Table 1.
The major physiological roles of NPY receptors in humans, their agonists, and their antagonists
NPY receptors | Expression | Function | Agonist | Antagonist | References |
---|---|---|---|---|---|
Y1R |
Periphery, hypothalamus, hippocampus, neocortex, thalamus |
Food intake, energy homeostasis, body weight, angiogenesis, anti-anxiety, ethanol consumption, pain signaling, bone homeostasis, regulation blood pressure, sedation |
[Leu31,Pro34]NPY, [Phe7,Pro34]pNPY, [D-Arg25]NPY, [D-His26]-NPY |
1229U91,J-104870, J-115814,BMS-193885, SAR-135966,BVD-10, compound 3,BIBP3226, compound 4,SR120819A, BIBO3304 |
[14, 86, 124, 125] |
Y2R |
Brain, hippocampus, thalamus, hypothalamus |
Food intake, energy homeostasis, colonic transit, pain signaling, cardiovascular regulation, anxiety, neuronal excitability, angiogenesis, ethanol consumption, bone formation |
PYY(3–36),TM-30335, NPY13-36,obinepitide |
BII20246,JNJ-31020028, JNJ-5207787(compound 7), T4-[NPY(33–36)]4 |
[14, 59, 86, 124, 125] |
Y4R |
Gastrointestinal tract, hippocampus, pancreas, hypothalamus, prostate, human epidermis |
Food intake, energy homeostasis, regulates bone volume, body weight, affects fertility, muscle contraction |
BVD-74D,1229U91, Sub[-T yr-Arg-Leu-Arg-T yr-NH2]2, TM-30339,obinepitide |
[14, 21, 86, 124, 125] | |
Y5R | Hypothalamus |
Food intake, energy homeostasis, anticonvulsant, anxiety, mood control |
[D-Trp32]NPY, [D-Trp34]NPY, [cPP1-7, N P Y19-23, A l a31, Aib32, G l n34]hPP |
CGP71683A,S-25585, GW438014A,MK-0557, FMS-586,L-152,804 velneperit (S-2367), |
[14, 86, 124, 125] |