Modulated receptor theory

Receptor theory is based on the classical Law of Mass Action as developed by Michaelis and Menten (20) for the study of enzyme catalysis. The extrapolation of classical enzyme theory to receptors is, however, an approximation. In an enzyme-substrate (ES) interaction, the substrate S undergoes an enzyme-catalyzed conversion to a product or products. Because of the equilibrium established, product accumulation has the ability to reverse the reaction process. Alternatively, the latter can be used in other cellular pathways and is thus removed from the equilibrium situation or can act as a feedback modulator (21) to alter the ES reaction either positively or negatively (Equation 10.2). 

Allosteric modulation of seven transmembrane spanning receptors Theory, practice, and opportunities for central nervous system dmg discovery 12JMC1445. 

To check our theories, we devised an experiment that was planned to trigger an intercalation of harmine into the genetic material that would sustain and stabilize its charge-transfer energy within a superconducting matrix. We reasoned that an infusion of ayahuasca plus tryptamine (mushroom) admixtures would allow us to do the following (1) We would hear and vocally imitate the ESR modulation of the tryptamines as they intercalated with their RNA receptors. (2) The amplified tryptamine-RNA... 

The theory of selective nudear receptor modulation to achieve therapeutic value by an optimized activity profile different from the natural ligand has been also experimentally studied in several other receptors. 

After the formation of an RL eomplex, a functional response to receptor activation can be related to the concentration of the ligand present (Fig. 10.1a). Occupancy theory, developed by Clark in 1926 (22), is based on a dose/ concentration-response relationship. This theory has undergone eontinuous refinement based on experimental data to aid in further delineating the increasingly complex coneept of ligand efficacy (23) and to accommodate allosteric site modulation of receptor function (21,24,25), ternary complex models, (26,27) and their extension to constitutively active re-... 

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