Human pharmacological activity

Generally based on shared in vitro metabolite profile with humans. Pharmacologic activity is a secondary consideration. Rodent and nonrodent species are easily identified. 

Apart from finding structures that give energy minima, most molecular mechanics packages will calculate structural features such as the surface area or the molecular volume. Quantities such as these are often used to investigate relationships between molecular structure and pharmacological activity. This field of human endeavour is called QSAR (quantitative structure and activity relations). 

The pharmacological activities of the isomers should be compared in vitro and in vivo in both animals and humans. Separate toxicological evaluation of the enantiomers would not usually be required when the profile of the racemate was relatively benign but unexpected effects - especially if unusual or near-effective doses in animals or near planned human exposure - would warrant further studies with the individual isomers. 

Large quantities of pharmacologically active substances are used annually in human medicine for diagnosis, treatment, and prevention of illness or to avoid unwanted pregnancy. In animal and fish farming, drugs are mostly adminis-... 

The physiological similarity and phylogenetic proximity of nonhuman primates to humans are often cited as rationale for primate selection for safety studies especially when mechanisms of toxicity or pharmacologic action are expected to be closely related to potential physiological reactions in humans. Likewise, species selection is often based on the demonstration of pharmacologic activity of the test article. Many biopharmaceuticals do not exhibit their intended activity in nonprimate species, whereas small molecules may have activity across all species. 

Human pharmacology (Phase I) Assess tolerance Define/describe pharmacokinetics and pharmacodynamics Explore drug metabolism and drug interactions Estimate activity Dose-tolerance studies Single and multiple dose PK and/or PD studies Drug interaction studies... 

Mammalian cell lines are the ideal model for studying an effect on the current underlying fKii they allow to use physiological temperatures (37 °C) for the human species HER 293, CHO or L cells expressing hERG channels may be used as a primary test to study the pharmacological activity of a compound... 

Early IPL studies focused mostly on the metabolism of the bronchodilators and corticosteroids or the pharmacological activity of bronchodilators on the ex vivo preparation. Recently, the absorptive transfer of beclomethasone dipro-prionate (BDP) has been measured following administration to the human lung reperfusion model by two different commercially available inhalers for which human pharmacokinetic data are available for comparison [43],... 

An active ingredient that is intended to furnish pharmacological activity or other direct effect in the diagnosis, cure, mitigation, treatment, or prevention of a disease, or to affect the structure of any function of the human body, but does not include intermediates used in the synthesis of such ingredient. ... 

Servan-Schreiber D, Perlstein WM, Cohen JD, Mintun M. (1998). Selective pharmacological activation of limbic structures in human volunteers a positron emission tomography study. J Neuropsychiatry Clin Neurosci. 10(2) 148-59. 

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