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Agonist-directed trafficking, of receptor

Agonist-Directed Trafficking of Receptor Stimulus and Serotonin Receptors... [Pg.213]

As mentioned earlier, current models of receptor function provide for receptor conformations that interconvert between inactive and active states. The agonist-directed trafficking of receptor stimulus hypothesis suggests that there are multiple active conformations of a receptor that differ in their capacity to couple/activate effector pathways. Such multistate models predict that, like agonist-stimulated responses, constitutive receptor activity and the relative efficacy of inverse agonists should also be response dependent (Fig. 6). [Pg.221]

Berg KA, Maayani S, Goldfarb J, Scaramellini C, Leff P, Clarke WP. Effector pathway-dependent relative efficacy at serotonin type 2A and 2C receptors evidence for agonist-directed trafficking of receptor stimulus. Mol Pharmacol 1998 54 94-104. [Pg.231]

Brink CB. Protean behavior by agonists agonist-directed trafficking of receptor signaling. Trends Pharmacol Sci 2002 23 454-455. [Pg.233]

Agonist-Directed Trafficking of 5-HT Receptor-Mediated Signal Transduction... [Pg.207]

Fig. 2. Agonist-directed trafficking of 5-HT2C receptor stimulus. Concentration-response curves for 5-HT2C agonists measuring AA release (PLA2-AA) and IP accumulation (PLC-PI) in CHO-1C19 cells expressing the human 5-HT2c receptor (approx 200 fmol/mg protein). Cells, in serum-free medium, were labeled with 1 pCi/mL [3H]-myo-inositol (10-25 Ci/mmol) for 24 h and with 0.1 pCi/inL [14C]-arachidonic acid (57 mCi/mmol) for 4 h at 37°C. Measurements of PLC-mediated IP accumulation and PLA2-AA release were made from the same multiwell, simultaneously, after 10 min of... Fig. 2. Agonist-directed trafficking of 5-HT2C receptor stimulus. Concentration-response curves for 5-HT2C agonists measuring AA release (PLA2-AA) and IP accumulation (PLC-PI) in CHO-1C19 cells expressing the human 5-HT2c receptor (approx 200 fmol/mg protein). Cells, in serum-free medium, were labeled with 1 pCi/mL [3H]-myo-inositol (10-25 Ci/mmol) for 24 h and with 0.1 pCi/inL [14C]-arachidonic acid (57 mCi/mmol) for 4 h at 37°C. Measurements of PLC-mediated IP accumulation and PLA2-AA release were made from the same multiwell, simultaneously, after 10 min of...
Brink CB, Wade SM, Neubig RR. Agonist-directed trafficking of porcine a2A-adrenergic receptor signaling in Chinese hamster ovary cells 1-isoproterenol selectively activates Gs. J Pharmacol Exp Ther 2000 294 539-547. [Pg.73]

Cussac D, Newman-Tancredi A, Duqueyroix D, Pasteau V, Millan MJ. Differential activation of Gq/11 and Gi(3) proteins at 5-hydroxytryptamine(2C) receptors revealed by antibody capture assays influence of receptor reserve and relationship to agonist-directed trafficking. Mol Pharmacol 2002 62 578-589. [Pg.232]

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Agonist trafficking

Agonist-directed trafficking, of receptor stimulus

Agonist-directed trafficking, receptor

Receptor agonists

Trafficking

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