Lecture 13 (Last) Flashcards
Reasons why drugs fail to reacht he market?
- Toxcity
- Tolerance
- Effiacy
- Bioavailability
What is structure based - drug design?
Identifying drug targets and producing a drug to either inhibit or enhance target function
What is the downside of structure based design?
Without knowledge on the target, it cannot be made
What method is used to produce structure based design drug?
High throughput screeening
What is structure based drug design also known as
Direct drug design
What is Ligand based drug design
Used in the absence of an experimental 3D structure
What are SAR and QSAR?
Mathematical models used to predict physiochemica, biological properties of compounds from their chemical structure
What is Saturation in Pre-clincal trials?
Observes binding of tracer ligand to the receptor
What are the three methods of binding experiments?
Saturation, displacement and kinetic
What is Quantification in Pre-clinical trials?
Must be able to distinguish bound molecule from unbound
What is the disadvantage to Saturation binding experiments?
Ligand needs to be traceable
What is the function of Saturation in Pre-clinical trials?
Quantifies maximal number of binding sites and affinity of the ligand
What is Displacement in Pre-clinical trials?
Measurement of the affinity of a ligand - assessing the displacement of a labelled ligand
What are two competitive interactions?
Direct binding assey (DBA)
Indicator-displacement assay (IDA)
What is Kinetic in Pre-clinical trials?
Follow binding experiments over time
What is functional assays?
Any biological system that yields a biochemical product or physiological response to drug stimulation
What does functional assays affect?
Whole tissues, cells in culture, membran preparations
What animal is used for in-vivo studies?
Laboratory Mouse
What are the three R’s to the ethical use of mouses?
Replacement, reduction and reinfement
What is the purpose of Replacement?
a method of testing not entailing the use of protecting aniamls must be used instead of a regulated procedure whenever possible
What is the purpose of Reduction?
Whenever a programme involving the use of protected animals is carried out the number of protected animals used must be reduced to a minimum without compromising the objectives of the programe
What is the purpose of Refinement?
Breeding, accommodation and care of protected animals and the methods used in regulated procedures applied to such animals must be refined so as to eliminate or reduce to the minimum possible pain, suffering, distress or lasting harm to those animals
