Nifene is a high affinity, selective nicotinic α4β2* receptor partial agonist used in medical research for

nicotinic acetylcholine receptors Nicotinic acetylcholine receptors, or nAChRs, are receptor polypeptides that respond to the neurotransmitter acetylcholine. Nicotinic receptors also respond to drugs such as the agonist nicotine. They are found in the central and peripheral n ...

, usually in the form of nifene ( ¹⁸F) as a

positron emission tomography Positron emission tomography (PET) is a functional imaging technique that uses radioactive substances known as radiotracers to visualize and measure changes in Metabolism, metabolic processes, and in other physiological activities including bl ...

(PET)

radiotracer A radioactive tracer, radiotracer, or radioactive label is a chemical compound in which one or more atoms have been replaced by a radionuclide so by virtue of its radioactive decay it can be used to explore the mechanism of chemical reactions by tr ...

. Nifene has been used to assess the efficacy of acetylcholinesterase inhibitors in animal models, because the neurotransmitter acetylcholine competes with the binding of nifene at the nicotinic receptor site. Learning and behavior studies in animal models using nifene have suggested a potential role of the nicotinic receptors located in distinct white matter tracts. Nifene studies in animal models of lung cancer have suggested an upregulation of the nicotinic receptor in the lung tumors. Novel PET and SPECT imaging agents as potential

receptor antagonists A receptor antagonist is a type of Receptor (biochemistry), receptor ligand (biochemistry), ligand or drug that blocks or dampens a biological response by binding to and blocking a Receptor (biochemistry), receptor rather than activating it like ...

have been developed based on the structure of nifene; niodene for SPECT, nifrolene for PET and niofene for PET/SPECT. These new derivatives take advantage of the unique ''in vivo'' imaging properties of nifene. Human studies with ( ¹⁸F)-nifene make it a promising nicotinic α4β2* receptor PET radiotracer for scientific research and has exhibited reliable test-retest reproducibility. Human white matter thalamic radiations (or tracts) were well demarcated and quantified using ( ¹⁸F)-nifene.

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