Second where the effect of the active substance can Prescribed maximum effect and NVP-TAE684 the concentration of the H half Maximum effect. The slope of the hill coefficient obtained Ht or decreases the slope of the concentration effect as the value γ h Ago or lower than 1. Otherwise, k can For drugs that act as an antagonist inhibition model Imax, IC50 Selected Be selected, and γ shape parameters of the equation. 2 above. EC50 value reflects the strength of the molecule and can be compared to the Sch Estimates of the activity of T be secure in vitro. Important considerations for the translation of EC50 values and Emax in vitro, in vivo between species go Ren protein binding affinity t and pharmacological target expression, tissue distribution, and its active metabolite.
For small molecules, subject to significant plasma protein binding can k, It is necessary to correct for the unbound fraction betr Chtlich vary according to species. It is assumed that the free concentration in the plasma is in equilibrium with the free drug concentration Luteolin in the tissues, where the interaction with efflux and absorption can confuse the relationship. In addition, for small molecules and biologics, species differences in the interaction between the drug and drug target will also be considered. W During the drug discovery and optimization process, it can be a M Possibility for a consistent relationship between in vitro and in vivo parameters of the power of a gr Ere confidence in the measurements best His term. In cases F, Where the activity t In vitro pr Diktiv in vivo activity T to justify correct differences between the types of power, such as by Chien et al .
. Distribution of the drug to its target site of action may affect the pharmacodynamics of a drug. Therefore, if possible m, Should the measurement of tissue drug concentrations, which included the site of action set to define the framework for the delivery of drugs to the target. This additionally USEFUL information can help, the difference between control and properties, which can be imported in the selection of several potential candidates. The distinction between active and Drogenkriminalit t as well as special features and / or non-specific binding sites remains difficult. A better amplifier Ndnis of drug metabolism is also crucial because active metabolites may contribute to the effects of the drug and may confuse the concentration-response relationship.
Approach to model the effect of AR HO47108 and its active metabolite AR HO47116 on the inhibition of gastric acid In dogs have been reported. Optimal distribution of the drug to its target or biophase must also as part of the PK / PD predictions are considered. But according to the site of action may or k tools for assessing biophase concentrations Can not exist. If available, k Can the Durchl Permeability and the distribution link to the site of action in combination with in vivo measurements of the activity Evaluated t to set the properties for redistribution. Distribution of drugs to the target tissue is h Examined frequently in models of diseases of the central nervous system, oncology and infectious disease.
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