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N-methyl serotonin analogues from the Bufo bufo toad venom interact efficiently with the α7 nicotinic acetylcholine receptors.

E V Kryukova, D S Lebedev, I A Ivanov, D A Ivanov, V G Starkov, V I Tsetlin, Yu N Utkin

Doklady. Biochemistry and biophysics 2017 DOI: 10.1134/s1607672917010136 (opens in new tab)

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AI-extracted from the abstract
Characteristics Peer reviewed
Topics Serotonin 5-MeO-DMT
Keywords Cell line Animals Bufo bufo Rats Amphibian venoms Ligands Protein binding
Key points Bufotenine and bufotenidine (5-HTQ), isolated from Bufo bufo parotid secretion, bound neuronal alpha7 nicotinic acetylcholine receptors with higher affinity and selectivity than muscular cholinergic receptors. Bufotenine was the most efficient binder, 5-HTQ was an order of magnitude lower, and serotonin showed minimal activity.

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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