FMS586 free base is a selective neuropeptide Y Y5 receptor antagonist with oral activity. FMS586 can completely block the significant increase in adrenocorticotropic hormone (ACTH) and cortisol caused by the Y(5) selective agonist hPP. FMS586 also reversed the significant upregulation of adrenocorticotropic hormone (CRF) and antidiuretic hormone (AVP) mRNA expression induced by central injection of hPP. FMS586 provides the first evidence that selective stimulation of Y(5) receptors triggers activation of the HPA axis.
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