indomethacin and nimesulide but weaker than rofecoxib.

Key words: 3-benzoyl-1-methyl-4-phenyl-4-piperidinol-hydrochloride, COX enzymes, inflammation