Raclopride
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Raclopride is a typical antipsychotic. It acts as a selective
antagonist An antagonist is a character in a story who is presented as the main enemy or rival of the protagonist and is often depicted as a villain.D2 dopamine receptors. It has been used in trials studying Parkinson Disease. Its selectivity to the cerebral D2 receptors is characterized by its respective Ki-values, which are as follows: 1.8, 3.5, 2400 and 18000 nM for D2, D3, D4 and D1 receptors respectively. It can be radiolabelled with radioisotopes, e.g. 3H or 11C and used as a tracer for ''
in vitro ''In vitro'' (meaning ''in glass'', or ''in the glass'') Research, studies are performed with Cell (biology), cells or biological molecules outside their normal biological context. Colloquially called "test-tube experiments", these studies in ...
'' imaging ( autoradiography) as well as ''
in vivo Studies that are ''in vivo'' (Latin for "within the living"; often not italicized in English) are those in which the effects of various biological entities are tested on whole, living organisms or cells, usually animals, including humans, an ...
'' imaging
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 metabolic processes, and in other physiological activities including blood flow, r ...
(PET). Images obtained by cerebral PET scanning (e.g. PET/CT or PET/MRI) allow the non-invasive assessment of the binding capacity of the cerebral D2 dopamine
receptor Receptor may refer to: * Sensory receptor, in physiology, any neurite structure that, on receiving environmental stimuli, produces an informative nerve impulse *Receptor (biochemistry), in biochemistry, a protein molecule that receives and respond ...
, which can be useful for the diagnosis of movement disorders. In particular, cerebral D2 receptor binding as measured by carbon-11-raclopride (11C-raclopride) has shown to reflect disease severity of
Huntington's disease Huntington's disease (HD), also known as Huntington's chorea, is an incurable neurodegenerative disease that is mostly Genetic disorder#Autosomal dominant, inherited. It typically presents as a triad of progressive psychiatric, cognitive, and ...
, a genetic disease characterized by selective degeneration of cerebral D2 receptors. Other studies have investigated the relationship of D2 receptor binding capacity and personality disorders. One study found decreased binding in the '' detachment'' personality trait. Radiolabelled raclopride is also commonly used to determine the efficacy and neurotoxicity of
dopaminergic Dopaminergic means "related to dopamine" (literally, "working on dopamine"), a common neurotransmitter. Dopaminergic substances or actions increase dopamine-related activity in the brain. Dopaminergic pathways, Dopaminergic brain pathways facil ...
drugs.


References

Benzamides Chloroarenes D2 antagonists Phenol ethers Pyrrolidines Typical antipsychotics {{nervous-system-drug-stub