Medicine Flashcards
What is involved in the process of drug discovery?
Target identification
Hit & lead identification
Lead optimisation
Pre-clinical development
What is involved in the process of drug development?
Clinical development Phase I, II, III
Launch and post launch
What happens as lipophilicty increases?
A compound is more likely to get more potent, less soluble and more toxic
How can lipophilicity of a compound be measured?
By allowing it to partition between 2 immiscible phases
What does LogD >0 mean?
More of the compound is in the organic phase than in the aqueous phase - the drug is hydrophobic
What does LogD<0 mean?
More of the compound is in the aqueous phase than in the organic phase - the drug is hydrophilic
Which solvent is used for most LogD measurements?
n-octanol
What is mass spectrometry?
A technique used to measure the relative mass of molecules
What can mass spec verify?
- Identity of a drug
- Presence of a particular drug in formulated products
- Verify presence of drugs and drug metabolites in samples
What is M+ in mass spec?
The molecular ion - has the highest molecular mass but isn’t always the most abundant
How is sample vaporisation achieved?
By using heat, placing sample in a vacuum or by using fast atom bombardment
What are the ionisation techniques?
Electron impact ionisation Chemical ionisation Fast atom bombardment Matrix assisted laser desorption ionisation Electrospray ionisation Atmospheric pressure chemical ionisation
What is the degree of fragmentation for the different ionisation techniques?
EI > CI»_space; FAB, ESI, APCI, MALDI
What is gas chromatography used for?
Analysis of non-polar volatile analytes
What are the most common targets for drug discovery?
G protein coupled receptors
