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• W1975492041 abstract "GR128107 (3-(1-acetyl-3-methyl-piperidine)-5-methoxyindole) has previously been reported to be a competitive melatonin receptor antagonist in blocking melatonin inhibition of [3H]-dopamine release from rabbit retina, a response mediated by the MT2 receptor subtype. GR128107, like melatonin, induced a rapid (maximum response in 60–90 min) pigment aggregation in a clonal line of Xenopus laevis melanophores. GR128107 behaved as a partial agonist (pEC50 8.58±0.03, n=3) with an Emax of 0.83 (relative to melatonin, pEC50 10.09±0.03, n=3). The concentration-response curve for pigment granule aggregation to both melatonin and GR128107 was displaced in a parallel, rightward manner by melatonin receptor antagonists with very similar potencies; estimated pKB RJ252 (against melatonin 4.60/against GR128107 4.54) <GR135533 (6.40/6.14) < Luzindole (6.45/6.49) < S20929 (6.58/6.65) < 4-P-PDOT (6.73/6.85). Both melatonin- and GR128107-induced pigment granule aggregation was prevented by pre-treatment of melanophores with pertussis toxin (10–1000 ng ml−1). Prolonged pre-treatment of melanophores with melatonin desensitized the pigment aggregation response to GR128107. In desensitized cells, the maximal aggregation produced by GR128107 was only 0.27±0.01 (n=4) and the pEC50 was reduced (vehicle 8.57±0.12; melatonin pre-treated 7.84±0.09, n=4). The maximal response to melatonin in desensitized melanophores was unchanged but the pEC50 was reduced (vehicle 10.49±0.03; melatonin pre-treated 9.83±0.04, n=4). These results demonstrate that GR128107 induces pigment granule aggregation in Xenopus melanophores by activating a cell membrane melatonin receptor coupled via a pertussis toxin-sensitive G-protein. The partial agonist activity of GR128107 in melanophores may be apparent because of the very high density of melatonin receptors in these cells (Bmax 1223 fmol mg protein−1) compared to the low density of sites in rabbit retina (Bmax 3.1 fmol mg protein−1). This suggestion is supported by the finding that GR128107, like melatonin, acted as a full agonist and inhibited forskolin-stimulation of cyclic AMP accumulation in NIH-3T3 cells expressing a high density of human mt1 or MT2 receptors. British Journal of Pharmacology (1999) 126, 1237–1245; doi:10.1038/sj.bjp.0702404" @default.
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• W1975492041 date "1999-03-01" @default.
• W1975492041 modified "2023-10-17" @default.
• W1975492041 title "The putative melatonin receptor antagonist GR128107 is a partial agonist on<i>Xenopus laevis</i>melanophores" @default.
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• W1975492041 doi "https://doi.org/10.1038/sj.bjp.0702404" @default.
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