NPY Y2 antagonist 2 is a modulator targeting the neuropeptide Y (NPY) receptor Y2 , with pK i values of 6.8 nM and 7.2 nM in human and rat brains, respectively, and demonstrating blood-brain barrier penetration . NPY Y2 antagonist 2 shows selectivity for the Y1 and Y5 receptors . NPY Y2 antagonist 2 blocks the negative feedback regulation mediated by the NPY Y2 receptor , thereby increasing endogenous NPY release and enhancing Y1 receptor activation, resulting in the modulation of central neurotransmitter release. NPY Y2 antagonist 2 exhibits moderate in vivo clearance, high free fraction in rat brain, and a favorable brain/plasma ratio and brain exposure. NPY Y2 antagonist 2 is applicable for research in conditions such as mood disorders, anxiety induced by alcohol withdrawal, and social anxiety associated with nicotine withdrawal.
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