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Lismedetomidine (HS-10381) is a small molecule prodrug of dexmedetomidine, a selective alpha-2 adrenergic receptor agonist. Developed by Hansoh Pharmaceutical, it is primarily formulated as a transdermal patch for the treatment of Alzheimer's disease and related cognitive impairments. As a prodrug, lismedetomidine is an L-lysine conjugate of dexmedetomidine that is converted in vivo to the active moiety. Dexmedetomidine acts on alpha-2 adrenergic receptors in the central nervous system to modulate the release of norepinephrine and other neurotransmitters. In the context of neurodegenerative diseases, alpha-2 agonists are investigated for their potential to manage neuropsychiatric symptoms such as agitation, aggression, and sleep disturbances, and may also possess neuroprotective properties. The transdermal delivery system is designed to provide stable plasma concentrations over an extended period, potentially improving tolerability and patient compliance compared to traditional systemic administration.
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