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.
Rosen
T J
TJ
Central Research Division, Pfizer Inc., Groton, CT 06340, USA.
Coffman
K J
KJ
McLean
S
S
Crawford
R T
RT
Bryce
D K
DK
Gohda
Y
Y
Tsuchiya
M
M
Nagahisa
A
A
Nakane
M
M
Lowe
J A
JA
D000818:Animals; D002211:Capsaicin / Q000037:antagonists & inhibitors; D002460:Cell Line; D006168:Guinea Pigs; D006801:Humans; D009043:Motor Activity / Q000187:drug effects; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D013329:Structure-Activity Relationship
D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines; C099414:(2S,3S)-2-phenyl-3-((5-trifluoromethoxy-2-methoxy)benzylamino)piperidine; D002211:Capsaicin