(R)-(+)-HA-966 ((+)-HA-966) is a partial agonist antagonist of glycinesite of the N-methyl-D-aspartate (NMDA) receptor complex. (R)-(+)-HA-966 selectively blocks the activation of the mesolimbic dopamine system by amphetamine, has the potential for neuro
7-Chlorokynurenic acid sodium salt (7-CKA sodium salt) is a potent and selective antagonist of the glycine B coagonist site of the NMDA receptor (IC50: 0.56 μM). It is also a potent inhibitor of the reuptake of glutamate into synaptic vesicles (Ki: 0.59 μ
H-Arg-Gly-Asp-Cys-OH is a tetrapeptide that contains the arginine-glycine-aspartate (RGD) motif, a sequence that acts as a recognition site for various adhesion proteins.1It inhibits the binding of fibrinogen to endothelial cells and ADP-stimulated platelets with IC50values of 320 and 35 μM, respectively.2Implantation of titanium rods coated with H-Arg-Gly-Asp-Cys-OH increases bone formation in rat femurs.3H-Arg-Gly-Asp-Cys-OH has been conjugated to polyethylenimine to improve gene transfection efficiency.4 1.Park, H.S., Kim, C., and Kang, Y.K.Preferred conformations of RGDX tetrapeptides to inhibit the binding of fibrinogen to plateletsBiopolymers63(5)298-313(2002) 2.Tranqui, L., Andrieux, A., Hudry-Clergeon, G., et al.Differential structural requirements for fibrinogen binding to platelets and to endothelial cellsJ. Cell Biol.108(6)2519-2527(1989) 3.Ferris, D.M., Moodie, G.D., Dimond, P.M., et al.RGD-coated titanium implants stimulate increased bone formation in vivoBiomaterials20(23-24)2323-2331(1999) 4.Kunath, K., Merdan, T., Hegener, O., et al.Integrin targeting using RGD-PEI conjugates for in vitro gene transferJ. Gene Med.5(7)588-599(2003)
Obestatin is a 23 amino acid peptide hormone with a conserved C-terminal glycine residue and amidation site that is formed by cleavage of the ghrelin and obestatin prepropeptide.1It binds to the orphan receptor GPR39 (Kd= 1 nM) and stimulates cAMP production in CHO and HEK293 cells overexpressing human GPR39. Obestatin inhibits contraction of isolated mouse jejunum muscle strips induced by ghrelin .In vivo, obestatin (12.5-1,000 nmol/kg) suppresses food intake in a time- and dose-dependent manner and reduces body weight gain and gastric emptying in mice. Obestatin (0.22 g per animal) also reduces food intake and glucose response without affecting plasma insulin responses in fasted high-fat diet fed mice.2 1.Zhang, J.V., Ren, P.C., Avsian-Kretchmer, O., et al.Obestatin, a peptide encoded by the ghrelin gene, opposes ghrelin's effects on food intakeScience310(5750)996-999(2005) 2.Subasinghage, A.P., Green, B.D., Flatt, P.R., et al.Metabolic and structural properties of human obestatin {1-23} and two fragment peptidesPeptides31(9)1697-1705(2010)