caa a22 4500 469079304 CHVBK 20180323132945.0 cr unu---uuuuu 170328e19920301xx s 000 0 eng 10.1007/BF00168692 doi (NATIONALLICENCE)springer-10.1007/BF00168692 Radiolabeling of dopamine uptake sites in mouse striatum: comparison of binding sites for cocaine, mazindol, and GBR 12935 [Elektronische Daten] [Maarten Reith, Gabor Selmeci] Summary: This study addressed the possibility of a unique binding interaction between cocaine and the dopamine transporter as compared with other blockers of dopamine uptake. Cocaine binding sites in a fresh P2 fraction of mouse striatum were labeled with [3H]CFT, a phenyltropane analog of cocaine also known as WIN 35,428, and compared with sites labeled with [3H]mazindol or [3H]GBR 12935. Under the conditions used, homogeneous binding was observed that was inhibited monophasically by cocaine, CFT, and mazindol; the same potencies were observed with the three radioligands. Saturation analysis in the presence and in the absence of unlabeled inhibitor (CFT, mazindol, cocaine) indicated a change in the Kd but not the Bmax, consonant with a competitive mechanism. Tris-HCl reduced the affinity of each radioligand and unlabeled inhibitor without changing the Bmax. N-Ethylmaleimide reduced the binding of all radioligands equally and cocaine offered protection. The dissociation rate of [3H]CFT and [3H]mazindol binding was not affected by the presence of mazindol and CFT, respectively. The Bmax of [3H]CFT and [3H]mazindol binding was the same; the relatively higher value for [3H]GBR 12935 binding in analyses involving varying tritiated GBR 12935 only, was due primarily to an underestimation of the specific activity of [3H]GBR 12935. All results are in agreement with a one-site model in which cocaine, CFT, mazindol, and GBR 12935 share a common binding site in mouse striatum. Springer-Verlag, 1992 Cocaine binding nationallicence Mazindol binding nationallicence GBR 12935 binding nationallicence N-ethylmaleimide nationallicence Mouse striatum nationallicence Reith Maarten Division of Neurochemistry, N. S. Kline Institute for Psychiatric Research, Oak and Plaza Sts, 10962, Orangeburg, NY, USA aut Selmeci Gabor Division of Neurochemistry, N. S. Kline Institute for Psychiatric Research, Oak and Plaza Sts, 10962, Orangeburg, NY, USA aut Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 345/3(1992-03-01), 309-318 0028-1298 345:3<309 1992 345 210 https://doi.org/10.1007/BF00168692 text/html Onlinezugriff via DOI 1 research-article jats NATIONALLICENCE 856 40 https://doi.org/10.1007/BF00168692 text/html Onlinezugriff via DOI NATIONALLICENCE 700 1- Reith Maarten Division of Neurochemistry, N. S. Kline Institute for Psychiatric Research, Oak and Plaza Sts, 10962, Orangeburg, NY, USA aut NATIONALLICENCE 700 1- Selmeci Gabor Division of Neurochemistry, N. S. Kline Institute for Psychiatric Research, Oak and Plaza Sts, 10962, Orangeburg, NY, USA aut NATIONALLICENCE 773 0- Naunyn-Schmiedeberg's Archives of Pharmacology Springer-Verlag 345/3(1992-03-01), 309-318 0028-1298 345:3<309 1992 345 210 Metadata rights reserved Springer special CC-BY-NC licence nationallicence BK010053 XK010053 XK010000 NATIONALLICENCE NATIONALLICENCE NL-springer