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Apronalide is a hypnotic and sedative drug of the ureide (acylurea) group. It was first synthesized in 1926 by Hoffmann-La Roche. Structurally, it is an acyclic analog of barbiturates (N-acylurea), sharing similar but milder pharmacological effects compared to barbiturates. Apronalide acts as a positive allosteric modulator of the GABAA receptor, enhancing inhibitory neurotransmission in the central nervous system and producing sedative-hypnotic effects. It was formerly used as a daytime sedative and for mild to moderate pain relief (including headache) but was withdrawn from most markets after being linked to thrombocytopenic purpura and other adverse effects. Apronalide remains approved only in Japan, where it is sometimes used in combination with caffeine and ibuprofen for headache treatment.
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