Synthesis, in vitro binding profile, and autoradiographic analysis of [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine, a highly potent and selective nonpeptide substance P receptor antagonist radioligand.
The synthesis of a highly potent and selective NK1 receptor antagonist radioligand, [3H]-cis-3-[(2-methoxybenzyl)amino]-2-phenylpiperidine (6a) is described. The in vitro binding pharmacology and autoradiographic distribution of 6a in guinea pig brain following peripheral administration are also reported.
Rosen
T
T
Pfizer Central Research, Department of Medicinal Chemistry, Groton, Connecticut 06340.
Seeger
T F
TF
McLean
S
S
Desai
M C
MC
Guarino
K J
KJ
Bryce
D
D
Pratt
K
K
Heym
J
J
Chalabi
P M
PM
Windels
J H
JH
D000595:Amino Acid Sequence; D000818:Animals; D001345:Autoradiography; D001921:Brain / Q000378:metabolism; D006168:Guinea Pigs; D008297:Male; D008969:Molecular Sequence Data; D015288:Neurokinin A / Q000037:antagonists & inhibitors*; D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines / Q000138:chemical synthesis* / Q000378:metabolism / Q000494:pharmacology*; D011869:Radioligand Assay; D013237:Stereoisomerism; D013373:Substance P / Q000737:chemistry
D064729:Neurokinin-1 Receptor Antagonists; D010880:Piperidines; C080755:3-(2-methoxybenzylamino)-2-phenylpiperidine; D013373:Substance P; D015288:Neurokinin A