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Seung Jae Lee et al.
Clinical drug investigation, 32(11), 735-745 (2012-09-29)
It has been suggested that neither dose titration nor the use of a loading dose was required for amisulpride and that 800 mg/day could be given from the first day with a low risk of extrapyramidal symptoms (EPS). However, no
W Hauber et al.
Behavioural brain research, 106(1-2), 143-150 (1999-12-14)
In the present study, the involvement of dopamine D1 and D2 receptors in the dorsal globus pallidus (GP) in motor control was investigated in rats. Results show that bilateral microinfusions of the dopamine D1 receptor antagonist SCH23390 or the dopamine
M C Mauri et al.
Drug safety, 14(5), 288-298 (1996-05-01)
Sulpiride is a substituted benzamide with a selective action on receptors of the dopamine D2-like family, and clinical and pharmacological data suggest that it could be considered to be an atypical antipsychotic. Sulpiride penetrates the blood-brain barrier poorly because of
C F Caley et al.
The Annals of pharmacotherapy, 29(2), 152-160 (1995-02-01)
To review the pharmacology, pharmacokinetics, clinical investigations, and adverse effects of sulpiride as a treatment for schizophrenia. Information was selected from a MEDLINE search of English-language medical literature using "sulpiride" as the search term. Manual searches of pertinent journal article
Jeetendra Singh Negi et al.
Carbohydrate polymers, 92(2), 1835-1843 (2013-02-13)
The purpose of this research was to investigate inclusion complex formation between poorly soluble drug amisulpride (AMI) and γ-cyclodextrin (γ-CD). The solubility of AMI was enhanced by formation of inclusion complex of AMI with nano-hydrophobic cavity of γ-CD. The stoichiometry
Tomoko Minakuchi et al.
Journal of medicinal chemistry, 52(8), 2226-2232 (2009-03-26)
The beta-carbonic anhydrase (CA, EC 4.2.1.1) encoded by the gene Rv1284 (mtCA 1) of Mycobacterium tuberculosis shows appreciable catalytic activity for CO(2) hydration, with a k(cat) of 3.9 x 10(5) s(-1) and a k(cat)/K(m) of 3.7 x 10(7) M(-1) s(-1).
Isao Nishimori et al.
Journal of medicinal chemistry, 48(24), 7860-7866 (2005-11-24)
A lately discovered carbonic anhydrase (hCA, EC 4.2.1.1), the mitochondrial hCA VB, was cloned, expressed, and purified. Kinetic parameters proved it to be 3.37 times more effective than hCA VA as a catalyst for the physiological reaction, with kcat =
Anaphylaxis due to sulpiride and sensitization to metamizole.
M I Alvarado et al.
Journal of investigational allergology & clinical immunology, 22(5), 379-380 (2012-10-30)
José M Entrena et al.
Psychopharmacology, 205(1), 21-33 (2009-03-28)
We evaluated the effects of haloperidol and its metabolites on capsaicin-induced mechanical hypersensitivity (allodynia) and on nociceptive pain induced by punctate mechanical stimuli in mice. Subcutaneous administration of haloperidol or its metabolites I or II (reduced haloperidol) dose-dependently reversed capsaicin-induced
J A Keja et al.
The Journal of physiology, 450, 409-435 (1992-05-01)
1. Whole-cell voltage clamp recordings were made from 141 rat pituitary melanotropic cells in short-term, serum-free, primary culture. The effects of the dopamine D2 receptor agonist, LY 171555, on sodium, potassium and barium currents were investigated. 2. Application of 1
Daniela Vullo et al.
Bioorganic & medicinal chemistry letters, 15(4), 963-969 (2005-02-03)
The inhibition of a newly cloned human carbonic anhydrase (CA, EC 4.2.1.1), isozyme XII (hCA XII), has been investigated with a series of sulfonamides, including some clinically used derivatives (acetazolamide, methazolamide, ethoxzolamide, dichlorophenamide, dorzolamide, brinzolamide, benzolamide, and sulpiride, or indisulam
Elisabeth Piccart et al.
The Journal of neuroscience : the official journal of the Society for Neuroscience, 35(31), 11144-11152 (2015-08-08)
Increased dopaminergic signaling is a hallmark of severe mesencephalic pathologies such as schizophrenia and psychostimulant abuse. Activity of midbrain dopaminergic neurons is under strict control of inhibitory D2 autoreceptors. Application of the modulatory peptide neurotensin (NT) to midbrain dopaminergic neurons
S V Kuznetsov et al.
Zhurnal evoliutsionnoi biokhimii i fiziologii, 48(4), 367-379 (2012-09-28)
Study of parameters of the cardiac, respiratory, and motor activity (MA) was carried out on newborn rat pups for the first day after birth (P0) and at the 14th day of postnatal development (P14) after change of the level of
Kiera-Nicole Lee et al.
PloS one, 10(8), e0135578-e0135578 (2015-08-15)
Formation of episodic memories (i.e. remembered experiences) requires a process called consolidation which involves communication between the neocortex and hippocampus. However, the neuromodulatory mechanisms underlying this neocortico-hippocampal communication are poorly understood. Here, we examined the involvement of dopamine D1 receptors
Pär Matsson et al.
Journal of medicinal chemistry, 48(2), 604-613 (2005-01-22)
The influence of different drug transport routes in intestinal drug permeability screening assays was studied. Three experimental models were compared: the small-intestine-like 2/4/A1 cell model, which has a leaky paracellular pathway, the Caco-2 cell model, which has a tighter paracellular
K R Müller-Vahl
Der Nervenarzt, 78(3), 264-264 (2006-08-23)
The treatment of Tourette's syndrome is a challenge. Dopamine receptor antagonists are the drugs of first choice for the treatment of tics. Because large controlled trials are lacking, there is no consensus about which of the different neuroleptic drugs should
Giuseppina De Simone et al.
Journal of medicinal chemistry, 49(18), 5544-5551 (2006-09-01)
An approach for designing bioreductive, hypoxia-activatable carbonic anhydrase (CA, EC 4.2.1.1) inhibitors targeting the tumor-associated isoforms is reported. Sulfonamides incorporating 3,3'-dithiodipropionamide/2,2'-dithiodibenzamido moieties were prepared and reduced enzymatically/chemically in conditions present in hypoxic tumors, leading to thiols. The X-ray crystal structure
Krzysztof Ciszowski et al.
Przeglad lekarski, 67(8), 606-609 (2010-01-01)
Sulpiride is a benzamide neuroleptic used in the treatment of some psychiatric and gastroenterological disorders. Its antipsychotic, antiautistic, activizing and antidepressive properties result from antagonistic action to dopaminergic D2, D3 and D4 receptors in the central nervous system (CNS). The
Saeid Yazdi-Ravandi et al.
Pharmacology, biochemistry, and behavior, 126, 1-6 (2014-09-03)
Previous studies have shown that there are functional interactions among the lateral hypothalamus (LH), ventral tegmental area (VTA) and the nucleus accumbens (NAc), implicating pain modulation in the central nervous system. It has been shown that the LH-VTA orexinergic projecting
S E O'Connor et al.
General pharmacology, 13(3), 185-193 (1982-01-01)
1. The clinical and experimental pharmacology of sulpiride, its effects on the CNS, gastrointestinal tract and cardiovascular system have been reviewed. 2. The majority of its actions are attributable to blockade of dopamine receptors. 3. Although sulpiride has a high
Pil H Lee et al.
Bioorganic & medicinal chemistry letters, 20(1), 69-73 (2009-12-08)
A multiple linear regression QSAR model was developed based on a set of 61 compounds with internally consistent permeability data measured across Franz cell. The data was normalized using a mean permeability value of a reference compound, 3-isobutyl-1-methylxanthine (IBMX). The
Sven Kroener et al.
PloS one, 4(8), e6507-e6507 (2009-08-06)
The importance of dopamine (DA) for prefrontal cortical (PFC) cognitive functions is widely recognized, but its mechanisms of action remain controversial. DA is thought to increase signal gain in active networks according to an inverted U dose-response curve, and these
Peter J Gaskill et al.
PloS one, 9(9), e108232-e108232 (2014-10-01)
Macrophages are the primary cell type infected with HIV in the central nervous system, and infection of these cells is a major component in the development of neuropathogenesis and HIV-associated neurocognitive disorders. Within the brains of drug abusers, macrophages are
Anthony Bertucci et al.
Bioorganic & medicinal chemistry letters, 21(2), 710-714 (2011-01-07)
The catalytic activity and the inhibition of a new coral carbonic anhydrase (CA, EC 4.2.1.1), from the scleractinian coral Stylophora pistillata, STPCA-2, has been investigated. STPCA-2 has high catalytic activity for the physiological reaction being less sensitive to anion and
S Berretta et al.
The European journal of neuroscience, 11(12), 4309-4319 (1999-12-14)
Dopamine D2-class receptors have been shown to control the excitability of striatal neurons in response to cortical activation. It has been unclear, however, whether such receptors could regulate the number of striatal neurons activated by cortical stimulation, and thus affect
Isao Nishimori et al.
Journal of medicinal chemistry, 50(2), 381-388 (2007-01-19)
The secretory isozyme of human carbonic anhydrase (hCA, EC 4.2.1.1), hCA VI, has been cloned, expressed, and purified in a bacterial expression system. The kinetic parameters for the CO2 hydration reaction proved hCA VI to possess a kcat of 3.4
Phedias Diamandis et al.
Nature chemical biology, 3(5), 268-273 (2007-04-10)
The identification of self-renewing and multipotent neural stem cells (NSCs) in the mammalian brain holds promise for the treatment of neurological diseases and has yielded new insight into brain cancer. However, the complete repertoire of signaling pathways that governs the
Abbas Haghparast et al.
Neuroscience letters, 556, 10-14 (2013-10-10)
Our previous study showed that chemical stimulation of the lateral hypothalamus (LH) by carbachol can produce conditioned place preference (CPP) in rats. Also, it has been indicated that orexin activates the mesolimbic dopamine projecting neurons to the nucleus accumbens (NAc)
Manthena V S Varma et al.
Journal of medicinal chemistry, 52(15), 4844-4852 (2009-05-19)
Kidney plays an important role in the elimination of drugs, especially with low or negligible hepatic clearance. An analysis of the interrelation of physicochemical properties and the human renal clearance for a data set of 391 drugs or compounds tested
Denis Fourches et al.
Chemical research in toxicology, 23(1), 171-183 (2009-12-18)
Drug-induced liver injury is one of the main causes of drug attrition. The ability to predict the liver effects of drug candidates from their chemical structures is critical to help guide experimental drug discovery projects toward safer medicines. In this
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