A study on application of impregnated synthetic peptide TLC stationary phases for the screening of 5-HT(1A) ligands. Part 2.

摘要

Six extended analogues of the recently described peptides (LDVL, ADVL) were designed and synthesized on a solid support, and then impregnated on TLC stationary phases. The impact of the impregnated peptide sequence modi fi cations on the chromatographic retard, DeltaR(f) (difference in the migration of tested compound on control and impregnated plates), of 42 arylpiperazine 5-HT(1A) receptor ligands was studied. None of the new models tested made a better prediction of 5-HT(1A) af fi nity than that utilizing ADVL tetrapeptide. Further validation of the ADVL model on a set of 22 structurally differentiated 2-methoxy-phenylpiperazine derivatives con fi rmed its effectiveness in the af fi nity discrimination of a coherent group of 5-HT(1A) receptor ligands. Copyright 2004 John Wiley & Sons, Ltd.