Search results for "PAM"
showing 10 items of 1768 documents
Biochemical evidence that the atypical antipsychotic drugs clozapine and risperidone block 5-HT(2C) receptors in vivo.
2002
Clozapine and risperidone are two atypical antipsychotic drugs which bind, among other receptors, to 5-HT(2C) receptor subtypes. They inhibit the basal inositol phosphate production in mammalian cells expressing rat or human 5-HT(2C) receptors. This biochemical effect is indicative of inverse agonist activity at these receptors. There is evidence that 5-HT(2C) receptors are involved in the control of the activity of central dopaminergic system. Therefore, the effects of clozapine (5 mg/kg ip), risperidone (0.08 mg/kg ip) and of the typical antipsychotic haloperidol (0.1 mg/kg ip) were studied on the extracellular concentration of dopamine (DA) in the nucleus accumbens of chloral hydrate-ane…
Low-dose dopamine agonist administration blocks vascular endothelial growth factor (VEGF)-mediated vascular hyperpermeability without altering VEGF r…
2006
No specific treatment is available for ovarian hyperstimulation syndrome (OHSS), the most important complication in infertile women treated with gonadotropins. OHSS is caused by increased vascular permeability (VP) through ovarian hypersecretion of vascular endothelial growth factor (VEGF)activating VEGF receptor 2 (VEGFR-2). We previously demonstrated in an OHSS rodent model that increased VP was prevented by inactivating VEGFR-2 with a receptor antagonist(SU5416).However,duetoitstoxicity(thromboembolism) and disruption of VEGFR-2-dependent angiogenic processes critical for pregnancy, this kind of compound cannot be used clinically to prevent OHSS. Dopamine receptor 2 (Dp-r2) agonists, use…
Modulation by fenoldopam (SKF 82526) and bromocriptine of the electrically evoked release of vasopressin from the rat neurohypophysis. Effects of dop…
1986
1. Single neurointermediate lobes were fixed by their stalks to a platinum wire electrode and incubated in Krebs-bicarbonate solution. Vasopressin release into the medium was determined by a radioimmunoassay. Vasopressin secretion was increased by electrical stimulation (15 Hz, 10 s trains with 10 s intervals for 10 min). 2. Fenoldopam (SKF 82526) had a dual effect on vasopressin release, 30 nM decreasing (by 30%) and 3 μM increasing (by 32%) the evoked vasopressin secretion. The facilitatory effect of fenoldopam was antagonized in a concentration-dependent manner by flupenthixol but not by sulpiride. Sulpiride (1 μM) prevented the inhibitory effect of fenoldopam (30 μM). 3. After pretreatm…
WIN55,212-2, a cannabinoid receptor agonist, protects against nigrostriatal cell loss in the 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine mouse model…
2009
Parkinson's disease (PD) is characterized by the progressive loss of nigrostriatal dopamine neurons leading to motor disturbances and cognitive impairment. Current pharmacotherapies relieve PD symptoms temporarily but fail to prevent or slow down the disease progression. In this study, we investigated the molecular mechanisms by which the non-selective cannabinoid receptor agonist WIN55,212-2 (WIN) protects mouse nigrostriatal neurons from 1-methyl-4-phenyl-1,2,3,6-tetrahydropyridine (MPTP)-induced neurotoxicity and neuroinflammation. Stereological analyses showed that chronic treatment with WIN (4 mg/kg, intraperitoneal), initiated 24 h after MPTP administration, protected against MPTP-ind…
Roxindole, a dopamine autoreceptor agonist, in the treatment of positive and negative schizophrenic symptoms
1994
Twenty schizophrenic inpatients with either predominantly positive or predominantly negative symptoms were treated with the dopamine autoreceptor agonist roxindole in prospective open clinical trials. There was no antipsychotic effect in the subgroup with positive symptoms, whereas the subgroup with negative symptoms, especially those with the residual type of schizophrenia, showed a moderate but significant 20% reduction in total scores on the Scale for the Assessment of Negative Symptoms.
Biogenic Amines Modulate Olfactory Receptor Neurons Firing Activity in Mamestra brassicae
2001
The modulatory effects of the biogenic amines octopamine and serotonin on pheromonal receptor neurons of Mamestra brassicae were investigated. The responses to sex pheromone components of two cells types (A and B) in single male long sensilla trichodea were monitored. Cell types A and B do not respond to the same compound. The response of type A to a pulse of the major sex pheromone component increased 5 min after octopamine injection. Responses of type B to other odorants increased after 30 min. In the absence of any pheromone stimulation the background firing activity of type A increased following octopamine injection. This background activity was used to evaluate the kinetics of octopami…
Die nächste Generation „atypischer” Antipsychotika: Der Beitrag der Positronenemissionstomographie
2003
Almost fifteen years of research with Positron Emission Tomography (PET) and Single Photon Emission Computed Tomography (SPECT) have led to a profound understanding of the relationships between antipsychotic doses and plasma levels on the one hand and occupancy of (striatal) D 2 -like dopamine receptors on the other hand as well as with the associated clinical effects and side effects. Furthermore, with the development of clinically atypical" antipsychotics PET studies helped to generate hypotheses regarding the essential pharmacological properties of this heterogeneous class of drugs. Possible mechanisms of action include combined D 2 -/5-HT 2 antagonism, preferential mesolimbic binding, a…
Study of the Expression of Angiogenic Factors and Dopaminergic Receptors: Correlation with ZAP70, CD38 and the Mutational State in Chronic Lymphocyti…
2006
Abstract The angiogenesis is a well known process implicate in the progression of CLL. In this disease has been described an increase of angiogenic and pro-angiogenic factors in serum and angiogenic receptors in B cells, mainly in advances stages. Recently had been known that the agonist of the dopaminergic receptor D2 can inhibit the tumour growth and a possible mechanism mediator is the internalization of VEGFR-2. The aim of this work had been to analyze the expression of the dopaminergic receptors (D1, D2, D3, D4 and D5), the angiogenic receptors and its correlation with the main biological factor implicated in the illness (ZAP-70, CD38 and the mutational status of IgVH/BCL-6). We had de…
Pamatlīdzekļi un to uzskaite un analīze SIA "APLIS"
2020
Maģistra darba mērķis ir, pamatojoties uz pamatlīdzekļu uzskaites un analīzes teorētisko nostādņu analīzi, novērtēt pamatlīdzekļu uzskaites politiku uzņēmumā APLIS un uzglabāšana un noliktavu saimniecības nozarē kopumā, kā rezultātā izstrādāt priekšlikumus identificēto nepilnību novēršanai SIA APLIS. Pētījumā noskaidrots, ka noliktavas un uzglabāšanas nozarē pamatā dominē uzņēmumi, kas klasificējas, kā MVU, šiem uzņēmumiem populārākā pamatlīdzekļu novērtēšanas metode ir izmaksu metode, bet pamatlīdzekļu nolietojuma aprēķinā pielieto lineāro pamatlīdzekļu nolietojuma metodi. Atslēgvārdi - pamatlīdzekļi, pamatlīdzekļu uzskaite, aktīvi, bilance.
»…vzpomínám na něho ustavičně a přeji mu, aby se mu tatínek brzo vrátil«. O (terapeutycznej) roli pamięci w korespondencji więziennej Jana Zahradníčka
2020
Przedmiotem analizy są listy czeskiego poety Jana Zahradníčka wysyłane z komunistycznego więzienia do żony Marii w latach 1951–1960. Wybór to zapis zarówno życiowej traumy wynikającej z długo letniej izolacji oraz tragedii rodzinnej (śmierć dwóch córek), a jednocześnie świadectwo tego, że dzięki terapeutycznej roli pamięci autor przetrwał ów trudny czas. Punktem wyjścia są m. in. rozważania Aleidy Assmann, które co prawda prymarnie odnosiły się do pamięci kolektywnej społeczeństw dotkniętych traumatyczną przeszłością, ale mogą być także użyteczne dla rozpatrywanego tutaj studium przypadku jednostki.