Amauromine (CAS: 88360-87-6)

Amauromine is a fungal-derived diketopiperazine alkaloid originally isolated from Amauroascus sp. as a vasodilatory compound with low acute toxicity in mice. Structural characterization established the molecular formula C32H36N4O2. Subsequent studies revealed that amauromine acts as a cannabinoid receptor antagonist, inhibiting CB1 receptors (Ki = 0.178 µM) and exhibiting antagonistic activity at the orphan receptor GPR18 (IC50 = 3.74 µM), thereby identifying it as a bioactive GPCR modulator. Related diketopiperazine analogues isolated from Aspergillus terreus showed α-glucosidase inhibitory activity, further supporting the pharmacological relevance of this structural class. These data establish amauromine as a multifunctional fungal alkaloid with vasodilatory and receptor-modulating properties and potential utility as a lead structure for GPCR-targeted research.