STRUCTURE-ANTINOCICEPTIVE ACTIVITY OF NEUROTENSIN AND SOME NOVEL ANALOGS IN THE PERIAQUEDUCTAL GRAY REGION OF THE BRAIN-STEM

被引:81
作者
ALRODHAN, NRF
RICHELSON, E
GILBERT, JA
MCCORMICK, DJ
KANBA, KS
PFENNING, MA
NELSON, A
LARSON, EW
YAKSH, TL
机构
[1] TOKYO WOMENS MED COLL,DEPT PSYCHIAT,TOKYO 162,JAPAN
[2] MAYO CLIN & MAYO FDN,DEPT PSYCHIAT & PHARMACOL,ROCHESTER,MN 55905
[3] MAYO CLIN & MAYO FDN,DEPT BIOCHEM & MOLEC BIOL,ROCHESTER,MN 55905
[4] MAYO CLIN & MAYO GRAD SCH MED,ROCHESTER,MN 55901
[5] UNIV CALIF SAN DIEGO,DEPT ANESTHESIA,LA JOLLA,CA 92093
关键词
NEUROTENSIN; NEUROTENSIN RECEPTOR; STRUCTURE-ACTIVITY RELATIONSHIP; PAIN; ANTINOCICEPTION; PERIAQUEDUCTAL GRAY;
D O I
10.1016/0006-8993(91)90139-M
中图分类号
Q189 [神经科学];
学科分类号
071006 ;
摘要
Neurotensin, an endogenous tridecapeptide, produces a potent, naloxone-insensitive antinociceptive response when it is microinjected into the periaqueductal gray region of the rat brainstem. In the present study, the ED50 for neurotensin in inducing antinociception was 1.5 nmol, two times more potent than morphine. We sought to find whether neurotensin's antinociception effects were mediated by the same receptor that mediates its other functions. We found that the structure-activity relationship of neurotensin-induced antinociception was different from that required for the stimulation of intracellular cyclic GMP production in neuroblastoma clone N1E-115 and the binding to N1E-115 cells, human brain tissue, or rat periaqueductal gray. These data suggest there exists a subtype of neurotensin receptors in neural tissue that mediates its antinociceptive actions.
引用
收藏
页码:227 / 235
页数:9
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