THERAPEUTIC AND SCREENING METHODS EMPLOYING PARTIAL AGONISM OF THE∝-2A ADRENERGIC RECEPTOR SUBTYPE

摘要

Methods employing partial agonism of the alpha-2A adrenergic receptor ((alpha2A-AR) subtype in the treatment of attention deficit disorder (ADD), cognition enhancement, suppression of epilepsy, and protection against depression. The methods include the steps of administering a therapeutically effective amount of a weak partial agonist of the alpha 2A-adrenergic receptor subtype to the subject, wherein the weak partial agonist is selective for the alpha 2A-adrenergic receptor subtype; and treating the condition in the subject through the administering, wherein the treating occurs without evoking sedation in the subject. A method for identifying a selective, weak partial agonist for the alpha 2A-adrenergic receptor subtype is also disclosed. The method includes the steps of contacting the alpha 2A-adrenergic receptor subtype with a candidate compound; measuring a binding specificity, an activity level, or combination thereof of the alpha 2A adrenergic receptor subtype after the contacting; and determining that the candidate compound is a selective, weak partial agonist for the alpha 2A-adrenergic receptor subtype based on the measured binding specificity, activity level, or combination thereof.