Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist

The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses. The synthesis and SAR of benzylamine side chain analogs of the NK-1 recepto...

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Veröffentlicht in:	Bioorganic & medicinal chemistry letters 1998-02, Vol.8 (3), p.281-284
Hauptverfasser:	Rosen, Terry J., Coffman, Karen J., McLean, Stafford, Crawford, Rosemary T., Bryce, Dianne K., Gohda, Yoshiko, Tsuchiya, Megumi, Nagahisa, Atsushi, Nakane, Masami, Lowe, John A.
Format:	Artikel
Sprache:	eng
Schlagworte:	Animals Biological and medical sciences Capsaicin - antagonists & inhibitors Cell Line Digestive system Guinea Pigs Humans Medical sciences Motor Activity - drug effects Neurokinin-1 Receptor Antagonists Pharmacology. Drug treatments Piperidines - chemical synthesis Piperidines - chemistry Piperidines - pharmacology Structure-Activity Relationship
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Zusammenfassung:	The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses. The synthesis and SAR of benzylamine side chain analogs of the NK-1 receptor antagonist CP-99,994 are described. The 5-trifluoromethoxy analog, CP-122,721, shows superior in vivo blockade of NK-1 receptor mediated responses.
ISSN:	0960-894X 1464-3405
DOI:	10.1016/S0960-894X(98)00012-2