GR231118 (TFA)

GR231118 TFA, an analogue of the C-terminus of neuropeptide Y, is a potent , competitive and relative seletive antagonist at human neuropeptide YY receptor with a pKi of 10.4. GR231118 a potent agonist at the human neuropeptide YY4 receptor (pEC50=8.6; pKi=9.6) and a weak agonist at the human and rat neuropeptide Y Y2 and Y5 receptors. GR231118 also has high affinity for the mouse neuropeptide YY6 receptor (pKi= 8.8)[1].

OC(C(F)(F)F)=O.O=C1N2[C@](CCC2)([H])C(N[C@@H](CNC(CC[C@@H](C(N3C(CCC3)([H])C(N[C@@H](CNC(CC[C@@H]1NC([C@@H](N)[C@@H](C)CC)=O)=O)C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N)=O)CC4=CC=C(C=C4)O)=O)=O)=O)=O)CC5=CC=C(C=C5)O)=O)=O)=O)NC([C@@H](N)[C@@H](C)CC)=O)=O)C(N[C@H](C(N[C@@H](CCCNC(N)=N)C(N[C@@H](CC(C)C)C(N[C@@H](CCCNC(N)=N)C(N[C@H](C(N)=O)CC6=CC=C(C=C6)O)=O)=O)=O)=O)CC7=CC=C(C=C7)O)=O)=O

[1]E M Parker, et al. GR231118 (1229U91) and other analogues of the C-terminus of neuropeptide Y are potent neuropeptide Y Y1 receptor antagonists and neuropeptide Y Y4 receptor agonists. Eur J Pharmacol|[2]Y Dumont, et al. [(125)I]-GR231118: a high affinity radioligand to investigate neuropeptide Y Y(1) and Y(4) receptors. Br J Pharmacol. 2000 Jan;129(1):37-46.