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• W2058827213 abstract "Chemically funtionalized analogues of antagonists of the P2X7 receptor, an ATP-gated cation channel, were synthesized as tools for biophysical studies of the receptor. These functionalized congeners were intended for use in chemical conjugation with retention of biological potency. The antagonists were l-tyrosine derivatives, related to [N-benzyloxycarbonyl-O-(4-arylsulfonyl)-l-tyrosyl]benzoylpiperazine (such as MRS2409, 2). The analogues were demonstrated to be antagonists in an assay of human P2X7 receptor function, consisting of inhibition of ATP-induced K+ efflux in HEK293 cells expressing the recombinant receptor. The analogues were of the general structure R1-Tyr(OR2)-piperazinyl-R3, in which three positions (R1−R3) were systematically varied in structure through introduction of chemically reactive groups. Each of the three positions was designed to incorporate a 3- or 4-nitrophenyl group. The nitro groups were reduced using NaBH4−copper(II) acetylacetonate to amines, which were either converted to the isothiocyanate groups, as potential affinity labels for the receptor, or acylated, as models for conjugation. An alternate route to Nα-3-aminobenzyloxycarbonyl functionalization was devised. The various positions of functionalization were compared for effects on biological potency, and the R2 and R3 positions were found to be most amenable to derivatization with retention of high potency. Four dimeric permutations of the antagonists were synthesized by coupling each of the isothiocyanate derivatives to either the precursor amine or to other amine congeners. Only dimers linked at the R2-position were potent antagonists. In concentration−response studies, two derivatives, a 3-nitrobenzyloxycarbonyl derivative 18 and a 4-nitrotoluenesulfonate 26b, displayed IC50 values of roughly 100 nM as antagonists of P2X7 receptor-mediated K+ flux." @default.
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• W2058827213 date "2002-08-30" @default.
• W2058827213 modified "2023-10-14" @default.
• W2058827213 title "Functionalized Congeners of Tyrosine-Based P2X₇ Receptor Antagonists: Probing Multiple Sites for Linking and Dimerization" @default.
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• W2058827213 doi "https://doi.org/10.1021/bc020025i" @default.
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