非选择性和选择性阿片受体拮抗剂对乙酰氨基酚镇痛作用的影响[第三部分]
Effect of nonselective and selective opioid receptors antagonists on antinociceptive action of acetaminophen [part III].
作者信息
Bujalska M
机构信息
Department of Pharmacodynamics, Medical University of Warszawa, Krakowskie Przedmieście 26/28, PL 00-927 Warszawa, Poland.
出版信息
Pol J Pharmacol. 2004 Sep-Oct;56(5):539-45.
The influence of naloxone (NAL), a competitive antagonist of mu, kappa, delta and sigma receptors; D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH(2) (CTOP), selective antagonist of mu-opioid receptors; nor-binaltorphimine (NOR-BNI), a potent and higly selective kappa opioid receptor antagonist; naltrindole (NTI), a delta-opioid receptor antagonist and naltriben (NTB), a highly selective delta(2)-opioid receptor antagonist on antinociceptive action of acetaminophen (ACETA) was studied in rats. NAL administered intraperitoneally (ip) or intracerebroventricularly (icv), and CTOP and NOR-BNI administered icv, markedly decreased the antinociceptive activity of the high dose of ACETA (400 mg/kg). Pretreatment with NTI (sc), as well as with naloxone (it), and NTB (it) slightly but significantly attenuated the ACETA antinociception. The possible involvement of the opioidergic systems in antinociceptive activity of ACETA is discussed.
研究了纳洛酮（NAL），一种μ、κ、δ和σ受体的竞争性拮抗剂；D-苯丙氨酸-半胱氨酸-酪氨酸-D-色氨酸-鸟氨酸-苏氨酸-苯丙氨酸-苏氨酸-NH(2)（CTOP），μ阿片受体的选择性拮抗剂；去甲二氢吗啡酮（NOR-BNI），一种强效且高度选择性的κ阿片受体拮抗剂；纳曲吲哚（NTI），一种δ阿片受体拮抗剂以及纳曲苄（NTB），一种高度选择性的δ(2)阿片受体拮抗剂对大鼠对乙酰氨基酚（ACETA）镇痛作用的影响。腹腔注射（ip）或脑室内注射（icv）纳洛酮，以及脑室内注射CTOP和NOR-BNI，均显著降低了高剂量（400 mg/kg）ACETA的镇痛活性。皮下注射NTI以及腹腔注射纳洛酮和NTB进行预处理，可轻微但显著减弱ACETA的镇痛作用。文中讨论了阿片能系统在ACETA镇痛活性中可能的参与情况。
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