Blood-Brain Barrier in Drug Discovery: Optimizing Brain by Li Di, Edward H. Kerns

By Li Di, Edward H. Kerns

Focused on valuable apprehensive procedure (CNS) drug discovery efforts, this e-book educates drug researchers in regards to the blood-brain barrier (BBB) to allow them to impact vital advancements in a single of the main major – and such a lot not easy – parts of drug discovery.

• Written by way of international specialists to supply useful options 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 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 experiences of winning CNS and non-CNS medicines, classes realized and paths to the market

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Extra resources for Blood-Brain Barrier in Drug Discovery: Optimizing Brain Exposure of CNS Drugs and Minimizing Brain Side Effects for Peripheral Drugs

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The left panel of the illustration shows the assay and study types to be employed and the middle panel shows the parameters obtained with target values shown on the left. The focus of the workflow is on optimizing unbound brain concentrations as the basis for target exposure, PK/PD, and in vivo efficacy. c–t, concentration– time profile; CLint, intrinsic metabolic clearance; ER, efflux ratio; KD, potency of compound Papp, apparent permeability; PD, pharmacodynamics. STRATEGIES TO INCREASE/AVOID CNS PENETRATION/EXPOSURE 25 The latter is highly specific for the cell membrane of different cell types [80] and the membranes of the intracellular organelles [81, 82].

731. [26] Fung EK, Carson RE (2013) Cerebral blood flow with [15O] water PET studies using an image-derived input function and MR-defined carotid centerlines. Phys Med Biol 58(6):1903–1923. [27] Harada N, Ohba H, Fukumoto D, Kakiuchi T, Tsukada H (2004) Potential of [(18)F]betaCFT-FE (2beta-carbomethoxy-3beta-(4-fluorophenyl)-8-(2-[(18)F]fluoroethyl)nortropane) as a dopamine transporter ligand: a PET study in the conscious monkey brain. Synapse 54(1):37–45. [28] Palmer AM, Alavijeh MS (2013) Overview of experimental models of the blood-brain barrier in CNS drug discovery.

18 Pharmacokinetics of CNS Penetration most relevant surrogate PK compartment for the pharmacological effect. , intracellular enzymes), the ICF is the more relevant effect compartment. Principal NeuroPK Processes The following are the most important processes that describe the PK of a compound in the CNS: 1. Absorption, distribution, metabolism, excretion (ADME) processes which determine the systemic concentration–time profile in the blood circulation (as the source of input of the drug to the CNS) 2.

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