Wikipedia:WikiProject Chemicals/Chembox validation/VerifiedDataSandbox and Raclopride: Difference between pages

{{short description|Chemical compound}}

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| image = Raclopride.svg

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| CAS_number = 84225-95-6

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| KEGG = D82063

| ChEBI = 92070

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| IUPAC_name = 3,5-dichloro-''N''-<nowiki>[[</nowiki>(2''S'')-1-ethylpyrrolidin-2-yl]methyl]-2-hydroxy-6-methoxybenzamide

'''Raclopride''' is a [[typical antipsychotic]]. It acts as a selective [[receptor antagonist|antagonist]] on [[DRD2|D₂]] [[dopamine receptor]]s.<ref>{{cite journal |vauthors=Köhler C, Hall H, Ogren SO, Gawell L |title=Specific in vitro and in vivo binding of 3H-raclopride. A potent substituted benzamide drug with high affinity for dopamine D-2 receptors in the rat brain |journal=Biochemical Pharmacology |volume=34 |issue=13 |pages=2251–9 |year=1985 |pmid=4015674 |doi=10.1016/0006-2952(85)90778-6 }}</ref> It has been used in trials studying [[Parkinson Disease]].<ref name="pmid19966595">{{cite journal| author = Ishibashi K, Ishii K, Oda K, Mizusawa H, Ishiwata K | title = Competition between 11C-raclopride and endogenous dopamine in Parkinson's disease. | journal = Nucl Med Commun | year = 2010 | volume = 31 | issue = 2 | pages = 159–66 | pmid =19966595 | doi=10.1097/MNM.0b013e328333e3cb | pmc= | s2cid = 205821715 }} </ref>

Its selectivity to the cerebral [[DRD2|D₂ receptors]] is characterized by its respective K_i-values, which are as follows: 1.8, 3.5, 2400 and 18000 nM for [[DRD2|D₂]], [[DRD3|D₃]], [[DRD4|D₄]] and [[DRD1|D₁]] receptors respectively.

It can be [[radiolabelled]] with [[radioisotopes]], e.g. [[Tritium|³H]] or [[Isotopes_of_carbon#Carbon-11|¹¹C]] and used as a tracer for ''[[in vitro]]'' imaging ([[autoradiography]]) as well as ''[[in vivo]]'' imaging [[positron emission tomography]] (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 [[Dopamine_receptor_D2|D₂ dopamine]] [[Receptor (biochemistry)|receptor]], 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]], a genetic disease characterized by selective degeneration of cerebral [[DRD2|D₂ receptors]].<ref>{{cite journal |vauthors=Antonini A, Leenders KL, Spiegel R, Meier D, Vontobel P, Weigell-Weber M, Sanchez-Pernaute R, de Yébenez JG, Boesiger P, Weindl A, Maguire RP |title=Striatal glucose metabolism and dopamine D2 receptor binding in asymptomatic gene carriers and patients with Huntington's disease |journal=Brain |volume=119 |issue=6 |pages=2085–95 |year=1996 |pmid=9010012 |doi=10.1093/brain/119.6.2085 |doi-access=free }}</ref>

Other studies have investigated the relationship of [[DRD2|D₂]] receptor binding capacity and [[personality disorders]]. One study found decreased binding in the ''[[Emotional detachment|detachment]]'' [[personality trait]].<ref>{{cite journal |vauthors=Farde L, Gustavsson JP, Jönsson E |title=D2 dopamine receptors and personality traits |journal=Nature |volume=385 |issue=6617 |pages=590 |year=1997 |pmid=9024656 |doi=10.1038/385590a0 |bibcode=1997Natur.385..590F |s2cid=4235650 |doi-access=free }}</ref> Radiolabelled raclopride is also commonly used to determine the efficacy and [[neurotoxicity]] of [[dopaminergic]] drugs.

==References==

{{reflist}}

{{Dopaminergics}}

[[Category:Benzamides]]

[[Category:Chloroarenes]]

[[Category:D2 antagonists]]

[[Category:Phenol ethers]]

[[Category:Pyrrolidines]]

[[Category:Typical antipsychotics]]

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