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Synthesis of isotopically labeled CI S‐(3a R )‐(‐)‐2,3,3a,4,5,9b‐hexahydro‐3‐(N‐propyl)‐1 H ‐benz[ e ]indole‐9‐carboxamide, a 5‐HT 1A receptor agonist
Author(s) -
Stolle Wayne T.,
Easter John A.,
Ackland Mark J.,
HaadsmaSvensson Susanne R.,
Lin ChiuHong,
Hsi Richard S. P.
Publication year - 1997
Publication title -
journal of labelled compounds and radiopharmaceuticals
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.432
H-Index - 47
eISSN - 1099-1344
pISSN - 0362-4803
DOI - 10.1002/(sici)1099-1344(199711)39:11<891::aid-jlcr34>3.0.co;2-q
Subject(s) - chemistry , carboxamide , agonist , radioligand , adme , tritium , receptor , stereochemistry , indole test , pharmacology , biochemistry , in vitro , medicine , physics , nuclear physics
The title compound is a potent and selective 5‐HT 1A receptor agonist with clinical potentials for treating anxiety and depression. It has been labeled with stable and radioactive isotopes to support ADME studies in animals and human subjects. Its carboxamide group was labeled with C‐14, C‐13, or C‐13, N‐15, and O‐18. To provide a radioligand for investigating the receptor binding characteristics of the compound, we also labeled it with tritium in the N‐propyl group to obtain the high specific activity of 86.7 Ci/mmol. © 1997 John Wiley & Sons, Ltd.