| Application of NMR spectroscopy in medicinal chemistry and drug discovery. | |
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MedLine Citation:
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PMID: 20809893 Owner: NLM Status: MEDLINE |
Abstract/OtherAbstract:
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We describe the details of the magnetic resonance spectroscopy and chemical shift imaging techniques for the human brain which have been developed over the last two decades. With these non-invasive tools, it is now readily possible to repeatedly assay up to 20 common brain metabolites. From the perspective of drug discovery, each of these metabolites could fulfill a number of useful functions: disease biomarker, surrogate marker of drug delivery, surrogate marker of drug efficacy and so on. To facilitate the possible utility of clinical magnetic resonance spectroscopy in future drug discovery, the major portion of the review is devoted to a detailed description of the well-validated neurochemical profiles of many common human brain disorders, for which MRS data now exists. Beyond proton, MRS, the commonest tool provided by the manufacturers of clinical MRI equipment, lays the world of heteronuclear NMR more familiar to chemists. Here too, with relatively little effort it has been possible to define neurochemical profiles of human brain disorders using (13)C MRS in particular. The future for drug discovery scientists is discussed. Finally, recognizing that a known feature of MR is the lack of sensitivity, we describe new efforts to harness hyperpolarization, with its 50,000 signal amplification, to conventional MRS. |
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Authors:
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Brian Ross; Thao Tran; Pratip Bhattacharya; D Martin Watterson; Napapon Sailasuta |
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Publication Detail:
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Type: Journal Article; Review |
Journal Detail:
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Title: Current topics in medicinal chemistry Volume: 11 ISSN: 1873-4294 ISO Abbreviation: Curr Top Med Chem Publication Date: 2011 |
Date Detail:
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Created Date: 2011-01-19 Completed Date: 2011-04-07 Revised Date: 2012-04-23 |
Medline Journal Info:
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Nlm Unique ID: 101119673 Medline TA: Curr Top Med Chem Country: Netherlands |
Other Details:
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Languages: eng Pagination: 93-114 Citation Subset: IM |
Affiliation:
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Clinical Magnetic Resonance Spectroscopy Unit, Huntington Medical Research Institutes, Pasadena, CA, USA. bdross.hmri@gmail.com |
Export Citation:
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| MeSH Terms | |
Descriptor/Qualifier:
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Animals Central Nervous System / chemistry Chemistry, Pharmaceutical Drug Discovery* Humans Magnetic Resonance Spectroscopy / methods* Metabolomics Neurons / chemistry |
| Grant Support | |
ID/Acronym/Agency:
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R01 AG031311/AG/NIA NIH HHS; R01 AG031311-04/AG/NIA NIH HHS; R01 NS047586/NS/NINDS NIH HHS; R01 NS047586-04/NS/NINDS NIH HHS |
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