The effect of MDMA (“Ecstasy”) and its optical isomers on schedule-controlled responding in mice

Glennon, Richard A.; Little, Patrick; Rosecrans, John A.; Yousif, Mamoun

doi:10.1016/0091-3057(87)90141-9

Cited by 32 publications

(8 citation statements)

References 4 publications

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“…The current study used racemic compounds since these would be the form in which people both obtain and misuse them. While Schmidt et al (1986) reported that (+)-MDMA and (-)-MDMA were equipotent in releasing 5-HT in vitro, evidence from behavioural studies indicates that in vivo, the (+ )-enantiomer is as much as fourfold more potent (Hiramatsu et al, 1989;Glennon et al, 1987). Similarly, (+ )-MDA is more potent than (-)-MDA in evoking 5-HT-mediated behaviour (Hiramatsu et al, 1989).…”

Section: Discussionmentioning

confidence: 99%

The hyperthermic and neurotoxic effects of ‘Ecstasy’ (MDMA) and 3,4 methylenedioxyamphetamine (MDA) in the Dark Agouti (DA) rat, a model of the CYP2D6 poor metabolizer phenotype

Colado¹,

Williams²,

Green

1995

British J Pharmacology

153

100

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1 The effect of administration of 3,4-methylenedioxymethamphetamine (MDMA or 'Ecstasy') and its N-demethylated product, 3,4-methylenedioxyamphetamine (MDA) on both rectal temperature and long term neurotoxic loss of cerebral 5-hydroxytryptamine (5-HT) has been studied in male and female Dark Agouti (DA) rats. The female metabolizes debrisoquine more slowly than the male and its use has been suggested as a model of the human debrisoquine 4-hydroxylase poor

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Section: Discussionmentioning

confidence: 99%

The hyperthermic and neurotoxic effects of ‘Ecstasy’ (MDMA) and 3,4 methylenedioxyamphetamine (MDA) in the Dark Agouti (DA) rat, a model of the CYP2D6 poor metabolizer phenotype

Colado¹,

Williams²,

Green

1995

British J Pharmacology

153

100

View full text Add to dashboard Cite

show abstract

“…Thus, R(Ϫ)-MDMA may simply be less potent than S(ϩ)-or racemic MDMA in terms of discriminative stimulus effects. Likewise, the lethal effects of R(Ϫ)-MDMA are less potent than those of S(ϩ)-and racemic MDMA in mice (Fantegrossi et al, 2003), and R(Ϫ)-MDMA is 4-fold less potent than S(ϩ)-and racemic MDMA in suppressing operant responding in the mouse (Glennon et al, 1987). Such potency differences are not universally reported, however, because head twitch behavior elicited by S(ϩ)-and R(Ϫ)-MDMA occurs over a comparable dose range (Fantegrossi et al, 2005).…”

Section: Discussionmentioning

confidence: 99%

Discriminative Stimulus Effects of 3,4-Methylenedioxymethamphetamine and Its Enantiomers in Mice: Pharmacokinetic Considerations

Fantegrossi

Murai²,

Mathúna³

et al. 2009

J Pharmacol Exp Ther

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3,4-Methylenedioxymethamphetamine (MDMA) is a drug of abuse with mixed stimulant-and hallucinogen-like effects. The aims of the present studies were to establish discrimination of S(ϩ)-MDMA, R(Ϫ)-MDMA, or their combination as racemic MDMA in separate groups of mice to assess cross-substitution tests among all three compounds, to determine the time courses of the training doses, to assess pharmacokinetic variables after single injections and after cumulative dosing, and to define the metabolic dispositions of MDMA enantiomers and their metabolites. All three forms of MDMA served as discriminative stimuli, and with the exception of R(Ϫ)-MDMA in mice trained to discriminate the racemate, compounds substituted for one another. The onset of interoceptive effects for S(ϩ)-MDMA and racemic MDMA were faster than for R(Ϫ)-MDMA, and the duration of discriminative stimulus effects was shortest for R(Ϫ)-MDMA. S(ϩ)-MDMA and its metabolites were found in higher concentrations than R(Ϫ)-MDMA and its metabolites after a bolus dose of racemic MDMA. The N-dealkylation pathway is favored in mouse plasma with MDA as the main metabolite formed. Cumulative doses of MDMA lead to higher plasma concentrations compared with an equivalent single dose. 3,4-Methylenedioxyamphetamine (MDA) concentrations are lower after the cumulative dose compared with the single dose, which, coupled with the nonlinearity observed in MDMA pharmacokinetics after increased doses of racemic MDMA, suggests autoinhibition (or saturation) of MDMA metabolism in mice. In total, these studies suggest that the discriminative stimulus effects of racemic MDMA are perhaps driven by accumulation of S(ϩ)-MDMA and S(ϩ)-MDA in the mouse.

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“…In agreement with our results, previous studies have reported detrimental effects of acute MDMA on instrumental responding in different laboratory animals. Thus, rate-decreasing effects of MDMA on FR schedules of food reinforcement have been observed in pigeons (Nader et al 1989), rats (Li et al 1989;Nagilla et al 1998) and mice (Glennon et al 1987;Miczek and Haney 1994). Performance under PR schedules is also disrupted by acute doses of MDMA (1.0 mg/kg) in monkeys (Frederick and Paule 1997) and in rats (3.2 and 5.6 mg/kg; Laraway et al 2003).…”

Section: Discussionmentioning

confidence: 88%

Effects of repeated MDMA administration on the motivation for palatable food and extinction of operant responding in mice

et al. 2010

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The effect of MDMA (“Ecstasy”) and its optical isomers on schedule-controlled responding in mice

Cited by 32 publications

References 4 publications

The hyperthermic and neurotoxic effects of ‘Ecstasy’ (MDMA) and 3,4 methylenedioxyamphetamine (MDA) in the Dark Agouti (DA) rat, a model of the CYP2D6 poor metabolizer phenotype

The hyperthermic and neurotoxic effects of ‘Ecstasy’ (MDMA) and 3,4 methylenedioxyamphetamine (MDA) in the Dark Agouti (DA) rat, a model of the CYP2D6 poor metabolizer phenotype

Discriminative Stimulus Effects of 3,4-Methylenedioxymethamphetamine and Its Enantiomers in Mice: Pharmacokinetic Considerations

Effects of repeated MDMA administration on the motivation for palatable food and extinction of operant responding in mice

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