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

T J Rosen; K J Coffman; S McLean; R T Crawford; D K Bryce; Y Gohda; M Tsuchiya; A Nagahisa; M Nakane; J A Lowe 3rd

doi:10.1016/s0960-894x(98)00012-2

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

Bioorg Med Chem Lett. 1998 Feb 3;8(3):281-4. doi: 10.1016/s0960-894x(98)00012-2.

Authors

T J Rosen¹, K J Coffman, S McLean, R T Crawford, D K Bryce, Y Gohda, M Tsuchiya, A Nagahisa, M Nakane, J A Lowe 3rd

Affiliation

¹ Central Research Division, Pfizer Inc., Groton, CT 06340, USA.

PMID: 9871670
DOI: 10.1016/s0960-894x(98)00012-2

Abstract

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.

MeSH terms

Animals
Capsaicin / antagonists & inhibitors
Cell Line
Guinea Pigs
Humans
Motor Activity / drug effects
Neurokinin-1 Receptor Antagonists*
Piperidines / chemical synthesis*
Piperidines / chemistry
Piperidines / pharmacology
Structure-Activity Relationship

Substances

Neurokinin-1 Receptor Antagonists
Piperidines
(2S,3S)-2-phenyl-3-((5-trifluoromethoxy-2-methoxy)benzylamino)piperidine
Capsaicin