Antidepressant drugs given repeatedly change the binding of the dopamine D2 receptor agonist, [3H]N-0437, to dopamine D2 receptors in the rat brain. 1996

J Maj, and M Dziedzicka-Wasylewska, and R Rogoz, and Z Rogóz, and G Skuza
Institute of Pharmacology, Polish Academy of Sciences, Kraków, Poland.

The effects of antidepressants given in a single dose or repeatedly (10 mg/kg p.o., twice daily, 14 days) on binding to dopamine D2 receptors in the striatum and limbic forebrain of Wistar male rats were studied. [3H]N-0437, (2-(N[2,3(n)-3H]propyl-N-(2-thiofuranyl)-2'-ethylamino) -5-hydroxy-1,2,3,4-tetrahydronaphthalene), a dopamine D2 receptor agonist, was used as a ligand. Already a single dose of imipramine and fluoxetine caused a statistically significant decrease in the affinity of the ligand for dopamine D2 receptors in the striatum, but only at 72 h after drug administration. Also at 72 h after the single dose of mianserin a significant increase in the density of dopamine D2 receptors was observed. Repeated imipramine, amitriptyline and mianserin increased the affinity for dopamine D2 receptors in the striatum and in the limbic forebrain. Repeated fluoxetine increased that affinity in the striatum, but decreased it in the limbic forebrain. The density of dopamine D2 receptors was increased by the repeated administration of the antidepressants studied in the limbic forebrain, but was not changed in the striatum. The results obtained in the present study are in good agreement with the previously reported enhancement of behavioural responsiveness to dopamine and dopamine stimulants (dopamine D2 up-regulation) evoked by repeated treatment with antidepressants.

UI MeSH Term Description Entries
D007099 Imipramine The prototypical tricyclic antidepressant. It has been used in major depression, dysthymia, bipolar depression, attention-deficit disorders, agoraphobia, and panic disorders. It has less sedative effect than some other members of this therapeutic group. Imidobenzyle,Imizin,4,4'-Methylenebis(3-hydroxy-2-naphthoic acid)-3-(10,11-dihydro-5H-dibenzo(b,f)azepin-5-yl)-N,N-dimethyl-1-propanamine (1:2),Imipramine Hydrochloride,Imipramine Monohydrochloride,Imipramine Pamoate,Janimine,Melipramine,Norchlorimipramine,Pryleugan,Tofranil
D008032 Limbic System A set of forebrain structures common to all mammals that is defined functionally and anatomically. It is implicated in the higher integration of visceral, olfactory, and somatic information as well as homeostatic responses including fundamental survival behaviors (feeding, mating, emotion). For most authors, it includes the AMYGDALA; EPITHALAMUS; GYRUS CINGULI; hippocampal formation (see HIPPOCAMPUS); HYPOTHALAMUS; PARAHIPPOCAMPAL GYRUS; SEPTAL NUCLEI; anterior nuclear group of thalamus, and portions of the basal ganglia. (Parent, Carpenter's Human Neuroanatomy, 9th ed, p744; NeuroNames, http://rprcsgi.rprc.washington.edu/neuronames/index.html (September 2, 1998)). Limbic Systems,System, Limbic,Systems, Limbic
D008297 Male Males
D008803 Mianserin A tetracyclic compound with antidepressant effects. It may cause drowsiness and hematological problems. Its mechanism of therapeutic action is not well understood, although it apparently blocks alpha-adrenergic, histamine H1, and some types of serotonin receptors. Lerivon,Mianserin Hydrochloride,Mianserin Monohydrochloride,Org GB 94,Tolvon,Hydrochloride, Mianserin,Monohydrochloride, Mianserin
D011485 Protein Binding The process in which substances, either endogenous or exogenous, bind to proteins, peptides, enzymes, protein precursors, or allied compounds. Specific protein-binding measures are often used as assays in diagnostic assessments. Plasma Protein Binding Capacity,Binding, Protein
D003342 Corpus Striatum Striped GRAY MATTER and WHITE MATTER consisting of the NEOSTRIATUM and paleostriatum (GLOBUS PALLIDUS). It is located in front of and lateral to the THALAMUS in each cerebral hemisphere. The gray substance is made up of the CAUDATE NUCLEUS and the lentiform nucleus (the latter consisting of the GLOBUS PALLIDUS and PUTAMEN). The WHITE MATTER is the INTERNAL CAPSULE. Lenticular Nucleus,Lentiform Nucleus,Lentiform Nuclei,Nucleus Lentiformis,Lentiformis, Nucleus,Nuclei, Lentiform,Nucleus, Lenticular,Nucleus, Lentiform,Striatum, Corpus
D005473 Fluoxetine The first highly specific serotonin uptake inhibitor. It is used as an antidepressant and often has a more acceptable side-effects profile than traditional antidepressants. Fluoxetin,Fluoxetine Hydrochloride,Lilly-110140,N-Methyl-gamma-(4-(trifluoromethyl)phenoxy)benzenepropanamine,Prozac,Sarafem,Lilly 110140,Lilly110140
D000639 Amitriptyline Tricyclic antidepressant with anticholinergic and sedative properties. It appears to prevent the re-uptake of norepinephrine and serotonin at nerve terminals, thus potentiating the action of these neurotransmitters. Amitriptyline also appears to antagonize cholinergic and alpha-1 adrenergic responses to bioactive amines. Amineurin,Amitrip,Amitriptylin Beta,Amitriptylin Desitin,Amitriptylin RPh,Amitriptylin-Neuraxpharm,Amitriptyline Hydrochloride,Amitrol,Anapsique,Apo-Amitriptyline,Damilen,Domical,Elavil,Endep,Laroxyl,Lentizol,Novoprotect,Saroten,Sarotex,Syneudon,Triptafen,Tryptanol,Tryptine,Tryptizol,Amitriptylin Neuraxpharm,Apo Amitriptyline,Desitin, Amitriptylin,RPh, Amitriptylin
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D000928 Antidepressive Agents Mood-stimulating drugs used primarily in the treatment of affective disorders and related conditions. Several MONOAMINE OXIDASE INHIBITORS are useful as antidepressants apparently as a long-term consequence of their modulation of catecholamine levels. The tricyclic compounds useful as antidepressive agents (ANTIDEPRESSIVE AGENTS, TRICYCLIC) also appear to act through brain catecholamine systems. A third group (ANTIDEPRESSIVE AGENTS, SECOND-GENERATION) is a diverse group of drugs including some that act specifically on serotonergic systems. Antidepressant,Antidepressant Drug,Antidepressant Medication,Antidepressants,Antidepressive Agent,Thymoanaleptic,Thymoanaleptics,Thymoleptic,Thymoleptics,Antidepressant Drugs,Agent, Antidepressive,Drug, Antidepressant,Medication, Antidepressant

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