Imidazoline RX871024 raises diacylglycerol levels in rat pancreatic islets.
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.
Karolinska Institutet, Rolf Luft Center for Diabetes Research, Department of Molecular Medicine, Karolinska Hospital, Stockholm, S-171 76, Sweden.
A M
AM
Efanov
S V
SV
Zaitsev
P O
PO
Berggren
H J
HJ
Mest
S
S
Efendic
D000818:Animals; D001952:Bridged-Ring Compounds / Q000494:pharmacology; D002217:Carbachol / Q000494:pharmacology; D002478:Cells, Cultured; D004075:Diglycerides / Q000096:biosynthesis*; D004357:Drug Synergism; D007093:Imidazoles / Q000494:pharmacology*; D007211:Indoles / Q000494:pharmacology*; D007328:Insulin / Q000378:metabolism; D000078790:Insulin Secretion; D007515:Islets of Langerhans / Q000187:drug effects / Q000378:metabolism*; D009636:Norbornanes; D010726:Phosphodiesterase Inhibitors / Q000494:pharmacology; D051381:Rats; D017208:Rats, Wistar; D013859:Thiocarbamates; D013871:Thiones / Q000494:pharmacology
C101943:2-(2-imidazolin-2-yl)-1-phenyl-1H-indole; D001952:Bridged-Ring Compounds; D004075:Diglycerides; D007093:Imidazoles; D007211:Indoles; D007328:Insulin; D009636:Norbornanes; D010726:Phosphodiesterase Inhibitors; D013859:Thiocarbamates; D013871:Thiones; C046498:tricyclodecane-9-yl-xanthogenate; D002217:Carbachol