PET Imaging of Nicotinic Acetylcholine Receptors

2014-08-27 03:16:46 | BioPortfolio



- Central nicotinic acetylcholine receptors (nAChRs) are the primary target for the action of nicotine. In addition to being involved in tobacco dependence, they are also involved in a variety of brain disorders, including Alzheimer's and Parkinson's diseases. Researchers are interested in developing better ways to study the action of nAChRs to improve treatments for smoking cessation and other problems affected by these receptors. These new study methods may involve different radiotracers, which are drugs that can help show brain activity during positron emission tomography (PET) scanning.


- To evaluate the feasibility of using a radiotracer, 2-[18F]F-A-85380, in PET scanning of the brain.


- Healthy volunteers between 21 and 45 years of age who do not use tobacco.


- Participants will be asked to avoid consuming alcohol or using a number of over-the-counter medications, including antihistamines, cough medicines, and nasal decongestants, for 5 days before the study day. Participants provide urine and breath samples at the start of the study to be tested for chemicals that may interfere with the study.

- Participants will visit the clinical center the morning of the day before the scanning session to provide blood and urine samples as required. Participants will return and be admitted for an overnight stay later that afternoon or evening.

- On the day of the study, participants will receive a single dose of the radiotracer 2-[18F]F-A-85380, and will have a series of PET scans over the next 7 hours and provide blood samples during that time. Participants will spend that night at the clinical center and leave on the morning after the end of the study.

- Participants will return for follow-up visits 2 weeks and 1 month after the end of the study.


Background: Central nicotinic acetylcholine receptors (nAChRs) mediate a variety of brain functions and have been implicated in the pathophysiology of Alzheimer's and Parkinson's diseases, other CNS disorders (Tourette's syndrome, epilepsy, etc.), and nicotine dependence. These receptors are the primary target for the action of nicotine, which is believed to cause tobacco dependence. The availability of a suitable agent that could image nAChRs with PET in humans would allow scientists to monitor the nAChRs in vivo for the purpose of determining their roles in the pathogenesis of neurodegenerative diseases and nicotine dependence.

Scientific Goals: The immediate goal of the proposed study is to evaluate the feasibility of using a radiotracer, 2-[18F]F-A-85380, developed by scientists in the NIDA Brain Imaging Center for external imaging of nAChRs in the human brain.

Study Population: Healthy adult participants, males and females between 21 and 45 years of age, will be recruited for this study. The goal is to complete studies of 7 male and 7 female subjects.

Experimental Design and Method: After being medically cleared and giving informed consent, participants will receive a single dose of the radiotracer, 2 [18F]F A 85380-Injection, and will undergo a series of PET scans acquired over the next 7 hours after the injection. The PET scans will be used to determine the time course of the distribution of the injected radioactivity in those organs expected to receive the highest radiation exposure and in the brain.

Benefits to participants and/or society: This protocol will provide no direct benefits to the research participants other than routine medical screening and attention from the research staff. The knowledge gained in this study may lead to the availability of an agent for external monitoring of nAChRs using PET. This agent would be a valuable tool for determining the role of nAChRs in the pathogenesis of neuropsychiatric diseases, including nicotine dependence and for developing medications for diseases that respond to nicotinic agonists.

Risks to participants: There is some risk attendant to the PET scans in general, involving exposure to radiation, arterial catheterization and venous catheterization. In addition, there is risk related to the administration of this radiopharmaceutical, as it will be given to humans for the first time in this study. Medical supervision will be provided throughout the study. A plan for monitoring potential side effects of this radiotracer is given.

Study Design



Healthy Volunteers


National Institute on Drug Abuse, Biomedical Research Center (BRC)
United States




National Institutes of Health Clinical Center (CC)

Results (where available)

View Results


Published on BioPortfolio: 2014-08-27T03:16:46-0400

Clinical Trials [2364 Associated Clinical Trials listed on BioPortfolio]

A Study of HMPL-689 in Healthy Volunteers

The purpose of this study is to evaluate the safety and tolerability of a single dose of HMPL-689 in healthy volunteers To determine the pharmacokinetic profile of single oral doses of HMP...

A Study To Evaluate The Safety And Tolerability Of Different Doses Of PF-03049423 In Healthy Adult Volunteers And Healthy Older Volunteers

The purpose this study is to evaluate the safety and toleration of PF-03049423 following multiple dose administration as an oral solution to healthy young adult volunteers and healthy elde...

Phase 1 Dosing Study of BAX 513 in Healthy Volunteers

The purpose of the study is to investigate whether orally administered BAX 513 (different doses administered for 5 days) affects hemostatic parameters in healthy volunteers.

A Study of Single Dose Inclacumab in Japanese Healthy Volunteers Compared to Caucasian Healthy Volunteers

This open-label, parallel group study will evaluate the safety, tolerability, pharmacokinetics and pharmacodynamics of single doses of inclacumab in Japanese healthy volunteers compared to...

SPM Regulation by Fish Oil Supplements in Healthy Volunteers

A randomised, double-blind, placebo-controlled study to determine whether fish oil supplementation regulates peripheral levels of specialized pro-resolving mediators and white blood cell r...

PubMed Articles [4686 Associated PubMed Articles listed on BioPortfolio]

Four Decades of β-Lactam Antibiotic Pharmacokinetics in Cystic Fibrosis.

The pharmacokinetics (PK) of β-lactam antibiotics in cystic fibrosis (CF) patients has been compared with that in healthy volunteers for over four decades; however, no quantitative models exist that ...

Exceptional Risk: Healthy Volunteers' Perceptions of HIV/AIDS Clinical Trials.

As with all early-stage testing of investigational drugs, clinical trials targeting HIV/AIDS can pose unknown risks to research subjects. Unlike sick participants seeking a therapeutic benefit, the mo...

First population pharmacokinetic analysis showing increased quinolone metabolite formation and clearance in cystic fibrosis patients compared to healthy volunteers.

Understanding the pharmacokinetics in cystic fibrosis (CF) patients is important for dosing. For antibiotics with extensive metabolism, however, a comparison of metabolite formation and elimination be...

Healthy volunteers' perceptions of risk in US Phase I clinical trials: A mixed-methods study.

There is limited research on healthy volunteers' perceptions of the risks of Phase I clinical trials. In order to contribute empirically to long-standing ethical concerns about healthy volunteers' inv...

FGF-21 levels in polyuria-polydipsia syndrome.

The pathomechanism of primary polydipsia is poorly understood. Recent animal data reported a connection between fibroblast growth factor 21 (FGF-21) and elevated fluid intake independently of hormonal...

Medical and Biotech [MESH] Definitions

Persons with no known significant health problems who are recruited to participate in research to test a new drug, device, or intervention as controls for a patient group. (from, accessed 2/14/2013)

Hospital or other institutional ethics committees established to consider the ethical dimensions of patient care. Distinguish from ETHICS COMMITTEES, RESEARCH, which are established to monitor the welfare of patients or healthy volunteers participating in research studies.

Human experimentation that is not intended to benefit the subjects on whom it is performed. Phase I drug studies (CLINICAL TRIALS, PHASE I AS TOPIC) and research involving healthy volunteers are examples of nontherapeutic human experimentation.

Healthy People Programs are a set of health objectives to be used by governments, communities, professional organizations, and others to help develop programs to improve health. It builds on initiatives pursued over the past two decades beginning with the 1979 Surgeon General's Report, Healthy People, Healthy People 2000: National Health Promotion and Disease Prevention Objectives, and Healthy People 2010. These established national health objectives and served as the basis for the development of state and community plans. These are administered by the Office of Disease Prevention and Health Promotion (ODPHP). Similar programs are conducted by other national governments.

Governmental guidelines and objectives pertaining to public food supply and nutrition including recommendations for healthy diet and changes in food habits to ensure healthy diet.

More From BioPortfolio on "PET Imaging of Nicotinic Acetylcholine Receptors"

Quick Search


Relevant Topics

Alzheimer's Disease
Of all the types of Dementia, Alzheimer's disease is the most common, affecting around 465,000 people in the UK. Neurons in the brain die, becuase  'plaques' and 'tangles' (mis-folded proteins) form in the brain. People with Al...

Psychiatry is the study of mental disorders and their diagnosis, management and prevention.  Conditions include schizophrenia, severe depression and panic disorders among others. There are pharmaceutical treatments as well as other therapies to help...

Parkinson's Disease
Parkinson's is a progressive neurological condition, affecting one person in every 500, 95% of which are over 40. It is caused by degeneration of more than 70% of the substantia nigra, which depletes the dopamine (the neurotransmitter involved in pro...

Searches Linking to this Trial