Michalska E, Malec D, Antkiewicz-Michaluk L
Department of Pharmacodynamics, Medical Academy, Lublin, Poland.
Pol J Pharmacol. 1994 Jan-Apr;46(1-2):43-9.
Naloxone (1 mg/kg ip) reduced analgesic effect of R-phenylisopropyladenosine (R-PIA-0.2 mg/kg sc) in hot plate and tail-immersion tests in mice and in tail-immersion test in rats. Also the effect of 2-chloroadenosine (2-CADO-2 mg/kg sc) was significantly reduced by naloxone in mice in both nociceptive tests. Naloxone induced partial reduction of analgesic effects of 5'-N-ethylcarboxamideadenosine (NECA-0.02-0.05 mg/kg sc) in mice and rats. Binding studies revealed that the affinity of adenosine agonists (R-PIA and NECA) to opioid receptors was about 5000 times weaker than the corresponding affinity of naloxone.
纳洛酮(1毫克/千克,腹腔注射)在小鼠的热板和尾浸试验以及大鼠的尾浸试验中,降低了R-苯异丙基腺苷(R-PIA-0.2毫克/千克,皮下注射)的镇痛效果。同样,在两种伤害性试验中,纳洛酮显著降低了2-氯腺苷(2-CADO-2毫克/千克,皮下注射)对小鼠的作用。纳洛酮使5'-N-乙基羧酰胺腺苷(NECA-0.02-0.05毫克/千克,皮下注射)对小鼠和大鼠的镇痛作用部分降低。结合研究表明,腺苷激动剂(R-PIA和NECA)对阿片受体的亲和力比纳洛酮相应的亲和力弱约5000倍。