Description
Amauromine is a neutral antagonist of the cannabinoid (CB) receptor CB
1 that is selective for CB
1 (K
i = 178 nM; K
b = 66.6 nM) over CB
2, with no activity at CB
2 receptors at concentrations up to 10 μM. It is also an antagonist of GPR18 (IC
50 = 3.74 μM). Amauromine has vasodilatory activity.
References
[1] MAHMOUD FAHMI ELSEBAI. Identification of a Potent and Selective Cannabinoid CB1 Receptor Antagonist from Auxarthron reticulatum[J]. ACS Medicinal Chemistry Letters, 2011, 2 11: 866-869. DOI:
10.1021/ml200183z[2] MAMONA NAZIR. GPR18 Inhibiting Amauromine and the Novel Triterpene Glycoside Auxarthonoside from the Sponge-Derived Fungus Auxarthron reticulatum.[J]. Planta medica, 2015, 81 12-13: 1141-1145. DOI:
10.1055/s-0035-1545979[3] SHIGEHIRO TAKASE. Structure of amauromine, a new alkaloid with vasodilating activity produced by amauroascus sp.[J]. Tetrahedron Letters, 1984, 25 41: Pages 4673-4676. DOI:
10.1016/s0040-4039(01)91230-4
