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VIP/PACAP Receptor Phosphorylation Assays

Vasoactive intestinal peptide (VIP) and pituitary adenylate cyclase-activating peptide (PACAP) receptors are activated by the endogenous peptides VIP, PACAP-38 and PACAP-27. VPAC1 and VPAC2 receptors display comparable affinity for the PACAP peptides and VIP. Most isoforms of the PAC1 receptor display  >100 fold higher affinity for the PACAP peptides than for VIP. PG 99-465 is a VPAC2 receptor antagonist but has been reported to have significant activity at VPAC1 and PAC1 receptors. The selective PAC1 receptor agonist maxadilan, was extracted from the salivary glands of sand flies and has no sequence homology to VIP or the PACAP peptides. Agonist stimulation normally leads to stimulation of intracellular cyclic AMP accumulation by coupling to Gs proteins. PAC1, VPAC1 and VPAC2 receptors belong to the family B of GPCRs. This family comprises receptors for all peptides structurally related to VIP and PACAP, and also receptors for parathyroid hormone, corticotropin-releasing factor, calcitonin and related peptides. For all family B receptors, the large N-terminal ectodomain plays a crucial role in ligand recognition. Both VIP and PACAP, acting through PAC1 and VPAC2 receptors, play roles in the control of circadian rhythms in the brain's "master clock" in the suprachiasmatic nuclei (SCN) of the hypothalamus. In addition, PAC1 and VPAC2 receptors on pancreatic β-cells have been implicated in the control of pancreatic insulin secretion.

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OD signals in pT444/pS447-PAC1 Phosphorylation Assay
pT444/pS447-PAC1 Phosphorylation Assay Kit
The pT444/pS447-PAC1 Phosphorylation Assay Kit allows determination of PAC1 Phosphorylation in 96-well plates without the need for Western blot analysis.
$ 600.00 *
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OD signals in pS450/pS452-PAC1 Phosphorylation Assay
pS450/pS452-PAC1 Phosphorylation Assay Kit
The pS450/pS452-PAC1 Phosphorylation Assay Kit allows determination of PAC1 Phosphorylation in 96-well plates without the need for Western blot analysis.
$ 600.00 *
Details

For more information on chemokine receptor pharmacology please refer to the IUPHAR database. For further reading refer to:

Harmar AJ, Arimura A, Gozes I, Journot L, Laburthe M, Pisegna JR, Rawlings SR, Robberecht P, Said SI, Sreedharan SP, Wank SA, Waschek JA. International Union of Pharmacology. XVIII. Nomenclature of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase-activating polypeptide. Pharmacol Rev. 1998 Jun;50(2):265-70. PMID: 9647867; PMCID: PMC6721840.

Vaudry D, Gonzalez BJ, Basille M, Yon L, Fournier A, Vaudry H. Pituitary adenylate cyclase-activating polypeptide and its receptors: from structure to functions. Pharmacol Rev. 2000 Jun;52(2):269-324. PMID: 10835102.

Harmar AJ, Fahrenkrug J, Gozes I, Laburthe M, May V, Pisegna JR, Vaudry D, Vaudry H, Waschek JA, Said SI. 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. doi: 10.1111/j.1476-5381.2012.01871.x. PMID: 22289055; PMCID: PMC3415633.

Laburthe M, Couvineau A, Marie JC. VPAC receptors for VIP and PACAP. Recept Channels. 2002;8(3-4):137-53. PMID: 12529932.

Fahrenkrug J, Goetzl EJ, Gozes I, Harmar A, Laburthe M, May V, Pisegna JR, Said SI, Vaudry H, Vaudry D, Waschek JA. VIP and PACAP receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database. IUPHAR/BPS Guide to Pharmacology CITE. 2019; 2019(4).

For more information on chemokine receptor pharmacology please refer to the  IUPHAR  database. For further reading refer to: Harmar AJ, Arimura A, Gozes I, Journot L, Laburthe M,... read more »
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VIP/PACAP Receptor Phosphorylation Assays

For more information on chemokine receptor pharmacology please refer to the IUPHAR database. For further reading refer to:

Harmar AJ, Arimura A, Gozes I, Journot L, Laburthe M, Pisegna JR, Rawlings SR, Robberecht P, Said SI, Sreedharan SP, Wank SA, Waschek JA. International Union of Pharmacology. XVIII. Nomenclature of receptors for vasoactive intestinal peptide and pituitary adenylate cyclase-activating polypeptide. Pharmacol Rev. 1998 Jun;50(2):265-70. PMID: 9647867; PMCID: PMC6721840.

Vaudry D, Gonzalez BJ, Basille M, Yon L, Fournier A, Vaudry H. Pituitary adenylate cyclase-activating polypeptide and its receptors: from structure to functions. Pharmacol Rev. 2000 Jun;52(2):269-324. PMID: 10835102.

Harmar AJ, Fahrenkrug J, Gozes I, Laburthe M, May V, Pisegna JR, Vaudry D, Vaudry H, Waschek JA, Said SI. 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. doi: 10.1111/j.1476-5381.2012.01871.x. PMID: 22289055; PMCID: PMC3415633.

Laburthe M, Couvineau A, Marie JC. VPAC receptors for VIP and PACAP. Recept Channels. 2002;8(3-4):137-53. PMID: 12529932.

Fahrenkrug J, Goetzl EJ, Gozes I, Harmar A, Laburthe M, May V, Pisegna JR, Said SI, Vaudry H, Vaudry D, Waschek JA. VIP and PACAP receptors (version 2019.4) in the IUPHAR/BPS Guide to Pharmacology Database. IUPHAR/BPS Guide to Pharmacology CITE. 2019; 2019(4).

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