Ueber Bufonin und Bufotalin, die wirksamen Bestandtheile des Krötenhautdrüsensecretes

Faust, Edwin Stanton

doi:10.1007/bf01929651

Cited by 29 publications

(1 citation statement)

References 5 publications

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“…The use of hallucinogenic compounds like bufotenin was classically described by the German pharmacologist Louis Lewin (Lewin 1924 ). The older literature on toxins in toad extracts was collected by Faust (Faust 1902 ): fatal intoxications of adult men by toads as early as 1575 were reported by Ambroise Paré (see (Faust 1902 )). Faust called the toxin “bufonin” which we now regard as “bufotenin” or “bufotenine” (Faust 1902 ).…”

Section: Introductionmentioning

confidence: 99%

Cardiovascular effects of bufotenin on human 5-HT4 serotonin receptors in cardiac preparations of transgenic mice and in human atrial preparations

Neumann

Schulz

Fehse

et al. 2023

Naunyn-Schmiedeberg's Arch Pharmacol

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It is unclear whether bufotenin (= N,N-dimethyl-serotonin = 5-hydroxy-N,N-dimethyl-tryptamine), a hallucinogenic drug, can act on human cardiac serotonin 5-HT4 receptors. Therefore, the aim of the study was to examine the cardiac effects of bufotenin and for comparison tryptamine in transgenic mice that only express the human 5-HT4 receptor in cardiomyocytes (5-HT4-TG), in their wild-type littermates (WT) and in isolated electrically driven (1 Hz) human atrial preparations. In 5-HT4-TG, we found that both bufotenin and tryptamine enhanced the force of contraction in left atrial preparations (pD2 = 6.77 or 5.5, respectively) and the beating rate in spontaneously beating right atrial preparations (pD2 = 7.04 or 5.86, respectively). Bufotenin (1 µM) increased left ventricular force of contraction and beating rate in Langendorff perfused hearts from 5-HT4-TG, whereas it was inactive in hearts from WT animals, as was tryptamine. The positive inotropic and chronotropic effects of bufotenin and tryptamine were potentiated by an inhibitor of monoamine oxidases (50 µM pargyline). Furthermore, bufotenin concentration- (0.1–10 µM) and time-dependently elevated force of contraction in isolated electrically stimulated musculi pectinati from the human atrium and these effects were likewise reversed by tropisetron (10 µM). We found that bufotenin (10 µM) increased the phosphorylation state of phospholamban in the isolated perfused hearts, left and right atrial muscle strips of 5-HT4-TG but not from WT and in isolated human right atrial preparations. In summary, we showed that bufotenin can increase the force of contraction via stimulation of human 5-HT4 receptors transgenic mouse cardiac preparations but notably also in human atrial preparations.

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Section: Introductionmentioning

confidence: 99%

Cardiovascular effects of bufotenin on human 5-HT4 serotonin receptors in cardiac preparations of transgenic mice and in human atrial preparations

Neumann

Schulz

Fehse

et al. 2023

Naunyn-Schmiedeberg's Arch Pharmacol

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Neuere Arbeiten zur chemischen Konstitution der herzaktiven Krötengifte

Sellhorn

1952

Archiv der Pharmazie

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Über herzaktive Krötengifte (Bufogenine). 2. Mitteilung. Konstitution de Bufalins

Meyer

1949

Helvetica Chimica Acta

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Abbau von Bufalin‐acetat mit KMnO4 in Aceton gab 3β‐Acetoxy‐14‐oxy‐14‐iso‐ätiocholansäure und 3β‐Acetoxy‐14‐oxy‐14‐iso‐20‐keto‐pregnan‐21‐säure‐Lacton‐(21 → 14). Damit ist es zum ersten Mal1) geglückt, ein herzaktives Krötengift in zwei Steroidderivate bekannter Struktur überzuführen und einwandfrei zu zeigen, dass Bufalin bis auf die Natur des Lactonringes auch räumlich genau gleich gebaut ist wie Digitoxigenin.

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Ueber Bufonin und Bufotalin, die wirksamen Bestandtheile des Krötenhautdrüsensecretes

Cited by 29 publications

References 5 publications

Cardiovascular effects of bufotenin on human 5-HT4 serotonin receptors in cardiac preparations of transgenic mice and in human atrial preparations

Cardiovascular effects of bufotenin on human 5-HT4 serotonin receptors in cardiac preparations of transgenic mice and in human atrial preparations

Neuere Arbeiten zur chemischen Konstitution der herzaktiven Krötengifte

Über herzaktive Krötengifte (Bufogenine). 2. Mitteilung. Konstitution de Bufalins

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