TY  - ADVS
AU  - Smith,Quentin R.
TI  - CNS drug design
T2  - Small molecule drug discovery,
PY  - 2008///
CY  - London
PB  - Henry Stewart Talks
KW  - Blood-Brain Barrier
KW  - Brain
KW  - Central Nervous System Diseases
KW  - drug therapy
KW  - Drug Design
KW  - Molecular Targeted Therapy
N1  - Animated audio-visual presentation with synchronized narration; Title from title frames; Contents: Central nervous system diseases -- Drug market for CNS disorders -- Traditional CNS drug targets -- Novel CNS drug targets -- Multiple obstacles for drug delivery to CNS -- Pathways for drug exchange within the CNS -- The structure of brain capillaries impedes uptake -- Measures of drug uptake and distribution in brain -- BBB permeability and solute lipid solubility -- Tissues capillary PS and 95 per cent equilibration time -- Cerebral blood flow affects drug uptake and Kin -- Initial uptake vs. steady-state distribution -- Plasma protein binding and brain drug uptake -- Brain capillary drug transporters -- Transporters and drug distribution across BBB -- "Enzymatic" blood-brain barrier -- Relation between bound and free drug -- Free drug distribution ratio at steady state -- BBB changes in pathology and disease -- Drug-like properties to cross the BBB -- Early findings in BBB drug uptake -- Measures of lipophilicity -- Passive permeability across lipid membranes -- Drug ionization -- Influence of pH on neutral fraction -- Lipinski "rule of five" -- Impact of hydrogen bonds and alkyl groups -- Positive CNS drugs -- Poor CNS drug -- in vitro measures -- In vivo measures -- Methods to improve brain uptake -- Simple rules for efflux transporters -- % drug distribution to brain -- Biologic compounds -- Brain pharmacokinetics; Access restricted to subscribers
UR  - https://hstalks.com/bs/762/
UR  - https://hstalks.com/bs/p/277/
UR  - https://hstalks.com/bs/p/739/
ER  -