Abstract:
:The seminal human dopamine D3 receptor (hD3R) ligand BP 897 has shown interesting properties during clinical trials. However, its lack of selectivity towards human adrenergic receptor impedes further development. Two approaches were followed to increase hD3R selectivity. The lead optimisation succeeded, we disclose here ligands with subnanomolar potency for D3R, combined with a good selectivity for the closely related human dopamine D2 and human adrenergic alpha-1 receptors.
journal_name
Bioorg Med Chem Lettjournal_title
Bioorganic & medicinal chemistry lettersauthors
Capet M,Calmels T,Levoin N,Danvy D,Berrebi-Bertrand I,Stark H,Schwartz JC,Lecomte JMdoi
10.1016/j.bmcl.2015.12.068subject
Has Abstractpub_date
2016-02-01 00:00:00pages
885-888issue
3eissn
0960-894Xissn
1464-3405pii
S0960-894X(15)30381-4journal_volume
26pub_type
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