Erowid References Database
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Ransom RW, Asarch KB, Shih JC.
“[3H] 1-[2-(4-Aminophenyl)Ethyl]-4-(3-Trifluoromethylphenyl)Piperazine: A Selective Radioligand for 5-HT1A Receptors in Rat Brain”.
Journal of Neurochemistry. 1986;46:68-75.
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Abstract
1-[2-(4-Aminophenyl)ethyl]-4-(3-trifluoromethylphenyl)piperazine (PAPP) inhibits [3H]5-hydroxytryptamine (5-HT, serotonin) binding to 5-HT,A and 5-HT1B sites in rat brain with apparent equilibrium dissociation constants (KD) Of 2.9 and 328 nM, respectively. [3H]PAPP was synthesized, its binding to central serotonin receptors was examined, and its potential usefulness as a 5-HT'A receptor radioligand was evaluated, With either 10 mcM 5-HT or 1 mcM 8-hydroxy-2-(di-n-propylamino)tetralin to define nonspecific binding, [3H]PAPP bound to a single class of sites in rat cortical membranes with a KD of 1.6 nM and a maximal binding density (Bmax.) of 162 fmol/mg of protein. d-Lysergic acid diethylamide and 5-HT, two nonselective inhibitors of [3H]5-HT binding, displaced 1 nM [3H]PAPP with a potency that matched their affinity for 5-HT' receptors. Spiperone and 8-hydroxy-2-(di-n-propylamino)tetralin, two compounds that discriminate [3H]5-HT binding to 5-HT1A and 5-HT1B sites, inhibited [3H]PAPP binding in accordance with their much higher affinities for the 5-HT1A receptor subtype. Furthermore, the ability of N-(m-trifluoromethylypheny)piperazine and ketanserin to inhibit [3H}PAPP binding reflected their low affinites for the 5-HT1A receptor. Several nonserotonergic compounds were also found to be relatively poor displceres of [3H]PAPP binding. The regional distribution of serotonin-sesitive [3H]PAPP sties correlated with the densities of 5-HT1A receptors in the cortex, hippocampus, corpus striatum, and cerebellum of the rat. These results indicated that [3H]PAPP binds selectively and with high affinity to 5-HT1A receptor sites in rat brain.
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