Use of Electronic Cigarettes Leads to Significant Beta2-Nicotinic Acetylcholine Receptor Occupancy: Evidence From a PET Imaging Study

Baldassarri, Stephen R.; Hillmer, Ansel T.; Anderson, Jon Mikael; Jatlow, Peter; Nabulsi, Nabeel; Labaree, David; Cosgrove, Kelly P.; O’Malley, Stephanie S.; Eissenberg, Thomas; Krishnan‐Sarin, Suchitra; Esterlis, Irina

doi:10.1093/ntr/ntx091

Cited by 39 publications

(33 citation statements)

References 44 publications

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“…First, imaging may identify patients with hypocholinergic function to select for cholinergic pharmacotherapy augmentation studies. Second, cholinergic ligand studies may be used for target engagement studies of novel compounds using target displacement techniques (Baldassarri et al, 2018). PET studies combining nicotinic and muscarinic ligands may be vey useful for improved selection of cholinergic compounds to mitigate specific clinical symptoms in PD.…”

Section: Discussionmentioning

confidence: 99%

Molecular Imaging of the Cholinergic System in Parkinson's Disease

Bohnen

Kanel

Müller

2018

International Review of Neurobiology

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One of the first identified neurotransmitter in the brain, acetylcholine is an important modulator that drives changes in neuronal and glial activity. For more than two decades, the main focus of molecular imaging of the cholinergic system in Parkinson’s disease (PD) has been on cognitive changes. Studies have shown that degeneration of the cholinergic system is a major determinant of dementia in PD. Within the last decade, the focus is expanding to studying cholinergic correlates of mobility impairments, dyskinesias, olfaction, sleep, visual hallucinations and risk taking behavior in this disorder. These studies increasingly recognize that the regional topography of cholinergic brain areas associates with specific functions. In parallel with this trend, more recent molecular cholinergic imaging approaches are investigating cholinergic modulatory functions and contributions to large-scale brain network functions. A novel area of research is imaging cholinergic innervation functions of peripheral autonomic organs that may have the potential of future prodromal diagnosis of PD. Finally, emerging evidence of hypercholinergic activity in prodromal and symptomatic LRRK2 PD may reflect neuronal cholinergic compensation versus a response to neuro-inflammation. Molecular imaging of the cholinergic system has led to many new insights in the etiology of many dopamine non-responsive symptoms of PD and is poised to guide and evaluate future cholinergic drug development in PD.

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Section: Discussionmentioning

confidence: 99%

Molecular Imaging of the Cholinergic System in Parkinson's Disease

Bohnen

Kanel

Müller

2018

International Review of Neurobiology

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“…Evidence is emerging suggesting compensatory behaviours occur in response to this variation, in a manner similar to that identified in cigarettes several decades ago [36]. Electronic cigarettes are as capable of saturating brain nicotinic receptors as conventional cigarettes [37]. This effect may not concur with the nicotine content listed on refill bottles, which may reflect inaccuracy of labelling and manufacturing.…”

Section: Electronic Cigarettes and Nicotine Addictionmentioning

confidence: 98%

Electronic cigarette use in youths: a position statement of the Forum of International Respiratory Societies

et al. 2018

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Children and adolescents are highly susceptible to nicotine addiction, which affects their brain development, even in those who smoke infrequently. Young people who become addicted to nicotine are at greater risk of becoming lifelong tobacco consumers. The use of nicotine-delivering electronic cigarettes has risen dramatically among youths worldwide. In addition to physical dependence, adolescents are susceptible to social and environmental influences to use electronic cigarettes. The product design, flavours, marketing, and perception of safety and acceptability have increased the appeal of electronic cigarettes to young people, thus leading to new generations addicted to nicotine. Moreover, there is growing evidence that electronic cigarettes in children and adolescents serve as a gateway to cigarette smoking. There can be no argument for harm reduction in children. To protect this vulnerable population from electronic cigarettes and other nicotine delivery devices, we recommend that electronic cigarettes be regulated as tobacco products and included in smoke-free policies. Sale of electronic cigarettes should be barred to youths worldwide. Flavouring should be prohibited in electronic cigarettes, and advertising accessible by youths and young adults be banned. Finally, we recommend greater research on the health effects of electronic cigarettes and surveillance of use across different countries.

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“…In this context, 2-[ 18 F]FA has been applied to reveal changes in α4β2 nACh receptor, for example by cigarette smoking showing that that smoking of one cigarette produced almost 90 % receptor occupancy 65 . Another study indicated that the use of electronic cigarettes leads to dose-dependent significant β2-nACh receptor occupancy together with reduction of craving similar with the use of a tobacco cigarette 66 .…”

Section: Types Of Challenges That Modulate Neurotransmission and mentioning

confidence: 99%