Role of the serotonin 5-HT2A receptor in the hyperlocomotive and hyperthermic effects of (+)-3,4-methylenedioxymethamphetamine

Herin, David V.; Liu, Shijing; Ullrich, Thomas; Rice, Kenner C.; Cunningham, Kathryn A.

doi:10.1007/s00213-004-2030-4

Cited by 70 publications

(69 citation statements)

References 40 publications

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“…The selectivity of the interaction between ketanserin and MDMA on verbal memory was also supported by the lack of any interactions between pretreatment and MDMA on safety measures such as blood pressure and body temperature. The latter finding is in line with a previous study that demonstrated that co-administration of ketanserin did not alter MDMA effects on physiological measures (ie, blood pressure, heart rate, and body temperature) and subjective measures (eg, well-being and positive mood) (Herin et al, 2005;Liechti et al, 2000). The selective interaction between ketanserin and MDMA effects on verbal memory may indicate differences in neural memory networks and differences in distributions of 5-HT 1A and 5-HT 2A receptors within these networks.…”

Section: Discussionsupporting

confidence: 92%

Blockade of 5-HT2 Receptor Selectively Prevents MDMA-Induced Verbal Memory Impairment

Wel

Kuypers

Theunissen

et al. 2011

Neuropsychopharmacol

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3,4-Methylenedioxymethamphetamine (MDMA) or 'ecstasy' has been associated with memory deficits during abstinence and intoxication. The human neuropharmacology of MDMA-induced memory impairment is unknown. This study investigated the role of 5-HT 2A and 5-HT 1A receptors in MDMA-induced memory impairment. Ketanserin is a 5-HT 2A receptor blocker and pindolol a 5-HT 1A receptor blocker. It was hypothesized that pretreatment with ketanserin and pindolol would protect against MDMA-induced memory impairment. Subjects (N ¼ 17) participated in a double-blind, placebo-controlled, within-subject design involving six experimental conditions consisting of pretreatment (T1) and treatment (T2). T1 preceded T2 by 30 min. T1-T2 combinations were: placebo-placebo, pindolol 20 mg-placebo, ketanserin 50 mg-placebo, placebo-MDMA 75 mg, pindolol 20 mg-MDMA 75 mg, and ketanserin 50 mg-MDMA 75 mg. Memory function was assessed at Tmax of MDMA by means of a word-learning task (WLT), a spatial memory task and a prospective memory task. MDMA significantly impaired performance in all memory tasks. Pretreatment with a 5-HT 2A receptor blocker selectively interacted with subsequent MDMA treatment and prevented MDMA-induced impairment in the WLT, but not in the spatial and prospective memory task. Pretreatment with a 5-HT 1A blocker did not affect MDMA-induced memory impairment in any of the tasks. Together, the results demonstrate that MDMA-induced impairment of verbal memory as measured in the WLT is mediated by 5-HT 2A receptor stimulation.

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Section: Discussionsupporting

confidence: 92%

Blockade of 5-HT2 Receptor Selectively Prevents MDMA-Induced Verbal Memory Impairment

Wel

Kuypers

Theunissen

et al. 2011

Neuropsychopharmacol

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“…The hypothermia-mediating populations of TA 1 R that modulate the influence of MDMA on core temperature are probably localized in thermoregulatory centers like medial optic area and arcuate hypothalamus (Borowsky et al, 2001; Har- greaves Bratincsák et al, 2008). Alternatively, they might be situated in monoaminergic neurons themselves (Mechan et al, 2002;Herin et al, 2005;Bexis and Docherty, 2008). Nonetheless, D 2 /D 3 , 5-HT 1A , and ␣ 2 -adrenergic autoreceptors are not involved in MDMA-induced hypothermia since antagonists did not modify its influence on core temperature (see Results) (Fig.…”

Section: Discussionmentioning

confidence: 99%

Genetic Deletion of Trace Amine 1 Receptors Reveals Their Role in Auto-Inhibiting the Actions of Ecstasy (MDMA)

Cara

Maggio²,

Aloisi³

et al. 2011

J. Neurosci.

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“…It has been described that local perfusion of the hypothalamus with 5-hydroxytryptophan (a 5-HT precursor) or fluoxetine (a 5-HT reuptake inhibitor) increases body temperature by increasing extracellular concentrations of 5-HT, which activate central 5-HT 2A receptors [20,21], although activation of these receptors in the peripheral system leads to hypothermia [22]. Additionally, an activation of 5-HT 1A receptors in the hypothalamus leads to hypothermia [23].…”

Section: Discussionmentioning

confidence: 99%

Serotonin is involved in the psychostimulant and hypothermic effect of 4-methylamphetamine in rats

Rubio

López-Arnau

Piccoli

et al. 2015

Neuroscience Letters

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Abstract4-methylamphetamine (4-MA) has recently emerged as a designer drug of abuse in Europe and it is consumed always with amphetamine. There have been reported some deaths and non-fatal intoxications related to 4-MA. We investigated the changes in locomotor activity and body temperature after 4-MA administration to male SpragueDawley rats. Our experiments were carried out at a normal or high ambient temperature. 4-MA (2.5 -10 mg/Kg, given subcutaneously) increased, in a dosedependent manner, the horizontal locomotor activity that was significantly reduced by ketanserin, p-cholorophenylalanine (pCPA) or haloperidol. In addition, we have studied the effect of 4-MA on core body temperature by means of an implanted electronic thermograph, enabling continuous measurement of body temperature. We observed a dose-dependent hypothermic response to 4-MA that reached a maximum 45 min after a single injection. We also evidenced slight tachyphylaxis to the hypothermic effect when 4-MA was administered four times in a 2 h interval. The pre-treatment of animals with pCPA or pindolol, but not with ketanserin, fully abolished the hypothermic effect of 4-MA. With all that, we conclude that hypothermia induced by 4-MA is due to the release of 5-HT which activates postsynaptic 5-HT 1A receptors.

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Role of the serotonin 5-HT2A receptor in the hyperlocomotive and hyperthermic effects of (+)-3,4-methylenedioxymethamphetamine

Cited by 70 publications

References 40 publications

Blockade of 5-HT2 Receptor Selectively Prevents MDMA-Induced Verbal Memory Impairment

Blockade of 5-HT2 Receptor Selectively Prevents MDMA-Induced Verbal Memory Impairment

Genetic Deletion of Trace Amine 1 Receptors Reveals Their Role in Auto-Inhibiting the Actions of Ecstasy (MDMA)

Serotonin is involved in the psychostimulant and hypothermic effect of 4-methylamphetamine in rats

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