Receptor kinetics

Combinations with similar stoichiometry would be likely to have similar conductance (i.e., four groups of 1,2-4,5-7, and 8), while the subunit arrangement may be more important for the receptor kinetics because the agonist binding site is located between an a and a (3 subunit. If the binding site is assumed to be between the a subunit and the (5 subunit on the right (in this linear representation), there are three groups (1) 1-2, 2 x (a3 - p2) (2) 3-6, (a3 - p2)(a3 - p4) and (3) 7-8, 2 x... 

The in vitro data and the results from this clinical trial were synthesized in a so-called dynamic model of receptor kinetics by Liggett [72]. According to this theory, Gly/Gly homozygous individuals are already down-regulated as a result of exposure to endogenous catecholamines. Thus, the recurring exogenous exposure to... 

FIGURE 5.17. Dynamics of molecular recognition. Binding of the target molecule to the receptor. Kinetic zone diagram and characteristic equations. Adapted from Figure 1 of reference 22, with permission from the American Chemical Society. 

One frequently encounters the case where the equilibrium dissociation constant (iQ, see above) is defined by microconstants with Tast rates on and off the receptor. However, any change in potency in a chemical series (affinity) must represent an increase in the on (k+i) rate or a decrease in the off rate (fe i). Occasionally, either by accident or design, the off rate is altered dramatically enough to redefine the receptor kinetics of the compound such that the rates influence the actual pharmacodynam-... 

Table 2. Ligand-receptor kinetic data for cucurbituril...

B. Goldstein and M. Dembo, Approximating the effects of diffusion on reversible reactions at the cell surface ligand receptor kinetics, Biophys. J. 68, 1222—1230 (1995). 

F. L. Tobin. 2005. Response to continuous and pulsatile PTH dosing a mathematical model for parathyroid hormone receptor kinetics. Bone 37 159-169. 

Rosengren R, Safe S, Bunce NJ. 1991. Structure-dependent interactions of ligands with the rat cytosolic Ah receptor Kinetic analysis [Abstract 10], Toxicologist 11 27. 

Jager T, Kooijman SALM. 2005. Modeling receptor kinetics in the analysis of survival data for organophosphorus pesticides. Environ Sci Technol 39 8307-8314. 

Identify if antagonist is orthosteric or allosteric with agonism Measure receptor kinetics... 

Valotis A, Neukam K, Elert O, et al. (2004). Human receptor kinetics, tissue binding affinity, and stability of mometasone furoate. J. Pharm. Sci. 93 1337-1350. 

As shown elsewhere [78], the determination of structure-activity relationships and receptor kinetics, extrapolatable to man, requires the use of Na /K -ATPase preparations from human tissues. Autopsy preparations are perfectly suitable when taken within 12 hours post-mortem [78,79]. The enzyme should be only partially purified to avoid the various possible artefacts of intensive purification procedures [80-82]. The interaction of cardiac glycosides and NaYK -ATPase is controlled by Na, Mg, and... 

Actually, the determination of the receptor-kinetics (pharmacodynamics) of a digitalis compound Table 4.6) can be indispensable for the understanding of its in vivo behaviour as shown for the above-mentioned 16a-hydroxy-digitoxin [51,254]. Naturally, knowledge of the dynamics of interaction will also make possible the more profound interpretation of the thermodynamic equilibrium data given in Tables 4.1-4.5. 

Schild, l.H., l.W. Clark, C.C. Canavier, D.L. Kunze, and M.C. Andresen (1995). Afferent synaptic drive of rat medial nucleus tractus sohtarius neurons dynamic simulation of graded vesicular mobilization, release, and non-NMDA receptor kinetics. /. Neurophysiol. 74,1529-1548. 

Larsson, B. and Nemere, I. 2003a. Effect of growth and maturation on membrane-initiated actions of 1,25-dihydroxyvitamin D3.1. Calcium transport, receptor kinetics, and signal transduction in intestine of male chickens. Endocrinology 144 1726-35. 

Receptor kinetics, in which slow receptor off-rates have been proposed to lead to enhanced duration of action in both inhaled P2AR agonists and inhaled muscarinic M3 receptor antagonists [12]. 

Lieto, A.M., Cush, R.C., Thompson, N.L. Ligand-receptor kinetics measured by total internal reflection with fluorescence correlation spectroscopy. Biophys. J. 85, 3294-3302 (2003)... 

Udgaonkar J, Hess G. Acetylcholine receptor kinetics chemical kinetics. J Memhr Biol 1986 93 93-109. 

Taking the Hgand binding experiments in Dictyostelium cells as an example [19], a single molecule approach to receptor kinetics in Hving cells will be... 

Example R9-3.4 Deteraiinadcm of Dead Polymer Distribution When Transfer to Monomer Is the Primary Termination Step R9-4. Oxygen Lirni(ed Fermenttitian Scale Up R9-5, Receptor Kinetics... 

The interaction involves the predicted norm of the respective chemical structure-biological activity correlation through the presence of the predicted initial (in time evolution of ligand-receptor kinetics) bound ligand to the receptor site, see Eq. (3.204), as well as the algebraic norm... 

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