Studies on the structural requirement for ligand binding to the neuropeptide Y (NPY) receptor from rat cerebral cortex.
Analogues of the NPY model peptide NPY 1-4-Aca-25-36 were synthesized by solid phase peptide synthesis using the tea-bag method for parallel peptide synthesis. The affinity of the peptides as ligands to the NPY receptor in rat cerebral cortex was investigated. The model compound NPY 1-4-Aca-25-36 was a relatively poor ligand to the NPY receptor in rat brain (IC50 = 0.40 microM). Arg35 and Arg33 were both important for ligand recognition by the NPY receptor. Substitutions in several positions in the region corresponding to the C-terminal part of NPY resulted in analogues with only minor reduction of the affinity for the NPY receptor.
Baeza
C R
CR
Department of Biochemistry, Stockholm University, Sweden.
Undén
A
A
D000595:Amino Acid Sequence; D000818:Animals; D002540:Cerebral Cortex / Q000378:metabolism*; D066298:In Vitro Techniques; D008024:Ligands; D008297:Male; D008969:Molecular Sequence Data; D009478:Neuropeptide Y / Q000378:metabolism*; D051381:Rats; D011919:Rats, Inbred Strains; D017476:Receptors, Neuropeptide Y; D017981:Receptors, Neurotransmitter / Q000378:metabolism*; D013329:Structure-Activity Relationship
D008024:Ligands; D009478:Neuropeptide Y; D017476:Receptors, Neuropeptide Y; D017981:Receptors, Neurotransmitter