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In a search for nonpeptide agonists for the neurotensin receptor (NTR1), we replaced the adamantyl amino acid moiety found in the antagonist SR48692 (1a) with leucine and related α-alkylamino acids found in peptide agonists. When tested in a calcium mobilization assay, we found that both d- and l-leucine confer partial agonist activity to the pyrazole scaffold with the l-enantiomer (3a) providing...
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