UpdatePrediction of blood–brain barrier penetration: are we missing the point?
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Drug-delivery nanocarriers to cross the blood-brain barrier
2016, Nanobiomaterials in Drug Delivery: Applications of NanobiomaterialsSingle compartment drug delivery
2014, Journal of Controlled ReleaseCitation Excerpt :A review of successful CNS drugs by Pajouhesh and Lenz identified several physicochemical properties of successful drugs (i.e. molecular weight < 500 Da, logP < 5, hydrogen bonding characteristics, and molecule flexibility) [107]. Modulating lipophilicity of drugs allows for passive diffusion of compounds across the BBB using the plasma membrane as a pathway [108–110]. Since this mechanism relies on passive diffusion, concentrations in the brain and circulation reach equilibrium, usually resulting in low brain concentrations and high systemic exposure.
Low brain penetrant CB1 receptor agonists for the treatment of neuropathic pain
2012, Bioorganic and Medicinal Chemistry LettersIn silico prediction of unbound brain-to-plasma concentration ratio using machine learning algorithms
2011, Journal of Molecular Graphics and ModellingCitation Excerpt :However, for drugs targeting proteins in the central nervous system (CNS) brain exposure may be the biggest hurdle to overcome in the drug discovery process [1]. In recent years, it has been observed [10,11] that Kp,brain or log BB may not reflect the relevant drug exposure in the brain since it is highly influenced by the relative binding affinity of compounds to plasma proteins and brain tissue [3]. It was highlighted that the pharmacological efficacy of a drug in the CNS is not dependent on the total but on the free drug concentration in the brain [3,12].
BrainPepPass: A Framework Based on Supervised Dimensionality Reduction for Predicting Blood-Brain Barrier-Penetrating Peptides
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