VPAC2 receptor

Pituitary adenylyl cyclase-activating polypeptide receptor VPAC2 (VIPR2) is a class B G protein-coupled receptor that binds both vasoactive intestinal peptide (VIP) and pituitary adenylyl cyclase-activating polypeptide (PACAP) with high affinity and primarily activates adenylyl cyclase-dependent signaling pathways^[1]^[2]. VPAC2 participates in neuroendocrine regulation, circadian rhythm synchronization, immune modulation, and metabolic control through cAMP-mediated intracellular signaling cascades^[1]^[3]. Mechanistically, VPAC2 belongs to the PACAP/VIP receptor family together with VPAC1 and PAC1; however, unlike PAC1, which displays marked preference for PACAP, VPAC2 recognizes VIP and PACAP with comparable affinity, providing a distinct signaling profile and physiological function^[2]^[4]. In experimental systems, VPAC2 signaling has been implicated in central nervous system development and neuroprotection, and VPAC2 receptor activation mediates VIP-induced protection against neonatal excitotoxic brain injury in mice^[5]. Genetic and pharmacological studies further associate VPAC2-regulated signaling with circadian clock function and neuropsychiatric phenotypes, supporting its relevance in neurological disease models^[3]^[6]. Beyond the nervous system, VPAC2 is expressed in pancreatic islets and contributes to peptide-mediated regulation of insulin and glucagon secretion, linking receptor activity to metabolic homeostasis^[7]. For experimental applications, selective VPAC2 agonists have been developed and are widely used to investigate receptor-specific signaling, cellular responses, and therapeutic potential within the VIP/PACAP receptor network^[8].

References:

[1]. Lu J, et al. Targeting VIP and PACAP Receptor Signaling: New Insights into Designing Drugs for the PACAP Subfamily of Receptors. Int J Mol Sci. 2022 Jul 22;23(15):8069. [Content Brief]

[2]. Harmar AJ, et al. Pharmacology and functions of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase-activating polypeptide: IUPHAR review 1. Br J Pharmacol. 2012 May;166(1):4-17. [Content Brief]

[3]. Aton SJ, et al. Vasoactive intestinal polypeptide mediates circadian rhythmicity and synchrony in mammalian clock neurons. Nat Neurosci. 2005;8(4):476-83. [Content Brief]

[4]. Harmar AJ, et al. International Union of Pharmacology. XVIII. Nomenclature of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase-activating polypeptide. Pharmacol Rev. 1998;50(2):265-70. [Content Brief]

[5]. Rangon CM, et al. VPAC2 receptors mediate vasoactive intestinal peptide-induced neuroprotection against neonatal excitotoxic brain lesions in mice. J Pharmacol Exp Ther. 2005;314(2):745-52. [Content Brief]

[6]. Piggins HD. Schizophrenia: Zooming in on a gene. Nature. 2011;471(7339):455-6. [Content Brief]

[7]. Ahrén B. Role of pituitary adenylate cyclase-activating polypeptide in the pancreatic endocrine system. Ann N Y Acad Sci. 2008;1144:28-35.

[8]. Gourlet P, et al. Novel cyclic peptide agonist of high potency and selectivity for the type II vasoactive intestinal peptide receptor. J Biol Chem. 1997;272(18):11734-9. [Content Brief]

VPAC2 receptor Agonists (2)

VPAC2 receptor Related Products (2):

By Type:	Selective (2)

Cat. No.	Product Name	Effect	Purity

HY-P10768A

Ro 25-1553 TFA	Agonist
Ro 25-1553 TFA is a 31 amino acid vasoactive intestinal peptide (VIP) analog, that acts as an agonist for VIP2 receptor (VPAC2 receptor). Ro 25-1553 TFA exhibits a bronchodilator effect in nerve-induced or Carbachol (HY-B1208)-induced tracheal smooth muscle contraction in guinea pig model.

HY-P10768

Ro 25-1553	Agonist
Ro 25-1553 is a selective VIP₂ receptor (VPAC₂ receptor) agonist. Ro 25-1553 exhibits bronchodilatory effects on tracheal smooth muscle contractions induced by nerve stimulation or Carbachol (HY-B1208). Ro 25-1553 produces a superimposed effect when combined with Formoterol and Salmeterol (HY-14302). Ro 25-1553 can be used for the study of bronchoconstriction.

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