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Captodiame, also known as captodiamine, is an antihistamine and a derivative of diphenhydramine used primarily as a sedative and anxiolytic. It has been suggested for use in preventing benzodiazepine withdrawal syndrome. Captodiame acts through multiple mechanisms: it is an antagonist at the 5-hydroxytryptamine (serotonin) receptor 2C (5-HT2C), and an agonist at both the sigma non-opioid intracellular receptor 1 (sigma-1) and dopamine D3 receptors. These actions contribute to its sedative, anxiolytic, and potential antidepressant effects. Captodiame is unique among similar agents in that it increases brain-derived neurotrophic factor (BDNF) levels specifically in the hypothalamus, which may relate to its ability to attenuate stress-induced anhedonia and corticotropin-releasing factor signaling[1][2][3][4][5][6].
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