Article ; Online: Bisoprolol-based
Bioorganic & medicinal chemistry letters
2021 Volume 36, Page(s) 127789
Abstract: The selectivity of a drug toward various isoforms of the target protein family is important in terms of toxicology. Typically, drug or candidate selectivity is assessed by in vitro assays, but in vivo investigations are currently lacking. Positron ... ...
Abstract | The selectivity of a drug toward various isoforms of the target protein family is important in terms of toxicology. Typically, drug or candidate selectivity is assessed by in vitro assays, but in vivo investigations are currently lacking. Positron emission tomography (PET) allows the non-invasive determination of the in vivo distribution of a radiolabeled drug, which can provide in vivo data regarding drug selectivity. Since the discovery of propranolol, a non-selective β-blocker inhibiting both β |
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MeSH term(s) | Adrenergic beta-Antagonists/chemical synthesis ; Adrenergic beta-Antagonists/chemistry ; Adrenergic beta-Antagonists/pharmacology ; Animals ; Bisoprolol/chemical synthesis ; Bisoprolol/chemistry ; Bisoprolol/pharmacology ; Dose-Response Relationship, Drug ; Fluorine Radioisotopes ; Heart/drug effects ; Mice ; Mice, Inbred BALB C ; Molecular Structure ; Positron-Emission Tomography ; Receptors, Adrenergic, beta-1/metabolism ; Structure-Activity Relationship ; Tissue Distribution |
Chemical Substances | Adrenergic beta-Antagonists ; Fluorine Radioisotopes ; Receptors, Adrenergic, beta-1 ; Bisoprolol (Y41JS2NL6U) |
Language | English |
Publishing date | 2021-01-14 |
Publishing country | England |
Document type | Journal Article ; Research Support, Non-U.S. Gov't |
ZDB-ID | 1063195-1 |
ISSN | 1464-3405 ; 0960-894X |
ISSN (online) | 1464-3405 |
ISSN | 0960-894X |
DOI | 10.1016/j.bmcl.2021.127789 |
Database | MEDical Literature Analysis and Retrieval System OnLINE |
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