In vitro evaluation of radioiodinated butyrophenones as radiotracer for dopamine receptor study |
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| Affiliation: | 1. Takarazuka Research Center, Sumitomo Chemical Co., Ltd., Takatsukasa, Takarazuka, Hyogo 665, Japan;3. Department of Family and Consumer Sciences, New Mexico State University, Las Cruces, NM;;4. Department of Nutritional Sciences, Rutgers University, New Brunswick, NJ; and;5. Department of Nursing, Center for Nursing Research and Evidence Based Practice, The Children''s Hospital of Philadelphia, Philadelphia, PA;1. Service de rhumatologie, centre Viggo-Petersen, hôpital Lariboisière, Assistance publique–hôpitaux de Paris, 2, rue Ambroise-Paré, 75010 Paris, France;2. Service de rhumatologie, CHU de Bordeaux, groupe hospitalier Pellegrin, 33000 Bordeaux, France;3. Service de néphrologie, hôpital Saint-Louis, Assistance publique–hôpitaux de Paris, 75010 Paris, France;4. Service de rhumatologie, hôpital Bichat–Claude-Bernard, Assistance publique–hôpitaux de Paris, 75018 Paris, France;5. Service de néphrologie, hôpital Pontchaillou, 35033 Rennes cedex, France;6. Service de rhumatologie, hôpital universitaire de Brest, 29200 Brest, France;7. Service de rhumatologie, hôpital Saint-Philibert, 59160 Lille, France;8. Service de néphrologie, hôpital Necker–Enfants-Malades, Assistance publique–hôpitaux de Paris, 75015 Paris, France;9. Service de rhumatologie, hôpitaux universitaires Pitié-Salpêtrière–Charles-Foix, Assistance publique–hôpitaux de Paris, 75013 Paris, France;10. Service de néphrologie, CHRU de Brest, 29200 Brest, France;11. Service de rhumatologie, CHU Roger-Salengro, 59160 Lille, France;12. Service de rhumatologie, CHU de Rennes, 35033 Rennes cedex, France;13. Inserm UMR 1132, université Paris Diderot, Sorbonne Paris Cité, 75475 Paris cedex 10, France |
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| Abstract: | Radioiodinated butyrophenone compounds are attracting the interest of those working on dopamine receptor studies; structure-activity relationship study has revealed the ortho position of the p-fluorobutyrophenone moiety as a very plausible iodination site. Various synthesized butyrophenones iodinated at the ortho position of p-fluorobutyrophenone moiety, 2′- iodohaloperidol (2′-IHP), 2′-iodotrifluperidol (2′-ITP) and 2′-iodospiperone (2′-ISP) were tested for their abilities to inhibit 3H-spiperone (SP) binding for the dopamine (D-2) receptor, together with reference compounds (SP, haloperidol (HP) and 4-iodospiperone (4- ISP)). The order of binding affinity of the tested compounds was SP > 2′-ISP > HP > 4-ISP > 2′-IHP > 2′- ITP. Whereas, the serotonin (S-2) receptor binding affinity of SP and its iodinated analogues were in the order of SP > > 4-ISP > 2′-ISP. Furthermore, in the saturation binding study using the striatal membrane preparations, the 2′-ISP displayed a KD of 0.25 nM with maximum number of binding site Bmax of 210 fmol/mg protein. These data indicated the 2′-ISP as holding high affinity for dopamine receptors and a low affinity for serotonin receptors. Thus, the 125I-2′-ISP was a very potent radioligand for in vitro dopamine (D-2) receptor studies, and 123I-2′-ISP holds very promising characteristics as for in vivo dopamine receptor studies, as well. |
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