期刊
JOURNAL OF PAIN
卷 11, 期 1, 页码 71-78出版社
CHURCHILL LIVINGSTONE
DOI: 10.1016/j.jpain.2009.08.001
关键词
alpha(2)-adrenoceptor agonist; antinociception; morphine; imidazolidine
资金
- Conselho Nacional de Desenvolvimento Cientifico e Tecnologic (CNPq, BR)
- Coordenacao de Aperfeicoamento de Pessoal de Nivel Superior (CAPES, BR)
- Fundacao Universitaria Jose Bonifacio (FUJB, BR)
- Fundacao Carlos Chagas Filho de Amparo a Pesquisa do Estado do Rio de Janeiro (FAPERJ, BR)
- Instituto do Milenio: Inovacao e Desenvolvimento de Farmacos e Medicamentos - IM-INOFAR
Finding new chemicals or adjuvants with analgesic effects in the central nervous system is clinically relevant due to the limited number of drugs with these properties. Here, we present PT-31, which is chemically related to 3-benzyl-imidazolidine, with an analgesic profile that results from alpha(2)-adrenoceptor activation. Intraperitoneal administration of PT-31 dose-dependently produced antinociception in the hot plate test, and interacted synergistically with morphine. This effect was completely reversed by yohimbine, a non-selective antagonist of alpha(2)-adrenoceptors, and by BRL 44408, a selective alpha(2A)-adrenoceptor antagonist. The combination of morphine and PT-31 produced greater antinociceptive activity than either alone, and isobolographic analysis revealed a synergistic interaction between these compounds. Docking results confirm the high affinity of the PT-31 ligand at the alpha(2A)-adrenoceptor. Perspective: This study introduces a new analgesic compound (PT-31) that acts via alpha(2A)-adrenoceptor activation. A significant increase in analgesia was observed when co-administered with morphine. PT-31 is an interesting new substance for pain therapy. (C) 2010 by the American Pain Society
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