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Design, Synthesis, and Optimization of Balanced Dual NK1/NK3 Receptor Antagonists
- Hanessian, Stephen;
- Jennequin, Thomas;
- Boyer, Nicolas;
- Babonneau, Vincent;
- Soma, Udaykumar;
- la Cour, Clotilde Mannoury;
- Millan, Mark J;
- De Nanteuil, Guillaume
Published Web Location
https://doi.org/10.1021/ml400528yAbstract
In connection with a program directed at potent and balanced dual NK1/NK3 receptor ligands, a focused exploration of an original class of peptidomimetic derivatives was performed. The rational design and molecular hybridization of a novel phenylalanine core series was achieved to maximize the in vitro affinity and antagonism at both human NK1 and NK3 receptors. This study led to the identification of a new potent dual NK1/NK3 antagonist with pK i values of 8.6 and 8.1, respectively.
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