High impact information on Lopac-Q-109

• The uptake of [3H]5HT was Na+ dependent and saturable (Kmapp: 166 +/- 15 nM, Vmax: 404 +/- 25 fmol/mg tissue, 30 min (diestrous); and Km: 165 +/- 39 nM, Vmax: 276 +/- 43 fmol/mg tissue, 30 min (estrous), n = 6), and was inhibited by imipramine, fluoxetine and 6-nitroquipazine (IC50: 2; 0.09 and 0.5 nM, respectively) [1].
• Nonlinear regression analysis of these curves was used to estimate the pKd-value of endogenous 5-HT and the 5-HT biophase concentration at the autoreceptor, in the absence and in the presence of 6-nitroquipazine and in the additional presence of metitepin or metergoline [2].
• Coadministration of carrier 6-nitroquipazine (5 mg/kg) significantly decreased the radioactivity in the hypothalamus, whereas that in the cerebellum and cerebral cortex was increased [3].
• In the caudate nucleus, however, where dopamine is the predominant monoamine (ratio of dopamine:5-HT:noradrenaline about 400:25:15) nomifensine (1, 10 microM) reduced the tritium accumulation to 65% whereas 6-nitroquipazine (1 microM) was ineffective [4].
• The effect of the catecholamine uptake inhibitor nomifensine and of the 5-hydroxytryptamine (5-HT) uptake blocker 6-nitroquipazine on the accumulation of [3H]-5-HT (0.1 microM, 60 min incubation) and [3H]-dopamine (0.1 microM, 30 min incubation) into slices of hippocampus and caudate nucleus of the rabbit was investigated [4].

Biological context of Lopac-Q-109

• The goal of these studies was to determine those positions on 6-nitroquipazine that could be derivatized without significantly decreasing the affinity of the drug for the binding site, so that radiolabels such as 123I, 76Br or 18F might be appended for in-vivo imaging studies of the 5-HT reuptake system [5].

Anatomical context of Lopac-Q-109

• Cortical slices were preincubated with [3H]5-HT in the presence of the selective noradrenaline uptake inhibitor, maprotiline (to avoid false labelling of noradrenergic axon terminals), and the superfused with solution containing the 5-HT reuptake inhibitor, 6-nitroquipazine [6].
• Eleven 4-substituted derivatives of 6-nitroquipazine were synthesized and evaluated for their abilities to displace [3H]citalopram binding to the rat cortical synaptic membranes [7].
• Nine derivatives of 6-nitroquipazine were synthesized and tested for their potential abilities to displace [3H]citalopram binding to the rat cortical membranes [8].

Associations of Lopac-Q-109 with other chemical compounds

• The decrease in the 5-HT content caused by 4, alpha-dimethyl-m-tyramine (H 77/77) is antagonized by DU 24565 at 1 mg/kg orally, without any effect on the depletion of catecholamines [9].
• The radioactivity in the hypothalamus and cerebral cortex after injection of 3H-paroxetine was significantly decreased by treatment with 6-nitroquipazine or paroxetine [10].

Gene context of Lopac-Q-109

• We report here on the synthesis and evaluation of SERT and 5-HT(1A) receptor affinity of long-chain arylpiperazines obtained either by modifying 6-nitroquipazine into a long-chain arylpiperazine or by inserting a modified 6-nitroquipazine moiety or other structures endowed with SERT affinity into a long-chain arylpiperazine with 5-HT(1A) affinity [11].

References