Smith, Quentin R.

CNS drug design [electronic resource] / Quentin R. Smith. - London : Henry Stewart Talks, 2008. - 1 online resource (1 streaming video file (46 min.) : color, sound). - Small molecule drug discovery, 2056-452X The blood-brain barrier : understanding the regulatory gatekeeper between brain and body, 2056-452X . - Henry Stewart talks. Biomedical & life sciences collection. Blood-brain barrier : understanding the regulatory gatekeeper between brain and body. Henry Stewart talks. Biomedical & life sciences collection. Small molecule drug discovery. .

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.

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Mode of access: World Wide Web.

1926 Henry Stewart Talks


Blood-Brain Barrier.
Brain.
Central Nervous System Diseases--drug therapy.
Drug Design.
Molecular Targeted Therapy.
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