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Horm Metab Res 2004; 36(4): 210-214
DOI: 10.1055/s-2004-814449
Original Basic
© Georg Thieme Verlag Stuttgart · New York

Signals in the Activation of Opioid µ-Receptors by Loperamide to Enhance Glucose Uptake into Cultured C2C12 Cells

I.  M.  Liu1 , S.  S.  Liou1 , W.  C.  Chen2 , P.  F.  Chen3 , J.  T.  Cheng3
  • 1The Department of Pharmacy, Tajen Institute of Technology, Yen-Pou, Ping Tung Shien, Taiwan 90701, R.O.C.
  • 2The Department of Chinese Medicine, Jin-Ai Municipal Hospital, Taipei City, Taiwan 10501, R.O.C.
  • 3The Department of Pharmacology, College of Medicine, National Cheng Kung University, Tainan City, Taiwan, R.O.C.
Further Information

Publication History

Received 12 August 2003

Accepted without Revision 10 November 2003

Publication Date:
28 April 2004 (online)

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Abstract

In an attempt to understand the signal pathways of opioid µ-receptors for glucose metabolism, we used loperamide to investigate the glucose uptake into the myoblast C2C12 cells. Loperamide enhanced the uptake of radioactive deoxyglucose into C2C12 cells in a concentration-dependent manner that was abolished in cells pre-incubated with naloxone or naloxonazine at concentrations sufficient to block opioid µ-receptors. Pharmacological inhibition of phospholipase C (PLC) by U73122 resulted in a concentration-dependent decrease in loperamide-stimulated uptake of radioactive deoxyglucose into C2C12 cells. This inhibition of glucose uptake by U73122 was specific since the inactive congener, U73343, failed to modify loperamide-stimulated glucose uptake. Moreover, both chelerythrine and GF 109203X diminished the action of loperamide at concentrations sufficient to inhibit protein kinase C (PKC). The obtained data suggest that an activation of opioid µ-receptors in C2C12 cells by loperamide may increase glucose uptake via the PLC-PKC pathway.

Key words

C2C12 cells - Loperamide - Opioid µ-receptors - Phospholipase C - Protein kinase C

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Prof. J.-T. Cheng

Department of Pharmacology · College of Medicine · National Cheng Kung University

Tainan City · Taiwan 70101 · R.O.C.

Phone: +886(6)2372706

Fax: +886(6)2386548 ·

Email: jtcheng@mail.ncku.edu.tw