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Evidence points to the existence of multiple classes of dopamine (DA) receptor in mammalian brain which can be distinguished by their pharmacological specificities and localizations, and by the actions they mediate. Among them, dopaminergic autoreceptors are regulatory receptors presumed to be present in the membrane of the DA neurones themselves, and believed to mediate an inhibition of these neurones' activity, either at nerve endings or on cell bodies. However, the pharmacology of autoreceptors remains to be established because attempts to characterize autoreceptors by 3H-ligand binding techniques have produced controversial data. Thus Seeman and co-workers stated that 3H-apomorphine selectively labels autoreceptors, whereas Creese et al. concluded that this ligand selectively labels postsynaptic DA receptors. In addition, large differences in the capacity and drug specificity of 3H-apomorphine receptor sites in rat striatum have been reported. We demonstrate here that 3H-apomorphine labels two classes of DA receptor, distinguishable using domperidone, a selective DA antagonist. Lesion studies indicate that they correspond to a certain class of postsynaptic receptor and to autoreceptors, respectively. Each of these classes displays a clearly distinct pharmacological specificity for antipsychotics and DA agonists.
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Neuronal release of endogenous dopamine was identified in mucosa-free preparations (muscle layer including intramural plexus) from guinea pig stomach corpus by measuring tissue dopamine content and dopamine release and by immunohistochemical methods using a dopamine antiserum. Dopamine content in mucosa-free preparations of guinea pig gastric corpus was one-tenth of norepinephrine content. Electrical transmural stimulation of mucosa-free preparations of gastric corpus increased the release of endogenous dopamine in a frequency-dependent (3-20 Hz) manner. The stimulated release of dopamine was prevented by either removal of external Ca2+ or treatment with tetrodotoxin. Dopamine-immunopositive nerve fibers surrounding choline acetyltransferase-immunopositive ganglion cells were seen in the myenteric plexus of whole mount preparations of gastric corpus even after bilateral transection of the splanchnic nerve proximal to the junction with the vagal nerve (section of nerves between the celiac ganglion and stomach). Domperidone and sulpiride potentiated the stimulated release of acetylcholine and reversed the dopamine-induced inhibition of acetylcholine release from mucosa-free preparations. These results indicate that dopamine is physiologically released from neurons and from possible dopaminergic nerve terminals and regulates cholinergic neuronal activity in the corpus of guinea pig stomach.
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3,4-Dihydroxyphenylethylamine (dopamine) D2 receptors, solubilized from bovine striatal membranes using a cholic acid-NaCl combination, exhibited the typical pharmacological characteristics of both agonist and antagonist binding. The rank order potency of the agonists and antagonists to displace [3H]spiroperidol binding was the same as that observed with membrane-bound receptors. Computer-assisted analysis of the [3H]spiroperidol/agonist competition curves revealed the retention of high- and low-affinity states of the D2 receptor in the solubilized preparations and the proportions of receptor subpopulations in the two affinity states were similar to those reported in membrane. Guanine nucleotide almost completely converted the high-affinity sites to low-affinity sites for the agonists. The binding of the high-affinity agonist [3H]N-n-propylnorapomorphine ([3H]NPA) was clearly demonstrated in the solubilized preparations for the first time. Addition of guanylyl-imidodiphosphate completely abolished the [3H]NPA binding. When the solubilized receptors were subjected to diethylaminoethyl-Sephacel chromatography, the dopaminergic binding sites eluted in two distinct peaks, showing six- to sevenfold purification of the receptors in the major peak. Binding studies performed on both peaks indicated that the receptor subpopulation present in the first peak may have a larger proportion of high-affinity binding sites than the second peak. The solubilized preparation also showed high-affinity binding of [35S]guanosine-5'-(gamma-thio)triphosphate, a result suggesting the presence of guanine nucleotide binding sites, which may interact with the solubilized D2 receptors. These data are consistent with the retention of the D2 receptor-guanine nucleotide regulatory protein complex in the solubilized preparations and should provide a suitable model system to study the receptor-effector interactions.
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The circadian rhythms of plasma prolactin (PRL) and cortisol and of oral temperature were simultaneously studied in 24 women with polycystic ovary syndrome (PCOS). The PRL response to thyrotropin-releasing hormone (TRH) and domperidone was also evaluated in some of these patients. The physiological circadian chrono-organization of prolactin and cortisol secretion and of oral temperature was maintained in PCOS. The PRL responsiveness to the specific stimulations fell within normal limits. These results do not support the hypothesis of an impaired central dopaminergic regulation of prolactin secretion in PCOS.
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Domperidone (5 mg i.v.) was given singly or together with apomorphine (0.25 mg i.v.) to healthy volunteers. The gastric emptying rate of a test meal of 750 ml of water was then measured using a dye dilution and double sampling technique. The effect of domperidone on gastric secretion was evaluated in patients with duodenal ulcer who received domperidone (5 mg i.v.) prior to continuous aspiration of the stomach contents for 120 minutes. Domperidone markedly increased the rate of emptying of the test meal. Following apomorphine the gastric emptying rate decreased and domperidone antagonized this slowing effect. The composition of gastric juice was not affected by an intravenous dose of domperidone. Domperidone appears to modulate gastric contractile activity without affecting gastric secretion.
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Observational retrospective studies have linked domperidone and prolonged QT interval, ventricular arrhythmias and risk of sudden death. Since then, antiemetic prescription was applied to other molecules (including metopimazine). The aim of this study was to evaluate the profile of adverse cardiac effects associated with QT prolongation for each antiemetic available in France.
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A simple and sensitive liquid chromatography-tandem mass spectrometry method was developed and validated for determining domperidone in human plasma. The analyte and internal standard (IS; mosapride) were isolated from plasma samples by protein precipitation with methanol (containing 0.1% formic acid). The chromatographic separation was performed on an Xterra MS C(18) Column (2.1 x 150 mm, 5.0 microm) with a gradient programme mobile phase consisting of 0.1% formic acid and acetonitrile at a flow rate of 0.30 mL/min. The total run time was 4.0 min. The analyses were carried out by multiple reaction monitoring using the parent-to-daughter combinations m/z 426 --> 175 and m/z 422 --> 198 (IS). The areas of peaks from the analyte and IS were used for quantification of domperidone. The method was validated according to the FDA guidelines on bioanalytical method validation. Validation results indicated that the lower limit of quantification was 0.2 ng/mL, and the assay exhibited a linear range of 0.2-60.0 ng/mL and gave a correlation coefficient (r(2)) of 0.999 or better. Quality control samples (0.4, 0.8, 15 and 50 ng/mL) in six replicates from three different analytical runs demonstrated an intra-assay precision (RSD) 4.43-6.26%, an inter-assay precision 5.25-7.45% and an overall accuracy (relative error) of <6.92%. The method can be applied to pharmacokinetic and bioequivalence studies of domperidone.
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Health providers face the challenge of prescribing or recommending galactagogues without the benefit of robust evidence. Given the suboptimal rates of exclusive breast-feeding worldwide and the availability and demand for medical and herbal lactation therapies, controlled trials and analyses investigating these medicines are urgently warranted.
Gastro-oesophageal regurgitation is considered a problem if it is frequent, persistent, and associated with other symptoms such as increased crying, discomfort with regurgitation, and frequent back arching. A cross-sectional survey of parents of 948 infants attending 19 primary care paediatric practices found that regurgitation of at least one episode a day was reported in 51% of infants aged 0-3 months.
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The mean particle size, PDI, zeta potential and entrapment efficiency of optimized SLN (SLN1) and NLC were found to be 30.45 nm, 0.156, 12.40 mV, 87.84% and 32.23 nm, 0.160, 10.47 mV, 90.49% respectively. DSC studies revealed that DOM was in an amorphous state and triglycerides were in the β prime form in SLN and NLC. Shape and surface morphology was determined by TEM revealed fairly spherical shape of nanoparticles. In vitro release studies demonstrated that both the SLN and NLC formulations possessed a controlled release over a period of 24 hrs. SLN and NLC formulations were subjected to stability over a period of 40 days. There was no significant (P<0.05) change in particle size, zeta potential, PDI and entrapment efficiency indicating the developed SLN and NLC were fairly stable.
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Parkinsonism, tremor, chorea-ballismus, dystonia, tardive dyskinesia, myoclonus, tics and akathisia can be induced by many drugs. The drugs that are most frequently implicated in movement disorders are antipsychotics, calcium antagonists, orthopramides and substituted benzamides (e.g. metoclopramide, sulpiride, clebopride, domperidone), CNS stimulants, antidepressants, anticonvulsants, antiparkinsonian drugs and lithium. It is possible for a single drug to induce 2 or more types of movement disorders in the same patient. Movement disorders are not always reversible after drug withdrawal.
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1. The influence of the selective DA1-agonist fenoldopam and the selective DA2-agonist quinpirole was investigated in the guinea-pig intact stomach model and in guinea-pig gastric corpus muscle strips. 2. In the intact stomach model, quinpirole induced a relaxation from 10(-6) M on. The relaxation by quinpirole (3 x 10(-5) M) was significantly inhibited by rauwolscine (10(-7) M), yohimbine (10(-7) M) and domperidone (10(-6) M). In the presence of tetrodotoxin, quinpirole (3 x 10(-5) M) induced a contraction. 3. In the same model, fenoldopam induced a relaxation but only at 3 x 10(-5) M. The relaxation by fenoldopam (3 x 10(-5) M) was not inhibited by SCH 23390 (10(-6) M). The relaxant effect of dopamine (3 x 10(-6) M) was significantly inhibited by rauwolscine (10(-7) M), yohimbine (3 x 10(-7) M), haloperidol (10(-6) M) and domperidone (10(-6) M). 4. In circular muscle strips of the gastric corpus, the electrically induced cholinergic contractions were inhibited by dopamine but not consistently influenced by quinpirole or fenoldopam. 5. Dopamine, fenoldopam and quinpirole induced an increase in basal tone of the strips. The contraction by dopamine (10(-5) M) was significantly antagonized by prazosin and methysergide. 6. No evidence was thus found for the presence of DA1-receptors in both guinea-pig stomach models. Equally, no evidence for the presence of DA2-receptors was found when studying quinpirole in the strips. Although the relaxant effect of quinpirole in the intact stomach seems predominantly mediated via alpha 2-adrenoceptors, an involvement of DA2-receptors cannot be excluded.
Homogenates of the pituitary of the goldfish (Carassius auratus) were incubated with [3H]spiperone under various experimental paradigms to evaluate the binding characteristics of the goldfish pituitary dopamine receptor. Binding was tissue specific as binding of [3H]spiperone to goldfish pituitary was greater than other tissue types examined, and the magnitude of binding was found to be dependent on pituitary (protein) content; also, specific binding was heat labile. Association was rapid and binding was reversible (dissociable) by addition of excess competing ligand (domperidone, a specific dopamine D2 receptor antagonist); the half-life (t1/2) of dissociation was 9.2 min and the estimated dissociation rate constant (k-1) was 7.56 x 10(-2) min-1); as well, the association rate was temperature dependent. Binding was saturable; saturation analysis using [3H]spiperone indicated a single class of binding sites with an estimated dissociation constant (Kd) and capacity of 7.39 +/- 1.23 x 10(-6) M and 31.56 +/- 2.72 x 10(-9) mol/mg protein, respectively. [3H]Spiperone binding was displaceable; displacement analysis using unlabeled domperidone indicated a single class of binding sites with estimated Kd and capacity of 2.94 +/- 0.54 x 10(-6) M and 19.47 +/- 3.12 x 10(-9) mol/mg protein, respectively. Binding was specifically inhibited by various dopamine antagonists and agonists. The density of binding sites differed significantly between regions of the goldfish pituitary; the number of binding sites in the pars distalis and neurointermediate lobes was estimated as 38.89 +/- 2.07 x 10(-9) mol/mg protein vs 109.45 +/- 25.33 x 10(-9) mol/mg protein, respectively; while the Kd's estimated as 3.73 +/- 0.248 x 10(-6) M vs 4.1 +/- 1.21 x 10(-6) M, respectively, were not significantly different. These data agree with previous in vivo and in vitro findings of the biological actions of dopamine agonists and antagonists in modifying gonadotropic hormone release in the goldfish and represent the first demonstration of the existence and binding characteristics of a dopamine/neuroleptic receptor in the pituitary of a nonmammalian vertebrate.
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This was a preliminary, prospective non-randomised, unblinded case-crossover study conducted in patients with longstanding, uncontrolled diabetes mellitus and gastroparesis. All patients received domperidone (20 mg four times a day) for 12 weeks, followed by a 2-3 week washout period, and then biweekly acupuncture treatments for 8 weeks. Gastric emptying rate, glucose and glycated haemoglobin (HbA1C) levels were measured at start and end of each treatment period. At each of these timepoints patients completed the Gastroparesis Cardinal Symptom Index (GCSI), the Satisfaction with Life Scale (SWLS), and the Short-Form 36 Health Survey Update (SF-36).
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Both cisapride and domperidone seem to be efficacious in functional dyspepsia, although this conclusion is largely based on global assessment by the investigator, which may not be an optimal outcome measure.
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Most patients with PD have a speech disorder. Of those, 89% have involvement of laryngeal function, and 45% have additional articulatory dysfunction. The effect of dopaminergic medications on these two dimensions of speech impairment in PD has not been selectively studied.
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The aim of this study was to identify SNPs that are associated with clinical efficacy and side effects of domperidone treatment for gastroparesis from DNA microarray experiments. This will help develop a strategy for rational selection of patients for domperidone therapy.
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Antidopaminergic gastrointestinal prokinetics (bromopride, clebopride, domperidone, levosulpiride and metoclopramide) have been exploited clinically for the management of motor disorders of the upper gastrointestinal tract, including functional dyspepsia, gastric stasis of various origins and emesis. The prokinetic effect of these drugs is mediated through the blockade of enteric (neuronal and muscular) inhibitory D2 receptors. The pharmacological profiles of the marketed compounds differ in terms of their molecular structure, affinity at D2 receptors, ability to interact with other receptor systems [5-hydroxytryptamine-3 (5-HT3) and 5-HT4 receptors for metoclopramide; 5-HT4 receptors for levosulpiride) and ability to permeate the blood-brain barrier (compared with the other compounds, domperidone does not easily cross the barrier). It has been suggested that the serotonergic (5-HT4) component of some antidopaminergic prokinetics may enhance their therapeutic efficacy in gastrointestinal disorders, such as functional dyspepsia and diabetic gastroparesis. The antagonism of central D2 receptors may lead to both therapeutic (e.g. anti-emetic effect due to D2 receptor blockade in the area postrema) and adverse (including hyperprolactinaemia and extrapyramidal dystonic reactions) effects. As the pituitary (as well as the area postrema) is outside the blood-brain barrier, hyperprolactinaemia is a side-effect occurring with all antidopaminergic prokinetics, although to different extents. Extrapyramidal reactions are most commonly observed with compounds crossing the blood-brain barrier, although with some differences amongst the various agents. Prokinetics with a high dissociation constant compared with that of dopamine at the D2 receptor (i.e. compounds that bind loosely to D2 receptors in the nigrostriatal pathway) elicit fewer extrapyramidal signs and symptoms. A knowledge of central and peripheral D2 receptor pharmacology can help the clinician to choose between the antidopaminergic prokinetics to obtain a more favourable risk/benefit ratio.
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Dopamine (DA) induction of the long-term enhancement (LTE) of the slow muscarinic depolarizing response to methacholine (MCh), equivalent to the slow EPSP (S-EPSP), was previously found to be mimicked by exogenous cyclic AMP (cAMP) in the rabbit superior cervical ganglion (SCG). DA-induced LTE of the S-EPSP was shown to be depressed by some DA antagonists. We now show that DA (15 microM), its analog, 2-amino-6,7-dihydroxy-1,2,3,4-tetrahydronaphthalene (ADTN), and a D2 receptor antagonist, metoclopramide, each can induce both LTE of MCh depolarization and an increase in ganglionic cAMP. Conversely, antagonists of DA-induced LTE also depress DA-induced rises in cAMP; these antagonists include haloperidol (1 microM), both (+) and (-) enantiomers of butaclamol (0.7-7 microM), flupenthixol (1 microM), and (+)-R-8-chloro-2,3,4,5-tetrahydro-3-methyl-5-phenyl-1H-3-benzazepine-7-o l (SCH-23390) (7 microM). The selective D2 antagonists sulpiride (10 microM) and domperidone (10 microM) affect neither DA action. Alpha-2 adrenergic agonists (alpha-methyl-norepinephrine and clonidine) produce no LTE; alpha-antagonist dihydroergotamine (35 microM) does not affect either DA action, although it can completely block the hyperpolarizing response to DA or other catecholamines. Beta-antagonist propranolol (5 microM) partially depresses DA-induced rises in cAMP but has no effect on the DA-induced LTE. (Butaclamol and propranolol in combination can completely block the cAMP rise induced by DA.) Beta-agonist isoproterenol can induce appreciable LTE of MCh depolarization, but this LTE is not depressed by propranolol (10 microM). Isoproterenol can elicit a substantial rise in cAMP.(ABSTRACT TRUNCATED AT 250 WORDS)
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Inducing lactation in the absence of pregnancy (nonpuerperal lactation) is not always successful and, in many cases, only partial breastfeeding is achieved. Different protocols have been described, but scientific evidence and research are lacking in this area. The authors describe the case of a woman with a history of a miscarriage, for whom the lactation induction process was so effective that she became a milk donor even before she received her adopted child. She had not previously used hormone treatment. She was given domperidone as a galactogogue for 1 month. The pumping protocol began with a double electric breast pump combined with manual pumping 6 months before her child was delivered, and 3 months later, she was accepted as a donor by our milk bank. This highlights the importance of regular stimulation as a milk production mechanism. This is the first case of human milk donation in an adoptive mother described in the literature.