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

✍ Scribed by Hank F. Kung; D. Andrew Stevenson; Zhi-Ping Zhuang; Mei-Ping Kung; Dana Frederick; Stephen D. Hurt

Publisher
John Wiley and Sons
Year
1996
Tongue
English
Weight
454 KB
Volume
23
Category
Article
ISSN
0887-4476

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✦ Synopsis

A new 5-HTIA receptor antagonist ligand, [3H]p-MPPF, 4-(2'-methoxy-)phenyl-l-[2'-(N-2-pyridyl)-p-fluorobenzamido]ethyl-piperazine, was prepared and characterized. It demonstrated high affinity and selectivity toward 5-HTlA receptors

(& = 0.34 t 0.12 nM and B, , = 145 t 35 fmol/mg protein in rat hippocampal membrane homogenates). The binding is not sensitive to 100 pM Gpp(NH)p. Initial autoradiography studies of rat brain sections exhibit regional localization consistent with the known 5-HTIA receptor distribution. This potential 5-HTI~ antagonist ligand may provide a powerful tool for 5-HTIA receptor pharmacology studies in the central nervous system.

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