Receptor binding, toxicolog

Basu, N., Klevanic, K., and Gamberg, M. et al. (2005). Effects of mercury on neurochemical receptor binding characteristics in wild mink. Environmental Toxicology and Chemistry 24, 1444-1450. 

Tonner LE, Katz DI, Heiman AS. 1997. The acute effect of lead acetate on glucocorticoid receptor binding in C6 glioma cells. Toxicology 116 109-122. 

For early clinical trials, where it is unlikely there will be full reproductive toxicology data, any application should include a discussion of whether any effects on reproduction can be anticipated from the primary pharmacodynamics. The nature of the target receptor binding and any potential for binding to receptors involved in reproduction should be considered. For compounds in classes already known to be teratogenic such as cytotoxic anticancer products, retinoids, or histone deacetylase inhibitors, it can be reasonably expected that... 

At the molecular level, the compound would be screened for activity on the target, for example, receptor binding affinity to cell membranes containing the homologous animal receptors (or if possible, on the cloned human receptors). Early studies would be done to predict effects that might later cause undesired drug metabolism or toxicologic complications. 

The data development effort planned by the EPA has the potential to add significantly to the database on endocrine disruption. The use of standardized laboratory protocols and careful evaluation procedures will maximize the value of the results. In addition to providing data relevant to the regulation of the chemicals being tested, the data will also be useful for understanding the relationship between the relatively simple endpoints examined in some of the Tier I screens (such as receptor binding) and the development of more toxicologically relevant apical endpoints noted in the Tier II tests. 

Receptor In toxicology Molecular structure in or on a cell, which specifically recognizes and binds to a compound and acts as a physiological signal transducer or mediator of an effect. 

Since the toxicology data on PCDEs is still limited, PCDEs should be considered as compounds having possible adverse effects on wildlife and humans until more data is provided. PCDEs have shown low toxic potency in fish, but this is also true for PCBs, some of which are quite toxic in mammals. Mono-ortho-PCBs have not caused rainbow trout early life stage mortality and non-ortho-PCBs have shown unexpectedly low early life stage mortality when comparing Ah-receptor binding affinities in mammals [144],... 

Howard MD, Pope CN. In vitro effects of chlorpyrifos, parathion, methyl parathion and their oxons on cardiac muscarinic receptor binding in neonatal and adult rats. Toxicology 2002 170(1—2) 1—10. 

The octanol/water partition coefficient is one of the most frequently used descriptors in biological quantitative structure activity relationships. It is considered to reflect the hydrophobicity of a molecule and therefore to be relevant both for correlating the transport properties and the receptor binding of biologically active molecules. Since pharmacological and toxicological research often concerns poorly characterized or not yet synthesized molecules, there is a... 

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