Synthesis and Structure−Activity Relationship of Fluoro Analogues of 8-{2-[4-(4-Methoxyphenyl)piperazin-1yl]ethyl}-8-azaspiro[4.5]decane-7,9-dione as Selective α<sub>1d</sub>-Adrenergic Receptor Antagonists

We have discovered high-affinity antagonists (exemplified by 11 and 12) that are the most selective for α1d-adrenergic receptors (α1d-AR) reported to date. In cloned receptor assay systems, 12 displays at least 95-fold selectivity for the α1d-AR over all other G-protein-coupled receptors tested, and the subtype selectivity of 11 was confirmed in pharmacologically defined isolated tissue preparations.

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PID https://www.doi.org/10.1021/jm0491391.s001
URL https://figshare.com/articles/journal_contribution/Synthesis_and_Structure_Activity_Relationship_of_Fluoro_Analogues_of_8_2_4_4_Methoxyphenyl_piperazin_1yl_ethyl_8_azaspiro_4_5_decane_7_9_dione_as_Selective_sub_1d_sub_Adrenergic_Receptor_Antagonists/3289969
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Access Right Open Access
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Author Konkel, Michael J.
Author Wetzel, John M.
Author Cahir, Marie
Author Craig, Douglas A.
Author Noble, Stewart A.
Author Gluchowski, Charles
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Collected From figshare
Hosted By figshare
Publication Date 2016-05-06
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Language English
Resource Type Other literature type
keyword Selective α 1
keyword α 1
system:type publication
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Source https://science-innovation-policy.openaire.eu/search/publication?articleId=r37980778c78::d9705becf02926255c310e7c337dfc6a
Author jsonws_user
Last Updated 26 December 2020, 17:45 (CET)
Created 26 December 2020, 17:45 (CET)