Abstract
Two low-molecular-weight compounds were isolated from the parotid gland secret of the toad Bufo bufo, which by absorption spectra and HPLC-MS/MS chromatography data correspond to di- and trimethyl derivatives of serotonin (5-hydorxytryptamine): bufotenine (confirmed by counter synthesis) and bufotenidine (5-HTQ). In experiments on competitive radioligand binding, these compounds showed a higher affinity and selectivity for neuronal α7 nicotinic acetylcholine receptors compared with the muscular cholinergic receptors. The most efficient compound in terms of binding value was bufotenine, the efficiency of 5-HTQ was an order of magnitude lower, and the minimal activity was exhibited by serotonin.
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Original Russian Text © E.V. Kryukova, D.S. Lebedev, I.A. Ivanov, D.A. Ivanov, V.G. Starkov, V.I. Tsetlin, Yu.N. Utkin, 2017, published in Doklady Akademii Nauk, 2017, Vol. 472, No. 4, pp. 483–486.
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Kryukova, E.V., Lebedev, D.S., Ivanov, I.A. et al. N-methyl serotonin analogues from the Bufo bufo toad venom interact efficiently with the α7 nicotinic acetylcholine receptors. Dokl Biochem Biophys 472, 52–55 (2017). https://doi.org/10.1134/S1607672917010136
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DOI: https://doi.org/10.1134/S1607672917010136