title: Preliminary study on application of impregnated synthetic peptide TLC stationary phases for the pre-screening of 5-HT1A ligands.
abstract: 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.
authors.affiliation: Department of Pharmaceutical Chemistry, Collegium Medicum of Jagiellonian University, 9 Medyczna St., 30-688 Kraków, Poland. mfzajdel@cyf-kr.edu.pl
authors.forename: Paweł
authors.initials: P
authors.lastname: Zajdel
authors.forename: Andrzej J
authors.initials: AJ
authors.lastname: Bojarski
authors.forename: Hanna
authors.initials: H
authors.lastname: Byrtus
authors.forename: Grazyna
authors.initials: G
authors.lastname: Chłoń-Rzepa
authors.forename: Jolanta
authors.initials: J
authors.lastname: Obniska
authors.forename: Pierre
authors.initials: P
authors.lastname: Chevallet
authors.forename: Jean
authors.initials: J
authors.lastname: Martinez
authors.forename: Maciej
authors.initials: M
authors.lastname: Pawłowski
mesh_terms: 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
chemical_list: D002021:Buffers; D008024:Ligands; D008565:Membrane Proteins; D010455:Peptides; D010879:Piperazines; D011985:Receptors, Serotonin; D001224:Aspartic Acid