M-15 - HIGH-AFFINITY CHIMERIC PEPTIDE THAT BLOCKS THE NEURONAL ACTIONS OF GALANIN IN THE HIPPOCAMPUS, LOCUS-CERULEUS, AND SPINAL-CORD

被引：166
作者：
BARTFAI, T
BEDECS, K
LAND, T
LANGEL, U
BERTORELLI, R
GIROTTI, P
CONSOLO, S
XU, XJ
WIESENFELDHALLIN, Z
NILSSON, S
PIERIBONE, VA
HOKFELT, T
机构：
[1] MARIO NEGRI INST PHARMACOL RES,I-20157 MILAN,ITALY
[2] KAROLINSKA INST,DEPT CLIN PHYSIOL,CLIN NEUROPHYSIOL SECT,S-14186 HUDDINGE,SWEDEN
[3] KAROLINSKA INST,DEPT HISTOL & NEUROBIOL,S-10401 STOCKHOLM 60,SWEDEN
来源：
PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA | 1991年 / 88卷 / 23期
关键词：
INHIBITORY NEUROPEPTIDE; ANTAGONIST; RELEASE; RECEPTOR; NOCICEPTIVE REFLEX;
D O I：
10.1073/pnas.88.23.10961
中图分类号：
O [数理科学和化学]; P [天文学、地球科学]; Q [生物科学]; N [自然科学总论];
学科分类号：
07 ; 0710 ; 09 ;
摘要：
The 20-amino acid peptide M-15 binds with high affinity (IC50 almost-equal-to 0.1 nM) to I-125-labeled galanin (I-125-GAL) binding sites in membranes from the ventral hippocampus, midbrain, and rat spinal cord. Receptor autoradiographic studies show that M-15 can displace I-125-GAL from all labeled sites. M-15 acts as a reversible high-affinity antagonist in blocking the inhibitory effects of GAL on the evoked release of acetylcholine in vivo in the hippocampus and on the GAL-induced hyperpolarization of locus coeruleus neurons in slices. M-15 also blocks the facilitatory effects of GAL on the spinal flexor reflex. Thus, the chimeric peptide M-15 [GAL-(1-13)-substance P-(5-11) amide] represents the first antagonist to the neuronal actions of GAL.
引用
收藏
页码：10961 / 10965
页数：5
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