Bufotenine esters.

R A Glennon; P K Gessner; D D Godse; B J Kline

doi:10.1021/jm00197a025

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Bufotenine esters.

R A Glennon·P K Gessner·D D Godse·B J Kline

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Abstract

Bufotenine (5-hydroxy-N,N-dimethyltryptamine) has been reported to be behaviorally inactive or only very weakly active in man and animals; this may be a consequence of its low partition coefficient and resultant inability to penetrate the blood--brain barrier. The acetyl, propionyl, butyryl, isobutyryl, and pivalyl esters of bufotenine were prepared for future pharmacological evaluation. Unexpectedly, it was found that these esters all possess a relatively high affinity for the serotonin receptors of the isolated rat stomach fundus preparation. A semiquantitative chromatographic measurement of ester hydrolysis suggests that extensive hydrolysis of the esters to bufotenine does not occur under the conditions of the affinity assay.

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Animals Bufotenin Esters Female Hydrolysis In Vitro Techniques Male Muscle Contraction Muscle, Smooth Rats Receptors, Serotonin Serotonin Structure-Activity Relationship Journal Article Research Support, U.S. Gov't, P.H.S.

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R A Glennon, P K Gessner, D D Godse, B J Kline. 1979. Bufotenine esters.. https://doi.org/10.1021/jm00197a025

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