The effect of psychostimulants on [3H]dopamine uptake and release in rat brain synaptic vesicles

Schwartz, K.; Weizman, Abraham; Rehavi, Moshe

doi:10.1007/s00702-005-0383-4

Cited by 15 publications

(4 citation statements)

References 14 publications

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“…Methamphetamine leads to reverse transport of cytosolic dopamine and induces conformational changes in the DAT, further facilitating cytosolic dopamine release [67]. Methamphetamine causes pH-driven release of dopamine from presynaptic vesicles and prevents reuptake of dopamine into presynaptic vesicles by binding to the VMAT-2 vesicular transporter [66,68]. Methamphetamine is a more potent releaser of dopamine than cocaine at equivalent concentrations [69,70].…”

Section: Discussionmentioning

confidence: 99%

Cocaine Versus Methamphetamine Users in the Emergency Department: How Do They Differ?

Richards¹,

Tabish²,

Wang³

et al. 2017

J Alcohol Drug Depend

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Background: Stimulant use disorder is a worldwide problem. Users present to the ED for diverse reasons including trauma, chest and abdominal pain, altered mental status, stroke, suicidality, and skin infection. Objective: To determine what differences exist between stimulant users. Methods: We compared Stimulant users presenting to an urban ED Level I trauma center over a 3-month period with toxicology screens positive for cocaine and/or methamphetamine. Results: Of 718 subjects (465 male, 253 female), 610 (85%) were positive for methamphetamine, 80 (11%) cocaine, and 28 (4%) both. Significant racial differences existed, but not for age, gender, and insurance status. Ethanol co-ingestion was higher for cocaine users, otherwise no significant differences were detected for laboratory values and maximum heart rate, and systolic/diastolic blood pressure. For presenting complaint, the proportion of cocaine users was higher for trauma and lower for altered level of consciousness than other subgroups. There was no significant difference in proportion of subjects admitted to the hospital, but cocaine users had a higher rate of elopement and were placed on 72-h psychiatric holds and/or transferred to inpatient psychiatric facilities at a significantly lower rate than the other subgroups. Conclusion: Cocaine users were more likely to present with trauma, elope from the ED, and have alcohol intoxication. Methamphetamine users were more likely to be Caucasian, have altered level of consciousness, be placed on psychiatric holds, or transferred to inpatient psychiatric facilities. These differences may be explained by regional preferences, socialization, personality types, and the unique neuropsychopharmacological differences between cocaine and methamphetamine.

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Section: Discussionmentioning

confidence: 99%

Cocaine Versus Methamphetamine Users in the Emergency Department: How Do They Differ?

Richards¹,

Tabish²,

Wang³

et al. 2017

J Alcohol Drug Depend

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“…Although this weak base hypothesis has been generally accepted, several other alternate mechanisms have also been proposed. For example, AMPH derivatives were also known to inhibit the vesicular [ 3 H] DA uptake through VMAT2 without altering the [ 3 H] DTBZOH binding capacity116. The VMAT2 inhibition could lead to an increase in cytosolic catecholamine levels resulting in increase of efflux through plasma membrane amine transporters.…”

Section: Pharmacologymentioning

confidence: 99%

Vesicular monoamine transporters: Structure‐function, pharmacology, and medicinal chemistry

Wimalasena

2011

Medicinal Research Reviews

164

140

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Vesicular monoamine transporters (VMAT) are responsible for the uptake of cytosolic monoamines into synaptic vesicles in monoaminergic neurons. Two closely related VMATs with distinct pharmacological properties and tissue distributions have been characterized. VMAT1 is preferentially expressed in neuroendocrine cells and VMAT2 is primarily expressed in the CNS. The neurotoxicity and addictive properties of various psychostimulants have been attributed, at least partly, to their interference with VMAT2 functions. The quantitative assessment of the VMAT2 density by PET scanning has been clinically useful for early diagnosis and monitoring of the progression of Parkinson's and Alzheimer's diseases and drug addiction. The classical VMAT2 inhibitor tetrabenazine has long been used for the treatment of chorea associated with Huntington's disease in UK, Canada and Australia and recently approved in the US. The VMAT2 imaging may also be useful for exploiting the onset of diabetes mellitus, since VMAT2 is also expressed in the β-cells of the pancreas. VMAT1 gene SLC18A1 is a locus with strong evidence of linkage with schizophrenia and thus, the polymorphic forms of the VMAT1 gene may confer susceptibility to schizophrenia. This review summarizes the current understanding of the structurefunction relationships of VMAT2, and the role of VMAT2 on addiction and psychostimulant induced neurotoxicity, and the therapeutic and diagnostic applications of specific VMAT2 ligands. The evidence for the linkage of VMAT1 gene with schizophrenia and bipolar disorder I are also discussed.

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“…Fleckenstein et al (2007) also proposed the "weak base hypothesis," which suggests that as weak bases, amphetamines can reduce the vesicular membrane pH gradient, compromising VMAT-2 activity and reducing vesicular sequestration of dopamine. However, it has been suggested that high concentrations of amphetamine (N100 μM) would be required to accomplish this effect (Schwartz et al, 2006). More recently Siciliano et al (2014) demonstrated that low concentrations (10 nM) of amphetamine cause DAT-dependent dopamine release.…”

Section: Dose Dependent Effects Of Amphetamine and Methamphetaminementioning

confidence: 98%

The neuroprotective potential of low-dose methamphetamine in preclinical models of stroke and traumatic brain injury

Rau

Ziemniak

Poulsen

2016

Progress in Neuro-Psychopharmacology and Biological Psychiatry

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Methamphetamine is a psychostimulant that was initially synthesized in 1920. Since then it has been used to treat attention deficit hyperactive disorder (ADHD), obesity and narcolepsy. However, methamphetamine has also become a major drug of abuse worldwide. Under conditions of abuse, which involve the administration of high repetitive doses, methamphetamine can produce considerable neurotoxic effects. However, recent evidence from our laboratory indicates that low doses of methamphetamine can produce robust neuroprotection when administered within 12h after severe traumatic brain injury (TBI) in rodents. Thus, it appears that methamphetamine under certain circumstances and correct dosing can produce a neuroprotective effect. This review addresses the neuroprotective potential of methamphetamine and focuses on the potential beneficial application for TBI.

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The effect of psychostimulants on [3H]dopamine uptake and release in rat brain synaptic vesicles

Cited by 15 publications

References 14 publications

Cocaine Versus Methamphetamine Users in the Emergency Department: How Do They Differ?

Cocaine Versus Methamphetamine Users in the Emergency Department: How Do They Differ?

Vesicular monoamine transporters: Structure‐function, pharmacology, and medicinal chemistry

The neuroprotective potential of low-dose methamphetamine in preclinical models of stroke and traumatic brain injury

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