New 5-HT1A receptor antagonist: [3H]p-MPPF.
A new 5-HT1A receptor antagonist ligand, [3H]p-MPPF, 4-(2'-methoxy-)-phenyl-1-[2'-(N-2"-pyridyl)-p-fluorobenzamido] ethyl-piperazine, was prepared and characterized. It demonstrated high affinity and selectivity toward 5-HT1A receptors (Kd = 0.34 +/- 0.12 nM and Bmax = 145 +/- 35 fmol/mg protein in rat hippocampal membrane homogenates). The binding is not sensitive to 100 microM Gpp(NH)p. Initial autoradiography studies of rat brain sections exhibit regional localization consistent with the known 5-HT1A receptor distribution. This potential 5-HT1A antagonist ligand may provide a powerful tool for 5-HT1A receptor pharmacology studies in the central nervous system.
Kung
H F
HF
Department of Radiology, University of Pennsylvania, Philadelphia 19104, USA.
Stevenson
D A
DA
Zhuang
Z P
ZP
Kung
M P
MP
Frederick
D
D
Hurt
S D
SD
D000631:Aminopyridines / Q000378:metabolism*; D000818:Animals; D001667:Binding, Competitive; D006624:Hippocampus / Q000378:metabolism*; D010879:Piperazines / Q000378:metabolism*; D011869:Radioligand Assay; D051381:Rats; D012702:Serotonin Antagonists / Q000378:metabolism*; D014316:Tritium
D000631:Aminopyridines; D010879:Piperazines; D012702:Serotonin Antagonists; D014316:Tritium; C099463:4-(2' methoxyphenyl)-1-(2'-(N-(2''-pyridinyl)-4-fluorobenzamido)ethyl)piperazine