Modulation of dopamine D3 receptor binding by N-ethylmaleimide and neurotensin
GTP or G protein inactivation by N-ethylmaleimide reduced the Bmax value but not the KD value of 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin ([3H]7-OH-DPAT) binding in the rat subcortical limbic area. Neurotensin (10 nM) increased the KD and the Bmax values of [3H]7-OH-DPAT binding, and these effe...
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| Published in | Brain research Vol. 643; no. 1-2; pp. 343 - 348 |
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| Main Authors | , , |
| Format | Journal Article |
| Language | English |
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London
Elsevier
18.04.1994
Amsterdam New York, NY |
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| Abstract | GTP or G protein inactivation by N-ethylmaleimide reduced the Bmax value but not the KD value of 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin ([3H]7-OH-DPAT) binding in the rat subcortical limbic area. Neurotensin (10 nM) increased the KD and the Bmax values of [3H]7-OH-DPAT binding, and these effects persisted also following N-ethylmaleimide pretreatment. N-Propylnorapomorphine, quinpirole, raclopride, and remoxipride inhibited [3H]7-OH-DPAT binding with Ki values of 0.093, 1.97, 10.6, and 710 nM, respectively. These findings indicate that the D3 receptor is coupled to G proteins in the brain, and that neurotensin can modulate D3 agonist binding by a G protein-independent mechanism. |
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| AbstractList | GTP or G protein inactivation by N-ethylmaleimide reduced the Bmax value but not the KD value of 7-[3H]hydroxy-N,N-di-n-propyl-2-aminotetralin ([3H]7-OH-DPAT) binding in the rat subcortical limbic area. Neurotensin (10 nM) increased the KD and the Bmax values of [3H]7-OH-DPAT binding, and these effects persisted also following N-ethylmaleimide pretreatment. N-Propylnorapomorphine, quinpirole, raclopride, and remoxipride inhibited [3H]7-OH-DPAT binding with Ki values of 0.093, 1.97, 10.6, and 710 nM, respectively. These findings indicate that the D3 receptor is coupled to G proteins in the brain, and that neurotensin can modulate D3 agonist binding by a G protein-independent mechanism. |
| Author | VON EULER, G HILLEFORS-BERGLUND, M YUN LIU |
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| Keywords | Vertebrata Mammalia Rat Rodentia Central nervous system Neurotensin Neuropeptide D3 Dopamine receptor Brain (vertebrata) G protein |
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| References | Barnes (10.1016/0006-8993(94)90045-0_bib3) 1978; 12 von Euler (10.1016/0006-8993(94)90045-0_bib21) 1990; 531 Dohlman (10.1016/0006-8993(94)90045-0_bib5) 1991; 60 Lowry (10.1016/0006-8993(94)90045-0_bib13) 1951; 193 Nemeroff (10.1016/0006-8993(94)90045-0_bib16) 1983; 225 Agnati (10.1016/0006-8993(94)90045-0_bib1) 1983; 119 Lévesque (10.1016/0006-8993(94)90045-0_bib12) 1992; 89 Feenstra (10.1016/0006-8993(94)90045-0_bib7) 1983; 324 Köhler (10.1016/0006-8993(94)90045-0_bib11) 1990; 82 Sokoloff (10.1016/0006-8993(94)90045-0_bib18) 1990; 347 Cheng (10.1016/0006-8993(94)90045-0_bib4) 1973; 22 Gilman (10.1016/0006-8993(94)90045-0_bib8) 1987; 56 Baldessarini (10.1016/0006-8993(94)90045-0_bib2) 1993; 239 Malmberg (10.1016/0006-8993(94)90045-0_bib14) 1993; 43 von Euler (10.1016/0006-8993(94)90045-0_bib22) 1991; 56 El Mestikawy (10.1016/0006-8993(94)90045-0_bib6) 1986; 46 Sokoloff (10.1016/0006-8993(94)90045-0_bib17) 1992; 225 von Euler (10.1016/0006-8993(94)90045-0_bib20) 1989; 135 Winslow (10.1016/0006-8993(94)90045-0_bib23) 1987; 262 Hall (10.1016/0006-8993(94)90045-0_bib9) 1990; 55 Nemeroff (10.1016/0006-8993(94)90045-0_bib15) 1987 Kebabian (10.1016/0006-8993(94)90045-0_bib10) 1979; 277 von Euler (10.1016/0006-8993(94)90045-0_bib19) 1991; 561 |
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| SubjectTerms | Animals Binding, Competitive Biological and medical sciences Cell Membrane - metabolism Central nervous system Central neurotransmission. Neuromudulation. Pathways and receptors Dopamine Agents - pharmacology Dose-Response Relationship, Drug Ethylmaleimide - pharmacology Fundamental and applied biological sciences. Psychology Kinetics Limbic System - metabolism Male Neurotensin - pharmacology Rats Rats, Sprague-Dawley Receptors, Dopamine - drug effects Receptors, Dopamine - metabolism Receptors, Dopamine D2 Receptors, Dopamine D3 Tetrahydronaphthalenes - metabolism Vertebrates: nervous system and sense organs |
| Title | Modulation of dopamine D3 receptor binding by N-ethylmaleimide and neurotensin |
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