Interactions of (+)- and (-)-8- and 7-hydroxy-2-(di-n-propylamino)tetralin at human (h)D3, hD2 and h serotonin1A receptors and their modulation of the activity of serotoninergic and dopaminergic neurones in rats.

The aminotetralins, 8-hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) and 7-OH-DPAT behave as preferential agonists at serotonin (5-HT)1A and dopamine D3 and D2 receptors, respectively. In our study, we evaluated the influence of their (+)- and (-) isomers on the electrical activity of serotoninergic neurones of the dorsal raphe nucleus (DRN), which bear 5-HT1A autoreceptors, and of dopaminergic neurones of the ventral tegmental area (VTA), which possess inhibitory D3 and D2 receptors. These actions were compared to their in vitro interactions with cloned, human (h)5-HT1A, hD3 and hD2 receptors.

Buspirone enhances duloxetine- and fluoxetine-induced increases in dialysate levels of dopamine and noradrenaline, but not serotonin, in the frontal cortex of freely moving rats.

A serotonin (5-HT)1A receptor partial agonist, buspirone, potentiates the clinical antidepressant properties of 5-HT reuptake inhibitors (SSRIs). Herein, we examined the interaction of buspirone with two SSRIs, duloxetine and fluoxetine, on extracellular levels of 5-HT, dopamine (DA), and noradrenaline (NAD) in single dialysate samples of freely moving rats. Duloxetine (5.

Potentiation of the fluoxetine-induced increase in dialysate levels of serotonin (5-HT) in the frontal cortex of freely moving rats by combined blockade of 5-HT1A and 5-HT1B receptors with WAY 100,635 and GR 127,935.

In this study, we examined the influence of blockade of serotonin (5-HT)1A and/or 5-HT1B autoreceptors on the fluoxetine-induced increase in dialysate levels of 5-HT as compared with dopamine (DA) and noradrenaline (NAD) in single samples of the frontal cortex (FCx) of freely moving rats. Fluoxetine (10.0 mg/kg, s.

Human monocytes activate porcine endothelial cells, resulting in increased E-selectin, interleukin-8, monocyte chemotactic protein-1, and plasminogen activator inhibitor-type-1 expression.

Monocytes (Mo) are thought to be important effector cells in early xenograft rejection. Effects of Mo-endothelial cell (EC) interactions on EC activation in vitro were studied by coculturing human Mo or human monocytoid cell lines, U937 and THP-1, with porcine EC. Without preactivation, U937 cells and Mo induced mRNA for the EC-specific adhesion receptor, E-selectin, expressed only on activated cells, after 2 hr.

Noradrenaline and adrenaline are high affinity agonists at dopamine D4 receptors.

The activity of monoamine neurotransmitters was examined at dopamine D4 receptors. In competition binding with [3H]spiperone, noradrenaline and adrenaline exhibited a high affinity binding component (KH = 12.1 nM and 5.

Loss of ATP diphosphohydrolase activity with endothelial cell activation.

Quiescent endothelial cells (EC) regulate blood flow and prevent intravascular thrombosis. This latter effect is mediated in a number of ways, including expression by EC of thrombomodulin and heparan sulfate, both of which are lost from the EC surface as part of the activation response to proinflammatory cytokines. Loss of these anticoagulant molecules potentiates the procoagulant properties of the injured vasculature.

Evaluation of the diabetes quality-of-life questionnaire in a Spanish population. An experience of translation and reliability.

The aim of this study was to evaluate the reliability of a version of the diabetes quality-of-life (DQOL) questionnaire adapted and translated into Spanish. The DQOL questionnaire consists of 46 items and is not sensitive to treatment regimens or self-monitoring; therefore, the instrument might be useful to a wide range of patients with diabetes who use different methods of diabetes management. 105 patients with insulin-dependent diabetes mellitus volunteered to complete the questionnaire.

Fourier-domain-based angular correlation for quasiperiodic pattern recognition. Applications to web inspection.

A Fourier-domain-based recognition technique is proposed for periodic and quasiperiodic pattern recognition. It is based on the angular correlation of the moduli of the sample and the reference Fourier spectra centered at the maximum central point. As in other correlation techniques, recognition is achieved when a high correlation peak is obtained, and this result occurs when the two spectra coincide.

[Presence of markers predictive of type I pre-diabetes mellitus status in relatives of patients with type I diabetes mellitus].

Background: The aim of this study was to analyze the predictive factors of IDDM in first degree relatives of IDDM patients.

Subjects And Methods: From 1992 to 1994, 1,053 first degree relatives were screened for measuring islet cell antibodies (ICA) by indirect immunofluorescence (iFl). In all ICA positive subjects, beta cell function was analyzed by intravenous glucose tolerance test (IVGTT) and other immunologic parameters were also studied: anti-insulin antibodies (IAA) by radiobinding and antibodies to glutamic acid decarboxylase (GADAb) by ELISA methods.

S 15535 and WAY 100,635 antagonise 5-HT-stimulated [35S]GTP gamma S binding at cloned human 5-HT1A receptors.

In Chinese hamster ovary (CHO) cells expressing cloned human 5-HT1A receptors, S 15535 (4-(benzodioxan-5-yl)1-(indan-2-yl)piperazine) exhibited high affinity (Ki = 0.79 nM), similar to that of 5-HT (0.61 nM), (+/-)-8-hydroxy-3-(di-n-propylamino)tetralin ((+/-)-8-OH-DPAT; 0.

Dopamine D3 (auto) receptors inhibit dopamine release in the frontal cortex of freely moving rats in vivo.

In freely moving rats, the novel, selective dopamine (DA) D3 receptor agonist PD 128,907 dose-dependently [effective dose (ED25) = 0.07 mg/kg, s.c.

Direct activation of porcine endothelial cells by human natural killer cells.

Endothelial cell (EC) activation is a consistent feature of discordant xenograft rejection. Treatment of xenograft recipients with complement inhibitors and xenoreactive natural antibody depletion leads to delayed xenograft rejection associated with a cellular infiltrate comprising up to 20% natural killer (NK) cells. To determine the importance of NK cells in xenograft rejection, we studied EC activation and cytotoxicity in co-cultures containing human NK cells and porcine EC.

Relationship between drug percolation threshold and particle size in matrix tablets.

Purpose: Since a previous qualitative study carried out by us showed the existence of an important influence of the particle size on the percolation thresholds and taking into account that the existing theoretical models can only provide qualitative explanation to this influence, the purpose of this work is to carry out the first quantitative study of the influence of the particle size over the drug percolation thresholds.

Methods: Matrix tablets have been elaborated using potassium chloride as drug model and Eudragit RS-PM as matrix forming material. Five different KCl particle size fractions have been employed whereas the Eudragit RS-PM particle size was kept constant.

Down-regulation of rat beta-adrenoceptors by clenbuterol or desipramine does not require chronic treatment: [3H] CGP-12177 binding reveals rapid (24 hour) modulation.

Desipramine (DMI, 15 mg/kg, s.c.) decreased [3H]CGP-12177-labelled cortical beta-adrenoceptor density (Bmax) by 30% upon chronic (14 day) treatment.

Pro- and antinociceptive actions of serotonin (5-HT)1A agonists and antagonists in rodents: relationship to algesiometric paradigm.

In mice injected with formalin into the hindpaw, the 5-HT1A receptor agonists, 8-OH-DPAT and flesinoxan, equipotently inhibited the early phase (EP) and late phase (LP) of licking. At higher doses, they provoked ataxia and inhibited the writhing elicited by intra-abdominal acetic acid. The antagonists, (-)-alprenolol, (-)-tertatolol, WAY-100,135 and S 15931 were more potent against the LP than the EP.

Clozapine is a partial agonist at cloned, human serotonin 5-HT1A receptors.

Clozapine exhibited 10-fold higher affinity than haloperidol for human 5-HT1A receptors expressed in Chinese Hamster Ovary cells (CHO-h5-HT1A) (Kis = 160 and 1910 nM respectively). Whereas haloperidol did not alter the basal binding of [35S]GTP gama S to CHO-h5HT1A membranes, clozapine stimulated it with an EC50 of 2320 nM and an efficacy of 49% (compared to 5-HT). The stimulation was antagonized by the selective 5-HT1A receptor antagonist, WAY 100635 (1 nM).

[3H](+)S 14297: a novel, selective radioligand at cloned human dopamine D3 receptors.

The selective dopamine D3 receptor antagonist [3H](+)S 14297 ((+)-[7-(N,N-dipropylamino)-5,6,7,8-tetrahydro-naphtho(2,3b)dihydro,2,3- furane]), labelled to high specific activity (145 Ci/mmol), bound to cloned human dopamine D3 receptors but displayed negligible binding to cloned human D2 receptors. [3H](+)S 14297 exhibited rapid association and dissociation, high affinity saturable binding (Kd = 7.0 nM) and a competition binding profile highly correlated with that of [125I]iodosulpride (r = 0.

Suppurative pylephlebitis and pylethrombosis: the role of anticoagulation.

Suppurative thrombophlebitis of the portal vein resulting from inflammatory intra-abdominal conditions is a rare complication that may result in pylethrombosis and portal hypertension. A case is presented with documented pylethrombosis caused by diverticulitis. Color flow Doppler scanning was used to establish the diagnosis.

Functional correlates of dopamine D3 receptor activation in the rat in vivo and their modulation by the selective antagonist, (+)-S 14297: II. Both D2 and "silent" D3 autoreceptors control synthesis and release in mesolimbic, mesocortical and nigrostriatal pathways.

The preferential dopamine (DA) D3 versus D2 receptor agonist, (+)-7-OH-DPAT, dose-dependently decreased DA synthesis in the nucleus accumbens, olfactory tubercles, striatum and frontal cortex. This action was potently mimicked by several other high-potency D3 agonists: CGS 15855A, (-)-quinpirole, quinelorane and N-0434. In contrast, piribedil, which displays a mild preference for D2 sites, was less active.