Neuropeptide Y Receptor
Neuropeptide Y (NPY) is a 36-amino acid peptide which belongs to the so-called NPY family of biologically active peptides, together with two other members, peptide YY and pancreatic polypeptide (PP). Originally NPY was isolated from brain extracts and found to be one of the most abundant neuropeptides within the brain. NPY has a pivotal role in many physiological functions such as food intake, energy homeostasis, circadian rhythm, and cognition. In addition, the peptide has been suggested to be a key component in the stress response, having anxiolytic properties. To date seven different Y receptors (Y1-Y8) have been described in vertebrates, of which up to 5 (Y1, Y2, Y4, Y5, y6) are present in mammals. While the Y1, Y2, Y4 and Y5 receptors are functional in all mammals, the y6 receptor is non-functional in several mammals including humans and has been lost in rats. The receptor originally identified as the Y3 receptor has been characterized as CXC chemokine receptor type 4 and is thus included in the chemokine receptor family.
NPY shows strong affinity for the Y1, Y2 and Y5 receptor, while PP is the preferential agonist at the Y4 receptor. Like NPY itself, the Y1 and Y2 receptors are widely distributed throughout the brain. Brain areas expressing Y1 and Y2 receptor immunoreactivity include the frontal cortex, lateral septum, NAc, bed nucleus of the stria terminalis, PVH, ARC, lateral hypothalamus, amygdala, hippocampus, NTS and area postrema. In contrast, Y4 receptor expression is restricted to only a few brain regions including the medial preoptic area, PVH, NTS and area postrema. Finally, the Y5 receptor occurs in several limbic brain areas but is less abundant than the Y1 or Y2 receptor. Interestingly, Y5 receptor expression coincides in most cases with Y1 receptor expression, but not vice versa.
References
1.Reichmann F, Holzer P. Neuropeptides. 2016;55:99–109.
NPY shows strong affinity for the Y1, Y2 and Y5 receptor, while PP is the preferential agonist at the Y4 receptor. Like NPY itself, the Y1 and Y2 receptors are widely distributed throughout the brain. Brain areas expressing Y1 and Y2 receptor immunoreactivity include the frontal cortex, lateral septum, NAc, bed nucleus of the stria terminalis, PVH, ARC, lateral hypothalamus, amygdala, hippocampus, NTS and area postrema. In contrast, Y4 receptor expression is restricted to only a few brain regions including the medial preoptic area, PVH, NTS and area postrema. Finally, the Y5 receptor occurs in several limbic brain areas but is less abundant than the Y1 or Y2 receptor. Interestingly, Y5 receptor expression coincides in most cases with Y1 receptor expression, but not vice versa.
References
1.Reichmann F, Holzer P. Neuropeptides. 2016;55:99–109.
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Neuropeptide Y Receptor
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RFRP-1 (human)
catalog no : M30817
cas no: 311309-25-8
Potent endogenous NPFF receptor agonist (EC50 values are 0.0011 and 29 nM for NPFF2 and NPFF1, respectively). Attenuates contractile function of isolated rat and rabbit cardiac myocytes. Reduces heart rate, stroke volume, ejection fraction and cardiac output, and increases plasma prolactin levels in rats. GnIH homolog. -
RFRP 3 (human)
catalog no : M30816
cas no: 311309-27-0
Agonist of the NPFF1 receptor (IC50 = 0.7 nM for inhibition of forskolin-induced cAMP production). Homolog of gonadotropin-inhibitory hormone (GnIH); inhibits activity of gonadotropin-releasing hormone (GnRH) neurons. -
Spexin
catalog no : M30806
cas no: 1370290-58-6
Potent galanin receptor 2/3 (GAL2/GAL3) agonist (EC50 values are 45.7 and 112.2 nM, respectively). Exhibits no significant activity at galanin receptor 1. Endogenous satiety-inducing peptide; inhibits long chain fatty acid uptake by adipocytes and decreases food consumption in diet-induced obese mice and rats. Attenuates LH secretion in goldfish. Exhibits anxiolytic effects in vivo. -
CART (55-102) (rat)
catalog no : M30707
cas no: 209615-79-2
Cocaine- and amphetamine-regulated transcript (CART) with potent appetite-suppressing activity. Satiety factor; inhibits normal and starvation-induced feeding. Closely related to the actions of leptin and neuropeptide Y; blocks the neuropeptide Y-induced feeding response. Induces anxiety and stress behavior in rodents. -
CART (55-102) (human)
catalog no : M30705
cas no: 214050-22-3
Cocaine- and amphetamine-regulated transcript (CART) with potent appetite-suppressing activity. Satiety factor; inhibits normal and starvation-induced feeding. Closely related to the actions of leptin and neuropeptide Y; blocks the neuropeptide Y-induced feeding response.