Synthesis and structure-activity relationships of CP-122,721, a second-generation NK-1 receptor antagonist. 1998

T J Rosen, and K J Coffman, and S McLean, and R T Crawford, and D K Bryce, and Y Gohda, and M Tsuchiya, and A Nagahisa, and M Nakane, and J A Lowe
Central Research Division, Pfizer Inc., Groton, CT 06340, USA.

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.

UI MeSH Term Description Entries
D009043 Motor Activity Body movements of a human or an animal as a behavioral phenomenon. Activities, Motor,Activity, Motor,Motor Activities
D010880 Piperidines A family of hexahydropyridines.
D002211 Capsaicin An alkylamide found in CAPSICUM that acts at TRPV CATION CHANNELS. 8-Methyl-N-Vanillyl-6-Nonenamide,Antiphlogistine Rub A-535 Capsaicin,Axsain,Capsaicine,Capsicum Farmaya,Capsidol,Capsin,Capzasin,Gelcen,Katrum,NGX-4010,Zacin,Zostrix,8 Methyl N Vanillyl 6 Nonenamide,NGX 4010,NGX4010
D002460 Cell Line Established cell cultures that have the potential to propagate indefinitely. Cell Lines,Line, Cell,Lines, Cell
D006168 Guinea Pigs A common name used for the genus Cavia. The most common species is Cavia porcellus which is the domesticated guinea pig used for pets and biomedical research. Cavia,Cavia porcellus,Guinea Pig,Pig, Guinea,Pigs, Guinea
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D013329 Structure-Activity Relationship The relationship between the chemical structure of a compound and its biological or pharmacological activity. Compounds are often classed together because they have structural characteristics in common including shape, size, stereochemical arrangement, and distribution of functional groups. Relationship, Structure-Activity,Relationships, Structure-Activity,Structure Activity Relationship,Structure-Activity Relationships
D064729 Neurokinin-1 Receptor Antagonists Compounds that inhibit or block the activity of NEUROKININ-1 RECEPTORS. Neurokinin 1 Receptor Antagonist,Neurokinin-1 Receptor Antagonist,Neurokinin-1 Receptor Blocker,Neuroleukin-1 Receptor Blocker,Substance P Receptor Antagonist,Substance P Receptor Blocker,Tachykinin Receptor 1 Antagonist,Tachykinin Receptor 1 Blocker,Neurokinin-1 Receptor Blockers,Neuroleukin-1 Receptor Blockers,Substance P Receptor Antagonists,Substance P Receptor Blockers,Tachykinin Receptor 1 Antagonists,Tachykinin Receptor 1 Blockers,Antagonist, Neurokinin-1 Receptor,Antagonists, Neurokinin-1 Receptor,Blocker, Neurokinin-1 Receptor,Blocker, Neuroleukin-1 Receptor,Blockers, Neurokinin-1 Receptor,Blockers, Neuroleukin-1 Receptor,Neurokinin 1 Receptor Antagonists,Neurokinin 1 Receptor Blocker,Neurokinin 1 Receptor Blockers,Neuroleukin 1 Receptor Blocker,Neuroleukin 1 Receptor Blockers,Receptor Antagonist, Neurokinin-1,Receptor Antagonists, Neurokinin-1,Receptor Blocker, Neurokinin-1,Receptor Blocker, Neuroleukin-1,Receptor Blockers, Neurokinin-1,Receptor Blockers, Neuroleukin-1

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