Preliminary selection of 5-HT1Areceptor ligands by TLC on plates impregnated with synthetic peptides

TLC on plates impregnated with synthetic peptides have been used for chromatographic determination of 5-HT 1A receptor affinity. The peptide sequence is derived from the III transmembrane domain of the 5-HT 1A receptor. The rate of migration of selected 3-( ω -aminoalkyl)-5,5-dialkyl-(or spirocycloalkyl-1′,5) hydantoin derivatives was compared with affinity data. The decrease in the rate of migration of tested compounds in one model employing the tetrapeptide H-Ala-Asp-Val-Leu-OH as impregnant correlated with the binding affinity of the compounds. This approach enables the use of TLC on an impregnated stationary phase for preliminary screening of newly synthesized ligands.