Diarylacetylene piperidinyl amides as novel anxiolytics |
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| Authors: | Kordik Cheryl P Luo Chi Gutherman Maryann Vaidya Anil H Rosenthal Daniel I Crooke Jeffrey J McKenney Sandra L Plata-Salaman Carlos R Reitz Allen B |
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| Institution: | Drug Discovery Division, Johnson & Johnson Pharmaceutical Research and Development LLC, Welsh and McKean Roads, Spring House, PA 19477, USA. ckordik@prdus.jnj.com |
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| Abstract: | N-Phenyl-2-1-3-(2-pyridinylethynyl)benzoyl]-4-piperidine]acetamide (9) and related piperidine acetamide derivatives have good oral activity in the elevated plus maze, an animal model predictive of clinical efficacy for the treatment of anxiety. Modest affinity was observed for the neurokinin NK-1 and 2 receptors, which are known to be involved in the regulation of mood and emotion. |
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