Abstract
AbstractThe advances in the molecular neurosciences during “the decade of the brain” in conjunction with new genomic and proteomic sciences have radically changed the paradigm of central nervous system (CNS) drug design and development. The classical, chemistry‐based small‐molecule drug discovery has been broadened by the twenty‐first century biology‐driven paradigm of large‐molecule neuropharmaceuticals: peptides, recombinant proteins, monoclonal antibodies, antisense oligonucleotides, and gene therapy. As this chapter will discuss, however, despite this progress in the field of neuroproteomics and rational drug design strategies, there is still a high failure rate of the candidates in later stages of projects and consequently an unsatisfied demand for novel neurotherapeutic and neurodiagnostic medicines. Therefore, CNS drug discovery and CNS drug targeting must be merged early in the CNS drug development process in order to obtain neuropharmaceuticals active in the brain following systemic administration.
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