Activity and distribution of binding sites in brain of a nonpeptide substance P (NK1) receptor antagonist.
CP-96,345, a nonpeptide substance P antagonist, is selective for the tachykinin NK1 receptor. The compound binds to a single population of sites in guinea pig brain and potently inhibits substance P-induced excitation of locus ceruleus neurons. CP-96,345 should be a useful tool for studying the action of substance P in the central nervous system.
McLean
S
S
Department of Neuroscience, Central Research Division, Pfizer Inc., Groton, CT 06340.
Ganong
A H
AH
Seeger
T F
TF
Bryce
D K
DK
Pratt
K G
KG
Reynolds
L S
LS
Siok
C J
CJ
Lowe
J A
JA
Heym
J
J
D000200:Action Potentials; D000818:Animals; D001345:Autoradiography; D001665:Binding Sites; D001667:Binding, Competitive; D001713:Biphenyl Compounds / Q000378:metabolism* / Q000494:pharmacology; D001921:Brain / Q000000981:diagnostic imaging / Q000378:metabolism*; D003342:Corpus Striatum / Q000000981:diagnostic imaging / Q000378:metabolism*; D006168:Guinea Pigs; D006863:Hydrogen-Ion Concentration; D008297:Male; D011877:Radionuclide Imaging; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter / Q000037:antagonists & inhibitors* / Q000378:metabolism*; D018039:Receptors, Tachykinin; D013053:Spectrophotometry; D013373:Substance P / Q000378:metabolism; D015320:Tachykinins / Q000378:metabolism
D001713:Biphenyl Compounds; D018040:Receptors, Neurokinin-1; D017981:Receptors, Neurotransmitter; D018039:Receptors, Tachykinin; D015320:Tachykinins; D013373:Substance P; C066892:CP 96345