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The novel high-affinity antagonist, galantide, blocks the galanin-mediated inhibition of glucose-induced insulin secretion.

作者信息

Lindskog S, Ahrén B, Land T, Langel U, Bartfai T

机构信息

Department of Pharmacology, Lund University, Sweden.

出版信息

Eur J Pharmacol. 1992 Jan 14;210(2):183-8. doi: 10.1016/0014-2999(92)90669-u.

DOI:10.1016/0014-2999(92)90669-u
PMID:1376272
Abstract

This study describes the synthesis and effects of the first antagonist to the widely distributed neuropeptide, galanin, which inhibits the secretion of insulin. The first galanin antagonist is a 20-amino acid-long chimeric peptide of the composition galanin-(1-12)-Pro-substance P-(5-11) amide: Gly-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-Gln-Gln-Phe-Phe-Gly- Leu-Met amide. The peptide dose dependently (IC50 = 1.0 nM) antagonizes the galanin-mediated inhibition of the glucose-induced insulin secretion from mouse pancreatic islets. The antagonist was also found to displace 125I-monoiodo-[Tyr26]galanin from membranes of the insulin producing Rin m 5F cells with an IC50 value of less than 0.1 nM. The antagonist is named galantide.

摘要

相似文献

1
The novel high-affinity antagonist, galantide, blocks the galanin-mediated inhibition of glucose-induced insulin secretion.
Eur J Pharmacol. 1992 Jan 14;210(2):183-8. doi: 10.1016/0014-2999(92)90669-u.
2
Blockade of galanin-induced inhibition of insulin secretion from isolated mouse islets by the non-methionine containing antagonist M35.不含甲硫氨酸的拮抗剂M35对甘丙肽诱导的分离小鼠胰岛胰岛素分泌抑制作用的阻断。
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N-terminally elongated fragments of galanin(1-16) inhibit insulin secretion from isolated mouse islets.甘丙肽（1-16）的N端延长片段抑制分离的小鼠胰岛分泌胰岛素。
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Proc Natl Acad Sci U S A. 1991 Dec 15;88(24):11435-9. doi: 10.1073/pnas.88.24.11435.

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Galanin type 1 receptor knockout mice show altered responses to high-fat diet and glucose challenge.
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Galanin receptor-mediated inhibition of glutamate release in the arcuate nucleus of the hypothalamus.甘丙肽受体介导的对下丘脑弓状核中谷氨酸释放的抑制作用。
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Galanin-acetylcholine interactions in rodent memory tasks and Alzheimer's disease.甘丙肽与乙酰胆碱在啮齿动物记忆任务及阿尔茨海默病中的相互作用。
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