Ethyl β-carboline-3-carboxylate is a polyaromatic small molecule isolable from human urine extracts, demonstrating anxiogenic effects as a partial inverse agonist of benzodiazepine activity at the GABAA receptors. β-carboline derivatives with a 3-position carbonyl functionality have demonstrated induction of convulsions and anxiogenesis comparable to the effects associated with cerebral electrolytic lesions. Ethyl β-carboline-3-carboxylate demonstrates displacement of diazepam from the benzodiazepine binding site.