Oleamide

Oleamide is an amide of oleic acid (Item No. 90260) and an agonist of cannabinoid 1 (CB₁) receptors (K_i = 8.13 µM in a radioligand binding assay).¹ It is selective for CB₁ over CB₂ receptors, where it inhibits binding of the CB receptor full agonist CP 55,940 by only 42.5% in HEK-293T cells expressing human CB₂ receptors when used at a concentration of 100 µM. Oleamide (10 µM) inhibits cAMP accumulation induced by forskolin (Item No. 11018) in N1E 115 mouse neuroblastoma cells, an effect that is reversed by the CB₁ antagonist SR141716A. Oleamide was first identified in the cerebrospinal fluid of sleep-deprived cats, and it has also been detected in the cerebrospinal fluid of rats and humans.² In rats, it induces physiological sleep when administered at doses ranging from 5 to 50 mg and increases food intake when administered into the nucleus accumbens shell, and in group-housed and socially isolated mice, it has anxiolytic-like effects.^2,3,4 Oleamide also induces transactivation of PPARα, PPARβ, and PPARγ and inhibits activity of the sarco/endoplasmic reticulum Ca²⁺-ATPase (SERCA) at concentrations in the low micromolar range.⁵

WARNING This product is not for human or veterinary use.

1. Leggett, J.D., Aspley, S., Beckett, S.R., et al. Oleamide is a selective endogenous agonist of rat and human CB₁ cannabinoid receptors. Br. J. Pharmacol. 141(2), 253-262 (2004).

2. Cravatt, B.F., Prospero-Garcia, O., Siuzdak, G., et al. Chemical characterization of a family of brain lipids that induce sleep. Science 268(5216), 1506-1509 (1995).

3. Soria-Gómez, E., Márquez-Diosdado, M.I., Montes-Rodríguez, C.J., et al. Oleamide administered into the nucleus accumbens shell regulates feeding behaviour via CB₁ and 5-HT_2C receptors. Int. J. Neuropsychopharmacol. 13(9), 1247-1254 (2010).

4. Wei, X.Y., Yang, J.Y., Dong, Y.X., et al. Anxiolytic-like effects of oleamide in group-housed and socially isolated mice. Prog. Neuropsychopharmacol. Biol. Psychiatry 31(6), 1189-1195 (2007).

5. Yamamaoto, S., Takehara, M., and Ushimaru, M. Inhibitory action of linoleamide and oleamide toward sarco/endoplasmic reticulum Ca²⁺-ATPase. Biochim. Biophys. Acta 1861(1 Pt A), 3399-3405 (2016).