Neuropeptide Y GPCR Family Subtypes and Products

What Are Neuropeptide Y Receptors?

Neuropeptide Y receptors are a family of G protein-coupled receptors (GPCRs) comprised of five receptor subtypes: Y1, Y2, Y3, Y4, and Y5; Y3 is not present in humans. The neuropeptide Y receptors play a role in appetite, anxiety, and circadian rhythm. Y1, Y2, Y4, and Y5 are all major drug targets for obesity treatment.

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Neuropeptide Y Receptor Information

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NPY1R (Neuropeptide Y receptor type 1) is a receptor for neuropeptide Y that is the most abundant peptide present in the mammalian central and peripheral nervous system. Neuropeptide Y exhibits a variety of potent central and peripheral effects including those on feeding, memory, blood pressure, cardiac contractility and intestinal secretions. Neuropeptide Y effects are mediated by several different receptor subtypes, Y- 1, Y-1-like, Y-2, Y-3, Y-4 and Y-5. NPY1R is correlated with food feeding and subnanomolar antagonists of NPY1R have been discovered as potential anti-obesity agents. NPY1R is also involved in cardiovascular actions of exogenous neuropeptide Y and plays a role in maintaining basal blood pressure and heart rate in ischaemic heart failure.

NPY2R (Y2) belongs to the family of G protein-coupled receptors. It is expressed at high levels in central nerve system, heart, ileum and colon. NPY2R shows high affinity for neuropeptide Y (NPY), peptide YY (PYY), and a fragment of NPY including amino acids 13 to 36. The rank order of affinity of this receptor for pancreatic polypeptides is PYY > NPY > PYY (3-36) > NPY (2-36) > [Il-31, Gln-34] PP > [Leu-31, Pro-34] NPY > PP, [Pro-34] PYY and NPY free acid. NPY exhibits a variety of potent central and peripheral effects including those on feeding, memory, blood pressure, and intestinal secretions. NPY2R has been shown to contribute to obesity.

NPY4R (Y4) has been reported to be expressed at highest levels in brain, coronary artery and ileum. Low levels in pancreas and kidney. It is also been detected in colon and small intestine and isolated from human colon and head/neck libraries. It is one of the receptors for neuropeptide Y and peptide YY. The rank order of affinity of this receptor for pancreatic polypeptides is PP, PP (2-36) and [Ile-31, Gln-34] PP > [Pro-34] PYY > PYY and [Leu-31, Pro-34] NPY > NPY > PYY (3-36) and NPY (2-36) > PP (13-36) > PP (31-36) > NPY free acid. Ligand: Neuropeptide Y, Peptide YY.

NPY5R encondes 456-amino acid protein with 7 putative transmembrane domains. It has shown to be expressed in the brain and hypothalamus. Y5 receptors’ pharmacological profile correlates it with peptides known to elicit a feeding response. It has been suggested to have effects on psychomotor activity, food intake, regulation of central endocrine secretion, and potent vasoactive effects on the cardiovascular system.

Neuropeptide Y Cell Lines

Receptor Family	Receptor	Species	Parental	Stable Cell Lines	Division-Arrested Cells	Membranes
Neuropeptide Y	Y1	human	CHO-K1 Gαqi5	CG1273-1	DCG1273-1	MCG1273-1
	Y2	human	CHO-K1 Gαqi5	CG1274-1	DCG1274-1	MCG1274-1
	Y2	rat	CHO-K1	Cr1274-1	DCr1274-1	MCr1274-1
	Y4	human	CHO-K1	C1300-1	DC1300-1	MC1300-1
	Y4	human	CHO-K1 Gαqi5	CG1300-1	DCG1300-1	MCG1300-1
	Y5	human	HEK293T	C1275a	DC1275a	MC1275a
	Y5	human	HEK293T Gαqi5	CG1275	DCG1275	MCG1275