New 5-HT1A receptor antagonist: [H-3]p-MPPF

被引：0
作者：
Kung, HF
Stevenson, A
Zhuang, ZP
Kung, MP
Frederick, D
Hurt, SD
机构：
[1] UNIV PENN,DEPT PHARMACOL,PHILADELPHIA,PA 19104
[2] DUPONT CO INC,NEN,MED PROD,BOSTON,MA 02118
来源：
SYNAPSE | 1996年 / 23卷 / 04期
关键词：
D O I：
10.1002/(SICI)1098-2396(199608)23:4<344::AID-SYN13>3.0.CO;2-X
中图分类号：
Q189 [神经科学];
学科分类号：
071006 ;
摘要：
A new 5-HT1A receptor antagonist ligand, [H-3]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 (K-d=0.34+/-0.12 nM and B-max=145+/-35 fmol/mg protein in rat hippocampal membrane homogenates). The binding is not sensitive to 100 mu M 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. (C) 1996 Wiley-Liss, Inc.
引用
收藏
页码：344 / 346
页数：3
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