Kinetic evidence for isomerization of the dopamine receptor-raclopride complex

Lepiku, Martin; Rinken, Ago; Järv, Jaak; Fuxé, Kjell

doi:10.1016/0197-0186(95)00123-9

Cited by 25 publications

(10 citation statements)

References 13 publications

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“…However, at the experimental conditions studied, we could not detect any D 2 -specific inhibition of cAMP formation despite the presence of these receptors. The presence of receptors was confirmed by specific binding of the D 2 -specific radioligand [ 3 H]raclopride, whose affinity (K D = 2.3 ± 0.2 nM) and number of binding sites (B max = 21 ± 1 fmol / mg tissue (ww)) were in good agreement with our previous data obtained for characterization of dopamine D 2 receptors (16,17). Quinpirole, a D2-family-selective agonist, had no significant influence at concentrations up to 10 μM neither on the cAMP accumulation generated by direct activation of AC with 0.1 μM forskolin (Fig.…”

Section: Resultssupporting

confidence: 78%

Modulation of Adenylyl Cyclase Activity in Rat Striatal Homogenate by Dopaminergic Receptors

2008

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Abstract. We have characterized the modulation of adenylyl cyclase (AC) activity by ligands of dopaminergic receptors in rat striatal homogenate and compared the results with receptorligand binding affinities. Despite the fact that rat striatum contains high level of both dopamine D 1 and D 2 receptors, only the D 1 -specific AC activation by agonists could be determined. All D 1 -receptor agonists (dopamine, dihydrexidine, and A 77636) used were able to increase cAMP accumulation in a concentration-dependent manner, while D 1 -receptor antagonists (SCH23390, SKF83566, and butaclamol) blocked the effects induced by the aforementioned agonists. At the same time, the D 2 -receptor agonist quinpirole and antagonist sulpiride had no effect on cAMP accumulation in striatal homogenate neither on the basal level nor on the activated level of AC, while inhibited [

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Section: Resultssupporting

confidence: 78%

Modulation of Adenylyl Cyclase Activity in Rat Striatal Homogenate by Dopaminergic Receptors

2008

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“…The brain samples were stored in polypropylene tubes at -82°C until assayed. The binding studies were performed as described previously [23], but slightly modified. In brief, the brain samples were homogenized using a glass Teflon homogenizer (Braun Melsungen AG, Melsungen, Germany; 10 strokes, 1,000 rpm) in ice-cold incubation buffer (mmol/l): 5.0 MgCl 2 ; 1.0 EDTA; 50 Tris HCl; 0.01% L(+)ascorbic acid, pH 7.4 at 20°C.…”

Section: [ 3 H]raclopride Bindingmentioning

confidence: 99%

“…Furthermore, the functional relationship between the monoamine reuptake blockade and D 2 receptor-binding changes is not known [19]. Therefore, in addition, our study tried to clarify whether [ 3 H]raclopride (a selective D 2 receptor ligand) binding [20][21][22][23] in the rat neostriatum is changed after acute or chronic antidepressant treatment under our laboratory conditions.…”

Section: Introductionmentioning

confidence: 99%

Acute and Chronic Citalopram Treatment Differently Modulates Rat Exploratory Behavior in the Exploration Box Test: No Evidence for Increased Anxiety or Changes in the [<sup>3</sup>H]Raclopride Binding

Matto

Allikmets²

1999

Pharmacology

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The effect of acute and chronic desipramine (10 mg/kg) and citalopram (10 mg/kg) treatment on rat exploratory behavior in the recently developed exploration box test was studied on 5 consecutive days. Acute desipramine but not citalopram treatment decreased the time spent exploring, the number of line crossings, rears, investigative approaches, entries into the large arena, and sum of exploratory events. After 3 weeks of pretreatment, both desipramine and citalopram attenuated rat exploratory behavior, whereas the number of entries into the large arena was unchanged. In the open field test, acute desipramine or citalopram treatment (5, 10, 15 mg/kg) attenuated rat exploratory behavior in a dose-dependent manner. In the subsequent rota-rod test, neither desipramine nor citalopram treatment (0–20 mg/kg) impaired motor performance capacity. In an additional experiment, [³H]raclopride binding was unchanged after single as well as 3 weeks of desipramine or citalopram treatment in the rat brain neostriatum. Our experiments demonstrate that acute citalopram treatment in the open field test and chronic citalopram treatment in the exploration box test attenuate rat exploratory behavior, but these effects may not be implicated with enhanced anxiety or changed dopamine D₂ receptor characteristics.

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“…Experiments were carried out as described by Lepiku et al (1996). Brain tissue was resuspended in ice-cold TrisHCl (50 mm, pH 7.4) containing NaCl (120 mm), MgCl 2 (5 mm) and EDTA (1 mm).…”

Section: [ 3 H]raclopride Binding Assaymentioning

confidence: 99%

Putamen Mitochondrial Energy Metabolism Is Highly Correlated to Emotional and Intellectual Impairment in Schizophrenics

Prince

Harro

Blennow

et al. 2000

Neuropsychopharmacology

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Kinetic evidence for isomerization of the dopamine receptor-raclopride complex

Cited by 25 publications

References 13 publications

Modulation of Adenylyl Cyclase Activity in Rat Striatal Homogenate by Dopaminergic Receptors

Modulation of Adenylyl Cyclase Activity in Rat Striatal Homogenate by Dopaminergic Receptors

Acute and Chronic Citalopram Treatment Differently Modulates Rat Exploratory Behavior in the Exploration Box Test: No Evidence for Increased Anxiety or Changes in the [<sup>3</sup>H]Raclopride Binding

Putamen Mitochondrial Energy Metabolism Is Highly Correlated to Emotional and Intellectual Impairment in Schizophrenics

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