Effect of nonselective and selective opioid receptors antagonists on antinociceptive action of acetaminophen [part III].

Polish journal of pharmacology Pub Date : 2004-09-01
M Bujalska
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Abstract

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.

非选择性和选择性阿片受体拮抗剂对对乙酰氨基酚抗痛觉作用的影响[第三部分]。
纳洛酮(NAL)对mu、kappa、delta和sigma受体的竞争性拮抗剂的影响;d - ph - cys - tyr - d - trp - orn - thr - pen - thr - nh (2) (CTOP),选择性阿片受体拮抗剂;一种强效、高选择性的阿片受体拮抗剂——非甲萘啡胺(NOR-BNI);研究了高选择性阿片受体拮抗剂纳曲多(NTI)和高选择性阿片受体拮抗剂纳曲本(NTB)对对乙酰氨基酚(ACETA)的抗伤害作用。腹腔(ip)或脑室(icv)给药NAL, CTOP和no - bni给药icv,显著降低了高剂量ACETA (400 mg/kg)的抗痛觉活性。NTI (sc)、纳洛酮(it)和NTB (it)预处理对ACETA的抗痛感有轻微但显著的减弱作用。讨论了阿片能系统可能参与乙酰乙酯的抗痛觉活性。
本文章由计算机程序翻译,如有差异,请以英文原文为准。
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