Godfrey Lisa, Yan Luo, Clarke Geoffrey D, Ledent Catherine, Kitchen Ian, Hourani Susanna M O
Pharmacology Group, School of Biomedical and Molecular Sciences, University of Surrey, Guildford, Surrey GU2 7XH, UK.
Eur J Pharmacol. 2006 Feb 15;531(1-3):80-6. doi: 10.1016/j.ejphar.2005.12.004. Epub 2006 Jan 30.
This study investigated the involvement of adenosine receptors in the interaction between paracetamol and caffeine in mice, using the adenosine A2A receptor antagonist 5-amino-7-(2-phenylethyl)-2-(2-furyl)pyrazolo[4,3-e]-1,2,4-triazolo[1,5-c]pyrimidine (SCH58261) and the adenosine A2B receptor antagonist 1-propyl-8-p-sulfophenylxanthine (PSB1115), in the tail immersion and hot-plate tests. Paracetamol (10-200 mg/kg) was antinociceptive in both tests, but, in contrast to previous studies, caffeine (10 mg/kg) was pronociceptive in the tail immersion test, and reduced the effects of paracetamol in both tests. SCH58261 (3 mg/kg) was antinociceptive in both tests and in its presence paracetamol (50 mg/kg) had no further effect. PSB1115 (10 mg/kg) had little effect alone but potentiated the effect of paracetamol (50 mg/kg) in the hot-plate test and abolished it in the tail immersion test. These results suggest that adenosine A2B receptors may be involved in the action of paracetamol in a pathway-dependent manner, and also support the existence of pronociceptive adenosine A2A receptors.
本研究利用腺苷A2A受体拮抗剂5-氨基-7-(2-苯乙基)-2-(2-呋喃基)吡唑并[4,3-e]-1,2,4-三唑并[1,5-c]嘧啶(SCH58261)和腺苷A2B受体拮抗剂1-丙基-8-对磺基苯基黄嘌呤(PSB1115),在小鼠的尾浸法和热板试验中,研究了腺苷受体在对乙酰氨基酚与咖啡因相互作用中的作用。对乙酰氨基酚(10 - 200 mg/kg)在两种试验中均具有镇痛作用,但与先前的研究不同,咖啡因(10 mg/kg)在尾浸法试验中具有促痛作用,并降低了对乙酰氨基酚在两种试验中的效果。SCH58261(3 mg/kg)在两种试验中均具有镇痛作用,在其存在的情况下,对乙酰氨基酚(50 mg/kg)没有进一步的作用。PSB1115(10 mg/kg)单独作用时作用很小,但在热板试验中增强了对乙酰氨基酚(50 mg/kg)的作用,在尾浸法试验中则消除了其作用。这些结果表明,腺苷A2B受体可能以途径依赖的方式参与对乙酰氨基酚的作用,也支持了促痛性腺苷A2A受体的存在。