Methyl arachidonate

Methyl arachidonate is a protein kinase C activator as well as an orally active substrate that undergoes esterase-mediated hydrolysis. Methyl arachidonate indirectly activates protein kinase C via eicosanoid metabolites generated through the arachidonic acid metabolic pathway, exerting effects via cyclooxygenase products at low concentrations and via lipoxygenase products at high concentrations. Methyl arachidonate can be used in studies related to lipodystrophy^[2]. In Vitro:Methyl arachidonate (50 μM; 5 min) is poorly active in activating purified rat brain protein kinase C in a phosphatidylserine- and calcium-free in vitro assay, inducing less than 20% of maximal activation^[1].
Methyl arachidonate (1-500 μM; 10 s-3 min) potently activates protein kinase C in intact human platelets in vitro in a concentration- and time-dependent manner, with maximal activation (101.0% of TPA control) at 500 μM for 1 min, and activation is mediated by eicosanoid metabolites, as shown by inhibition by cyclooxygenase and lipoxygenase inhibitors^[1]. In Vivo:Methyl arachidonate (14-42 mg; p.o.; daily/every 2nd day/every 4th day; 35 days) is twice as potent as methyl linoleate at promoting weight gain in fat-deficient rats, with 14 mg every 2nd day producing equivalent weight gain to 14 mg daily of methyl linoleate, but shows no superiority over methyl linoleate in curing associated skin lesions^[2].