Ligand-receptor interaction-induced

TABLE 3.1 Methods Used to Quantify Ligand-Receptor Interaction-Induced Changes in Intracellular 2nd Messengers... 

B. Ligand-receptor interaction -induced functional effects... 

Binding experiments are performed in order to characterize the affinity of a compound for a receptor but they do not establish whether a compound behaves as an agonist, an antagonist or an inverse agonist. Such determinations necessarily involve functional measurements of ligand-receptor interaction-induced changes in an intracellular signal (Table 3.1). 

Unfortunately, the impact of anticonvulsants on NA-induced seizures has not been modeled in this way. Given many countermeasures have different ligand-receptor interactions, such an approach would need to be expanded to the other excitatory and inhibitory neurotransmitters and... 

Drug-receptor interactions may quantitatively differ among rapidly converting multiple receptor states that are induced by agonist binding. While most studies commonly focus on analysis of ligand-receptor interactions and cellular responses under presumed steady-state conditions, experimental techniques available for the quantitative analysis of drug-receptor interactions with transient receptor conformational... 

The CXC CK family displays disparate angiogenic activity, depending on the presence or absence of the ELR motif (a NH2-terminal motif previously found to be important in ligand/receptor interactions). CXC CKs containing the ELR motif, such as IL-8, are potent angiogenic factors, inducing... 

The most extensively studied agonists are the halogenated aromatic hydrocarbons such as TCDD, polychlorinated biphenyls, and polychlorinated dibenzofurans as well as PAHs such as benzo[a]pyrene and 3-MC. One of the highest affinity ligands of the AHR and the most potent inducer of CYPlAl expression is TCDD. As the result of this ligand-receptor interaction, exposure to TCDD produces a wide variety of toxic effects that are species- and tissue-specific. The response to TCDD is due to the fact that TCDD has a remarkably high affinity for the AHR (on the order of 10 M, and that this ligand is... 

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