Preliminary study on application of impregnated synthetic peptide TLC stationary phases for the pre-screening of 5-HT1A ligands.
Chromatographic parameters (deltaR(f)), defined as a difference in the migration of tested compound on the control and peptide impregnated silica gel TLC plates, were determined for 42 arylpiperazine derivatives. An amino acid sequence of the peptide used for impregnation was derived from the III transmembrane segment of the 5-HT(1A) receptor in the close vicinity of aspartic acid (Asp 166) residue. It was found that the deltaR(f) values obtained in a model employing tetrapeptide P4LA (ADVL), as well as the calculated logP correlate with 5-HT(1A) receptor affinity of the studied compounds.
Zajdel
Paweł
P
Department of Pharmaceutical Chemistry, Collegium Medicum of Jagiellonian University, 9 Medyczna St., 30-688 Kraków, Poland. mfzajdel@cyf-kr.edu.pl
Bojarski
Andrzej J
AJ
Byrtus
Hanna
H
Chłoń-Rzepa
Grazyna
G
Obniska
Jolanta
J
Chevallet
Pierre
P
Martinez
Jean
J
Pawłowski
Maciej
M
D000595:Amino Acid Sequence; D001224:Aspartic Acid / Q000737:chemistry; D002021:Buffers; D002846:Chromatography, Affinity / Q000379:methods; D002855:Chromatography, Thin Layer / Q000379:methods; D057927:Hydrophobic and Hydrophilic Interactions; D008024:Ligands; D008565:Membrane Proteins / Q000737:chemistry / Q000302:isolation & purification; D015394:Molecular Structure; D010455:Peptides / Q000138:chemical synthesis* / Q000737:chemistry* / Q000378:metabolism; D010865:Pilot Projects; D010879:Piperazines / Q000737:chemistry; D011985:Receptors, Serotonin / Q000737:chemistry* / Q000378:metabolism; D013329:Structure-Activity Relationship
D002021:Buffers; D008024:Ligands; D008565:Membrane Proteins; D010455:Peptides; D010879:Piperazines; D011985:Receptors, Serotonin; D001224:Aspartic Acid