title: Identification of a non peptidic RANTES antagonist.
abstract: A series of phenothiazines demonstrating inhibition of RANTES binding to THP-1 cell membranes has been identified. The lead compound RP23618 (IC50 = 3 microM) was found to inhibit specific binding of 125I-RANTES, but not 125I-MCP-1 to THP-1 cell membranes and furthermore to antagonize RANTES, but not MCP-1-induced chemotaxis of THP-1 cells.
authors.affiliation: Rhône-Poulenc Rorer, Dagenham Research Centre, Dagenham, Essex, UK.
authors.forename: C
authors.initials: C
authors.lastname: Bright
authors.forename: T J
authors.initials: TJ
authors.lastname: Brown
authors.forename: P
authors.initials: P
authors.lastname: Cox
authors.forename: F
authors.initials: F
authors.lastname: Halley
authors.forename: P
authors.initials: P
authors.lastname: Lockey
authors.forename: I M
authors.initials: IM
authors.lastname: McLay
authors.forename: U
authors.initials: U
authors.lastname: Moore
authors.forename: B
authors.initials: B
authors.lastname: Porter
authors.forename: R J
authors.initials: RJ
authors.lastname: Williams
mesh_terms: D002462:Cell Membrane / Q000187:drug effects / Q000378:metabolism; D018932:Chemokine CCL2 / Q000378:metabolism; D018946:Chemokine CCL5 / Q000037:antagonists & inhibitors*; D015195:Drug Design; D006801:Humans; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D007700:Kinetics; D015394:Molecular Structure; D010640:Phenothiazines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D014407:Tumor Cells, Cultured
chemical_list: D018932:Chemokine CCL2; D018946:Chemokine CCL5; D007202:Indicators and Reagents; D007457:Iodine Radioisotopes; D010640:Phenothiazines; C116623:RP 23618