By Li Di, Edward H. Kerns
Focused on vital frightened process (CNS) drug discovery efforts, this publication educates drug researchers in regards to the blood-brain barrier (BBB) to allow them to have an effect on vital advancements in a single of the main major – and so much hard – components of drug discovery.
• Written via global specialists to supply functional suggestions to extend mind penetration or reduce CNS side-effects
• Reviews state of the art in silico, in vitro, and in vivo instruments to evaluate mind penetration and complicated CNS drug supply strategies
• Covers BBB body structure, medicinal chemistry layout rules, loose drug speculation for the BBB, and delivery mechanisms together with passive diffusion, uptake/efflux transporters, and receptor-mediated processes
• Highlights the advances in modelling BBB pharmacokinetics and dynamics relationships (PK/PD) and physiologically-based pharmacokinetics (PBPK)
• Discusses case reports of winning CNS and non-CNS medicinal drugs, classes realized and paths to the market
Read or Download Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs PDF
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Occupied with primary anxious procedure (CNS) drug discovery efforts, this publication educates drug researchers concerning the blood-brain barrier (BBB) to allow them to have an effect on vital advancements in a single of the main major – and so much tough – components of drug discovery. • Written through international specialists to supply functional ideas to extend mind penetration or reduce CNS side-effects• Reviews state of the art in silico, in vitro, and in vivo instruments to evaluate mind penetration and complex CNS drug supply strategies• Covers BBB body structure, medicinal chemistry layout ideas, loose drug speculation for the BBB, and delivery mechanisms together with passive diffusion, uptake/efflux transporters, and receptor-mediated processes• Highlights the advances in modelling BBB pharmacokinetics and dynamics relationships (PK/PD) and physiologically-based pharmacokinetics (PBPK)• Discusses case reviews of profitable CNS and non-CNS medicinal drugs, classes realized and paths to the marketplace
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Extra info for Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs
Transport processes which determine the BBB transfer of the drug between blood and brain (as the measure of the rate and extent of brain penetration) 3. Intrabrain distribution of the drug (as the key element to determine the active site concentration of the drug in the effect compartment) 4. Elimination of the drug from the CNS (often with ISF bulk flow into the CSF or back to blood across BBB) PK Measurements, PK Parameters, and Key Equations This paragraph focuses on those PK parameters and equations which are most c ritical for the understanding and optimization of CNS penetration and distribution of compounds in a drug discovery setting.
Drug Metab Dispos 2004 Jan;32(1):132–139.  Kodaira H, Kusuhara H, Fuse E, Ushiki J, Sugiyama Y (2014) Quantitative investigation of the brain-to-cerebrospinal fluid unbound drug concentration ratio under steady-state conditions in rats using a pharmacokinetic model and scaling factors for active efflux transporters. Drug Metab Dispos 42(6):983–989.  Reichel A, Begley DJ, Abbott NJ (2003) An overview of in vitro techniques for blood– brain barrier studies. Methods Mol Med 89:307–324.  Garberg P, Ball M, Borg N, Cecchelli R, Fenart L, Hurst RD, Lindmark T, Mabondzo A, Nilsson JE, Raub TJ, Stanimirovic D, Terasaki T, Oberg JO, Osterberg T (2005) In vitro models for the blood-brain barrier.
Exp Opin Drug Discov 4(3):207–218.  Zhang D, Surapaneni S (2012) ADME-Enabling Technologies in Drug Design and Development. John Wiley & Sons, NJ, p. 622.  Liu X, Smith BJ, Chen C, Callegari E, Becker SL, Chen X, Cianfrogna J, Doran AC, Doran SD, Gibbs JP, Hosea N, Liu J, Nelson FR, Szewc MA, Van Deusen J. (2005) Use of a physiologically based pharmacokinetic model to study the time to reach brain equilibrium: an experimental analysis of the role of blood-brain barrier permeability, plasma protein binding, and brain tissue binding.
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