A study on application of impregnated synthetic peptide TLC stationary phases for the screening of 5-HT1A ligands. Part 2.
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 modifications on the chromatographic retard, Delta R(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) affinity than that utilizing ADVL tetrapeptide. Further validation of the ADVL model on a set of 22 structurally differentiated 2-methoxy-phenylpiperazine derivatives confirmed its effectiveness in the affinity discrimination of a coherent group of 5-HT(1A) receptor ligands.
Zajdel
Paweł
P
Department of Pharmaceutical Chemistry, Jagiellonian University Medical College, 9 Medyczna Street, 30-688 Kraków, Poland. mfzajdel@cyf-kr.edu.pl
Bojarski
Andrzej J
AJ
Bugno
Ryszard
R
Jurczyk
Sławomir
S
Kołaczkowski
Marcin
M
Nowak
Mateusz
M
Subra
Gilles
G
Martinez
Jean
J
Pawłowski
Maciej
M
D002855:Chromatography, Thin Layer / Q000379:methods*; D008024:Ligands; D015394:Molecular Structure; D009842:Oligopeptides / Q000138:chemical synthesis* / Q000378:metabolism; D010879:Piperazines / Q000138:chemical synthesis; D044282:Receptor, Serotonin, 5-HT1A / Q000378:metabolism*
D008024:Ligands; D009842:Oligopeptides; D010879:Piperazines; D044282:Receptor, Serotonin, 5-HT1A