Baeza C R, Undén A
Department of Biochemistry, Stockholm University, Sweden.
FEBS Lett. 1990 Dec 17;277(1-2):23-5. doi: 10.1016/0014-5793(90)80800-x.
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.
采用茶袋法进行平行肽合成，通过固相肽合成法合成了NPY模型肽NPY 1-4-Aca-25-36的类似物。研究了这些肽作为配体与大鼠大脑皮质中NPY受体的亲和力。模型化合物NPY 1-4-Aca-25-36是大鼠脑中NPY受体的相对较差的配体（IC50 = 0.40 microM）。Arg35和Arg33对NPY受体识别配体都很重要。在与NPY C端部分相对应区域的几个位置进行取代，得到了对NPY受体亲和力仅略有降低的类似物。
