Blood and urine levels of N,N-dimethyltryptamine following administration of psychoactive dosages to human subjects

Kaplan, J. Martin; Mandel, L; Stillman, R. C.; Walker, Robert; Vandenheuvel, W.J.A.; Gillin, J. Christian; Wyatt, Richard Jed

doi:10.1007/bf00421376

Cited by 60 publications

(35 citation statements)

References 14 publications

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“…While oxidative deamination appears to be a major metabolic route, N-oxidation has also been identified as an important metabolic pathway of DMT both in vitro (Fish et al, 1955;Kaplan et al, 1974;Barker et al, 1980) and in vivo in rodents and rabbits (Sitaram et al, 1987a-c;Sitaram and McLeod, 1990). It is of interest to note that DMT-NO does not appear to be a substrate for MAO (Fish et al, 1955;Sitaram et al, 1987c).…”

Section: Major Constituents and Metabolites Of Ayahuasca In Urinementioning

confidence: 96%

“…or intravenous DMT administered without MAO inhibition is rapidly cleared from blood (Kaplan et al, 1974;Gillin et al, 1976) with less than 0.1% of the parent DMT being recoverable in human urine within a 24-hour collection period (Kaplan et al, 1974;Strassman et al, 1994). In vivo animal studies have also demonstrated a very rapid clearance of DMT from various tissues such as plasma, brain and liver (Cohen and Vogel, 1972;Mandel et al, 1977;Sitaram et al, 1987a, b).…”

Section: Major Constituents and Metabolites Of Ayahuasca In Urinementioning

confidence: 97%

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Methodology for and the determination of the major constituents and metabolites of the Amazonian botanical medicine ayahuasca in human urine

McIlhenny

Riba

Barbanoj

et al. 2010

Biomedical Chromatography

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Ayahuasca, also known as caapi or yage among various South American groups, holds a highly esteemed and millennia-old position in these cultures' medical and religious pharmacopeia. There is now an increasing interest in the potential for modern medical applications of ayahuasca, as well as concerns regarding its increasing potential for abuse. Toxicological and clinical research to address these issues will require information regarding its metabolism and clearance. Thus, a rapid, sensitive and specific method for characterization and quantitation of the major constituents and of the metabolites of ayahuasca in urine is needed. The present research provides a protocol for conducting such analyses. The characteristics of the method, conducted by sample dilution and using HPLC-electrospray ionization (ESI)-selected reaction monitoring (SRM)-tandem mass spectrometry, are presented. The application of the analytical protocol to urine samples collected from three individuals that were administered ayahuasca has also been demonstrated. The data show that the major metabolite of the hallucinogenic component of ayahuasca, N,N-dimethyltryptamine (DMT), is the corresponding N-oxide, the first time this metabolite has been described in in vivo studies in humans. Further, very little DMT was detected in urine, despite the inhibition of monoamine oxidase afforded by the presence of the harmala alkaloids in ayahuasca. The major harmala alkaloid excreted was tetrahydroharmine. Other excretion products and metabolites were also identified and quantified. The method described would be suitable for use in further toxicological and clinical research on ayahuasca.

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Section: Major Constituents and Metabolites Of Ayahuasca In Urinementioning

confidence: 96%

Section: Major Constituents and Metabolites Of Ayahuasca In Urinementioning

confidence: 97%

Methodology for and the determination of the major constituents and metabolites of the Amazonian botanical medicine ayahuasca in human urine

McIlhenny

Riba

Barbanoj

et al. 2010

Biomedical Chromatography

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“…DMT has been shown to produce psychedelic effects when administered to normal subjects (Szara, 1956;Kaplan, Mandel, Stillman, Walker, Van den Heuval, Gillin & Wyatt, 1974). DMT can be synthesized in the tissues of both man and animals (Axelrod, 1962;Mandell & Morgan, 1971;Saavedra & Axelrod, 1972;Mandel, Prasad, Lopez-Ramos & Walker, 1977), and no apparent tolerance seems to develop on repeated administration of this drug to the cat (Gillin, Cannon & Magyar, 1973) or squirrel monkey (Cole & Pieper, 1973).…”

Section: Introductionmentioning

confidence: 99%

BEHAVIOURAL CHANGES INDUCED BY N,N‐DIMETHYLTRYPTAMINE IN RODENTS

Jenner¹,

Marsden²,

Thanki³

1980

British J Pharmacology

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I N,N-Dimethyltryptamine (DMT) in pargyline pretreated rodents induced a dose-dependent behavioural syndrome consisting of hyperactivity, prostration and hindlimb abduction, mild tremor, Straub tail, retropulsion and jerking. 2 In rats pretreated with pargyline, the behavioural syndrome induced by DMT differed from that induced by L-tryptophan or quipazine, in the lack of forepaw treading and head-weaving and in the presence of only mild tremor. 3 The hyperactivity component of the DMT-induced behavioural syndrome in pargyline-pretreated mice was potentiated by cyproheptadine, methergoline, and mianserin, inhibited by cinanserin, haloperidol, pimozide, methiothepin and propranolol, and not affected by 501C67-sulphate and methysergide. 4 The maximal behavioural changes induced by DMT in rats, other than hyperactivity, were unaffected by pretreatment with cyproheptadine, methysergide, and cinanserin. However, propranolol reduced the intensity of all behavioural effects apart from body jerking, and methergoline decreased the duration of prostration. Phenoxybenzamine and haloperidol, in contrast, enhanced prostration. 5 DMT plus pargyline did not induce circling behaviour in mice with a unilateral 6-hydroxydopamine lesion of the nigro-striatal pathway. 6 The DMT-induced behavioural syndrome appears to consist of two components, (a) hyperactivity and (b) other behavioural changes. They differ in their response to drugs affecting brain monoamines. The hyperactivity component may be expressed via dopamine mechanisms, but the other behavioural changes are not. The two behaviours do not respond consistently to drugs believed to alter brain 5-hydroxytryptamine function.

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“…This approach is probably appropriate since about 40% of the exogenous bufotenine (in rats) is excreted in the urine either un changed or. conjugated (Sanders and Bush, 1967) while only about 0.7% of exogeneous DMT is recovered from the urine of humans (Kaplan et al, 1974). However, since only about 1.8% of exogenous DMT can be detected in the blood, it is possible that if small amounts of endogenous DMT were produced they might not be detectable in the urine or in the blood by present techniques (Kaplan et al, 1974).…”

Section: Dimethyltryptaminementioning

confidence: 89%

A Review of Nicotinic Acid, N-Methylated Indoleamines and Schizophrenia

Luchins¹,

Ban

Lehmann

1978

Int Pharmacopsychiatry

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The hypothesis that endogenously formed, N-methylated metabolites of indoleamines may play a role in the pathogenesis of schizophrenia was reviewed. Although N-methylated indoleamines can be produced in vivo and have significant psychotomimetic effects, there is little evidence for a specific increase in the méthylation of indoleamines in schizophrenic patients. It was noted that even if the relationship between schizophrenia and N-methylated indoleamines had existed, nicotinic acid would not be an appropriate therapeutic agent.

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Blood and urine levels of N,N-dimethyltryptamine following administration of psychoactive dosages to human subjects

Cited by 60 publications

References 14 publications

Methodology for and the determination of the major constituents and metabolites of the Amazonian botanical medicine ayahuasca in human urine

Methodology for and the determination of the major constituents and metabolites of the Amazonian botanical medicine ayahuasca in human urine

BEHAVIOURAL CHANGES INDUCED BY N,N‐DIMETHYLTRYPTAMINE IN RODENTS

A Review of Nicotinic Acid, N-Methylated Indoleamines and Schizophrenia

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