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Protean agonists

In conclusion, H3 ligands offer the attractive vista of multiple applications in various disorders, but the ultimate definition of their therapeutic utility will have to await clinical trial results. Future work will determine whether inverse agonists, neutral antagonists, or protean agonists will constitute the more useful pharmacological intervention. [Pg.188]

T. Kenakin, Protean agonists. Keys to receptor active states , Ann. N.Y. Acad. Sci. 1997, 812,116-125. [Pg.974]

Fig. 8. SB 242084 is a agonist for PLC-PI and an inverse agonist for PLA2-AA and GTP[y35S] binding to Gf/I (i.e., SB 242084 is a protean ligand) for the 5-HT2C receptor. Accumulation of IP and release of AA were measured in CHO-1C7 cells, which express a high level of the human 5-HT2C receptor (10-20 pmol/mg protein, optimized to detect... Fig. 8. SB 242084 is a agonist for PLC-PI and an inverse agonist for PLA2-AA and GTP[y35S] binding to Gf/I (i.e., SB 242084 is a protean ligand) for the 5-HT2C receptor. Accumulation of IP and release of AA were measured in CHO-1C7 cells, which express a high level of the human 5-HT2C receptor (10-20 pmol/mg protein, optimized to detect...
Brink CB. Protean behavior by agonists agonist-directed trafficking of receptor signaling. Trends Pharmacol Sci 2002 23 454-455. [Pg.233]

Ganguli SC, Park CG, Holtmann MH, Hadac EM, Kenakin TP, Miller LJ. Protean effects of a natural peptide agonist of the G protein-coupled secretin receptor demonstrated by receptor mutagenesis. J Pharmacol Exp Ther 1998 286 593-598. [Pg.233]

See other pages where Protean agonists is mentioned: [Pg.1278]    [Pg.184]    [Pg.219]    [Pg.1278]    [Pg.482]    [Pg.1278]    [Pg.184]    [Pg.219]    [Pg.1278]    [Pg.482]    [Pg.255]    [Pg.222]    [Pg.223]    [Pg.388]    [Pg.255]    [Pg.78]    [Pg.953]    [Pg.78]   
See also in sourсe #XX -- [ Pg.219 ]



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PROTEAN

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