Search results for "Sulpiride"
showing 10 items of 38 documents
The effects of dopamine D 2 and D 3 antagonists on spontaneous motor activity and morphine-induced hyperactivity in male mice
1999
Rationale: Dopaminergic neurotransmission, in particular the mesolimbic pathway, is involved in spontaneous locomotor activity and in morphine-induced hyperactivity, since the drugs acting on DA receptors can modify the action of morphine and this effect could be dependent on the type of DA receptor affected. Objective: In this study, the action of U-99194A maleate, haloperidol, sulpiride and morphine (5, 10, 20, 40 mg/kg) on locomotor activity in male mice was evaluated. Likewise, the effects of these dopaminergic antagonists on morphine-induced hyperactivity were studied. Methods: Animals treated with U-99194A maleate (2.5, 5, 10, 20 mg/kg), haloperidol (0.075, 0.1 mg/kg), sulpiride (20, …
Effects of sulpiride on the orienting movement evoked By acoustic stimulation in the Rat.
2000
Abstract Drugs that selectively block D 2 receptors are known to provoke a rapid cell firing increase followed by A9 and A10 dopaminergic (DA) neuron inactivation (depolarization block). In this study, possible relationships between cell firing rapid increase and specific behavioral effects, linked to sensorimotor integration, were investigated in the rat. To this purpose, with the aid of a video camera apparatus and a frame-by-frame analysis, effects of sulpiride-induced blockade of DA D 2 receptors were analyzed on the orienting movement of the head induced by acoustic stimulation. In a control group of rats, during trials lasting 20 min, latency and duration of head turning (HT) were 186…
The inhibition by dopamine of cholinergic transmission in the isolated guinea-pig ileum. Mediation through alpha-adrenoceptors.
1982
1. Segments of the guinea-pig ileum were incubated in Tyrode's solution containing 3 μM propranolol. Dopamine, like noradrenaline and clonidine, inhibited the twitch response to field stimulation. The inhibitory action of dopamine remained unchanged in the presence of the dopamine uptake inhibitor nomifensine (1 μM). Tissue from reserpine-pretreated amimals was insensitive to tyramine but the response to dopamine was not affected. It is, therefore, assumed that the effect of dopamine is due to a direct receptor stimulation and not to the release of noradrenaline. 2. The inhibitory action of dopamine was not antagonized by the dopamine receptor antagonists cis-flupenthixol, pimozide or dompe…
Sulpiride has an antiaggressive effect in mice without markedly depressing motor activity
1991
The atypical neuroleptic, sulpiride is a selective D2 antagonist, having a preferential action on mesolimbic regions. The effects of acute and chronic treatment with sulpiride on aggressive behaviour in male mice were studied using an ethologically based analysis. It was hypothesized that sulpiride would diminish "threat" and "attack" but would not produce marked "immobility", because of the mesolimbic effect referred to above. Isolated albino male mice (experimental animals) were confronted by "standard opponents". Acutely-treated experimental animals received an intraperitoneal injection of sulpiride (20, 50 or 100 mg/kg) 30 min before testing. Chronically-treated animals received sulpiri…
The Tuberohypophyseal Dopamine System: Dopaminergic Modulation of Vasopressin Release. Characterization of Release and Metabolism of3H-Dopamine
1986
Dopamine (DA) fibres originating in the arcuate nucleus project into the neural and intermediate lobes (N-IL) of the pituitary gland. It has been shown that DA and DA agonists decrease the electrically evoked vasopressin release from the isolated N-IL, an effect antagonized by D2 selective DA antagonists (see Holzbauer et al., 1983). However, there are also observations suggesting that there is an additional facilitation of the evoked vasopressin release via D1 receptors. Thus, SKF 82526 (6-chloro-7,8-drhydroxy-1-(p-hydroxyphenyl)-2,3,4,5-tetrahydro-1H-benzazepine mesylate) concentrationdependently decreased (max. 30 % at 30 nM) and increased (max. 40 % at 3 µM) the electrically evoked vaso…
Presynaptic regulation of the electrically evoked release of endogenous dopamine from the isolated neurointermediate lobe or isolated neural lobe of …
1988
Isolated neurointermediate lobes (NILs) or isolated neural lobes (NLs) of the rat pituitary gland were incubated in Krebs-HEPES solution which contained pargyline and the dopamine uptake inhibitor GBR 12921. The release of endogenous dopamine was determined by HPLC with electrochemical detection. Electrical stimulation of the pituitary stalk induced a frequency-dependent release of dopamine. The release of dopamine from the combined NIL evoked by stimulation at 15 Hz was increased by 130% in the presence of the dopamine D2 receptor antagonist, (-)-sulpiride; the (+)-enantiomer of sulpiride had virtually no effect. When the stimulation frequency was 3 Hz (-)-sulpiride caused an increase in d…
How Does the Benzamide Antipsychotic Amisulpride get into the Brain?—An In Vitro Approach Comparing Amisulpride with Clozapine
2003
This study evaluated the disposition of the two atypical antipsychotics, amisulpride (AMS) and clozapine (CLZ), and its main metabolite N-desmethylclozapine (DCLZ), to their target structures in the central nervous system by applying an in vitro blood-brain barrier and blood-cerebrospinal fluid (CSF) barrier based on monolayers of porcine brain microvessel endothelial cells (PMEC) or porcine choroid plexus epithelial cells (PCEC). Permeation studies through PMEC- and PCEC-monolayers were conducted for 60 min at drug concentrations of 1, 5, 10, and 30 muM applied to the donor compartment. PMEC were almost impermeable for AMS (permeation coefficient, P1 x 10(-7) cm/s) in the resorptive direct…
Influence of ventral tegmental area (A10 region) on flight behaviour elicited by hypothalamic stimulation in the cat.
1993
The influence of the ventral tegmental area (VTA) (dopaminergic A10 group neurons) on flight behaviour, induced by hypothalamic stimulation, was studied in the cat. Co-stimulation of hypothalamus and VTA (ipsi- or contralateral) induced an increase of the flight latency. Slow-motion analysis of flight behaviour showed that this increase was due to the augmentation of the fixation latency (FL) whereas the upright latency (UL) was not modified. Sulpiride injection (50 mg/kg i.p.) provoked the disappearance of VTA effect without affecting the basal behavioural sequence. The results show that DA A10 group neurons increase the attentive component of the flight reaction, suggesting a possible inf…
Inhibitory effect of A10 dopaminergic neurons of the ventral tegmental area on the orienting response evoked by acoustic stimulation in the cat.
1998
Abstract The effect of bilateral electric stimulation of A10 dopaminergic neurons of the ventral tegmental area (80–300 μA, 20–50 Hz, 0.1–0.5 ms, 2 s duration) on latency and duration of the orienting response, evoked by acoustic stimuli (4500–8000 Hz, 2 s), was studied in the cat. A10 neuron stimulation, simultaneous with the acoustic one, was performed with threshold parameters inducing minimal behavioral signs (head searching movement, sniffing, increase in alertness). By means of a videoanalysis system, a statistically significant increase, both of latency and duration of the response, was observed. The possible role of dopamine was studied administrating sulpiride (20 mg/kg IP), a dopa…
Serum Levels of Sulpiride Enantiomers after Oral Treatment with Racemic Sulpiride in Psychiatric Patients: a Pilot Study1
2001
Sulpiride (SULP), a substituted benzamide with high selectivity for D 2 -like dopamine receptors, has a chiral structure and is used in most countries as the racemate. In an open pilot study, we investigated 26 inpatients (13 female, 13 male) with schizophrenic or depressive disorder treated with SULP (mean daily dosage 64-1062 mg) administered orally, either as a monotherapy or as an add-on treatment to a stable and unchanged medication for 3-60 days. Serum levels of total SULP and of its enantiomers were measured by high-performance liquid chromatography (HPLC) procedures. Clinically relevant indicators of hepatic and renal function as well as retrospectively assessed clinical outcome par…