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Agonist-directed trafficking, receptor

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

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

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...
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]

Agonist-Directed Trafficking of5-HT1A Receptor Stimulus... [Pg.228]

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]

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]

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

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]

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Agonist trafficking

Agonist-directed trafficking, of receptor

Agonist-directed trafficking, of receptor stimulus

Agonist-directed trafficking, receptor evidence

Agonist-directed trafficking, receptor signaling overview

Agonist-directed trafficking, receptor stimulus

Receptor agonists

Trafficking

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