Inhibition of the effects of thrombin on guinea pig platelets by the diacylglycerol lipase inhibitor RHC 80267

Journal Article · Wed Oct 01 00:00:00 EDT 1986 · Thromb. Res.; (United States)

DOI:https://doi.org/10.1016/0049-3848(86)90182-9· OSTI ID:6840277

Amin, D; Sutherland, C A; Khandwala, A S; Jamall, I S; Kapoor, A L

Phospholipase C (PLC) and diacylglycerol lipase (DGL) activities were found in guinea pig platelet microsome preparations. No phospholipase A2 (PLA2) activity was detected. RHC 80267 (1,6-di (0-(carbamoyl) cyclohexanone oxime)hexane) inhibited DGL activity (IC50 = 4 uM) from guinea pig platelet microsomes but had no effect on PLC. RHC 80267 inhibited platelet aggregation (IC50 = 11 uM), release of arachidonic acid (AA), its metabolites, and ATP (IC50 = 4.5 uM) when guinea pig platelets were challenged with a low concentration of thrombin. We propose that PLC-DGL is an important enzymatic pathway for the release of AA in guinea pig platelets.

• Research Organization: St. John's Univ., Jamaica, NY
• OSTI ID: 6840277
• Journal Information: Thromb. Res.; (United States), Journal Name: Thromb. Res.; (United States) Vol. 1; ISSN THBRA
• Country of Publication: United States
• Language: English

Related Subjects

560300* -- Chemicals Metabolism & Toxicology
63 RADIATION, THERMAL, AND OTHER ENVIRON. POLLUTANT EFFECTS ON LIVING ORGS. AND BIOL. MAT.
ALKANES
ANIMALS
BIOLOGICAL EFFECTS
BIOLOGICAL MATERIALS
BLOOD
BLOOD CELLS
BLOOD PLATELETS
BODY FLUIDS
CARBOXYLESTERASES
CELL CONSTITUENTS
COAGULANTS
DRUGS
ENZYME INHIBITORS
ENZYMES
ESTERASES
GUINEA PIGS
HEMATOLOGIC AGENTS
HEMOSTATICS
HEXANE
HYDROCARBONS
HYDROLASES
INHIBITION
LIPASE
MAMMALS
MATERIALS
MICROSOMES
ORGANIC COMPOUNDS
ORGANOIDS
PEPTIDE HYDROLASES
RODENTS
SERINE PROTEINASES
THROMBIN
VERTEBRATES