Identification of a non peptidic RANTES antagonist

…, TJ Brown, P Cox, F Halley, P Lockey, IM McLay…

Index: Bright, Colin; Brown, Thomas J.; Cox, Paul; Halley, Frank; Lockey, Peter; McLay, Iain M.; Moore, Una; Porter, Barry; Williams, Robert J. Bioorganic and Medicinal Chemistry Letters, 1998 , vol. 8, # 7 p. 771 - 774

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Citation Number: 19

Abstract

A series of phenothiazines demonstrating inhibition of RANTES binding to THP-1 cell membranes has been identified. The lead compound RP23618 (IC50= 3μM) was found to inhibit specific binding of 125I-RANTES, but not 125I-MCP-1 to THP-1 cell membranes and furthermore to antagonise RANTES, but not MCP-1-induced chemotaxis of THP-1 cells.