咪唑啉RX871024可提高大鼠胰岛中的二酰甘油水平。

Imidazoline RX871024 raises diacylglycerol levels in rat pancreatic islets.

作者信息

Efanov A M, Zaitsev S V, Berggren P O, Mest H J, Efendic S

机构信息

Karolinska Institutet, Rolf Luft Center for Diabetes Research, Department of Molecular Medicine, Karolinska Hospital, Stockholm, S-171 76, Sweden.

出版信息

Biochem Biophys Res Commun. 2001 Mar;281(5):1070-3. doi: 10.1006/bbrc.2001.4483.

DOI:10.1006/bbrc.2001.4483

PMID:11243843

Abstract

Imidazoline compound RX871024 and carbamylcholine (CCh) stimulate insulin secretion in isolated rat pancreatic islets. Combination of CCh and RX871024 induces a synergetic effect on insulin secretion. RX871024 and CCh produce twofold increases in diacylglycerol (DAG) concentration. The combination of two compounds has an additive effect on DAG concentration. Effects of RX871024 on insulin secretion and DAG concentration are not dependent on the presence of D609, an inhibitor of phosphatidylcholine-specific phospholipase C. It is concluded that as in case with CCh the increase in DAG concentration induced by imidazoline RX871024 contributes to the insulinotropic activity of the compound.

摘要

咪唑啉化合物RX871024和氨甲酰胆碱（CCh）可刺激离体大鼠胰岛分泌胰岛素。CCh与RX871024联合使用对胰岛素分泌具有协同作用。RX871024和CCh可使二酰甘油（DAG）浓度增加两倍。两种化合物联合使用对DAG浓度具有相加作用。RX871024对胰岛素分泌和DAG浓度的影响不依赖于磷脂酰胆碱特异性磷脂酶C抑制剂D609的存在。得出的结论是，与CCh的情况一样，咪唑啉RX871024诱导的DAG浓度增加有助于该化合物的促胰岛素活性。