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The arginine vasopressin V1b receptor is a G protein-coupled receptor encoded by the AVPR1B gene, principally located in pituitary corticotrophs and various brain regions[1][7]. It binds the neurohypophyseal peptide arginine vasopressin (AVP), mediating its central role in regulating the HPA axis—specifically, facilitating the release of ACTH from the anterior pituitary upon AVP stimulation[1][5][7]. AVPR1B signaling is crucial for the physiological stress response, metabolic homeostasis (water, glucose, salt balance), and various neuroendocrine pathways[1][4]. Clinical and preclinical studies have implicated AVPR1B antagonists as promising therapeutic agents in depression and anxiety, particularly for patients exhibiting HPA axis dysregulation[2][4]. AVPR1B is also notably expressed in certain endocrine and neuroendocrine tumors (e.g., ACTH-secreting adenomas)[1]. Its pharmacology is characterized by both peptide and non-peptide agonists/antagonists, with ongoing drug development for neuropsychiatric and hormonal disorders[8].
Antagonism of AVPR1B inhibits HPA axis overactivity, reducing ACTH secretion and downstream cortisol release (useful in depression and anxiety) Agonists stimulate ACTH release via pituitary interaction
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