Search results for "Penicillamine"
showing 10 items of 27 documents
δ 1‐OPIOID receptor‐mediated controlofacetylcholine (ACh) release in human neocortex slices
1998
In slices of human neocortex, prelabelled with [3H]-choline, the release of [3H]-acetylcholine reflects the evoked release of endogenous acetylcholine which was elicited by the same electrical stimulation paradigm. [3H]-Acetylcholine release was depressed by the delta-opioid receptor agonist D-Pen2-D-Pen5-enkephalin. When the nerve endings were depolarized by elevating extracellular potassium the evoked [3H]-acetylcholine release was similarly depressed by D-Pen2-D-Pen5-enkephalin in the absence, but not in the presence, of tetrodotoxin which blocks action potential propagation. Therefore, the delta-opioid receptor inhibiting [3H]-acetylcholine release should not be located to cholinergic n…
Correlation of nitric oxide and atrial natriuretic peptide changes with altered cGMP homeostasis in liver cirrhosis.
2005
: Background: Cyclic GMP (cGMP) concentration is increased in plasma of patients with liver cirrhosis. Three possible mechanisms may contribute: increased cGMP synthesis by soluble (activated by nitric oxide), or particulate (activated by atrial natriuretic peptide (ANP)) guanylate cyclase or increased release from cells. Aim: The aim of this work was to analyze the possible contributors to increased plasma cGMP and to assess whether changes in the parameters of the system vary with the degree of liver disease (Child Pugh score) or by the presence of ascites. Methods: We measured cGMP in plasma and lymphocytes, soluble guanylate cyclase activation by nitric oxide in lymphocytes, nitrates an…
Foetal erythrocytes exhibit an increased ability to scavenge for nitric oxide
1998
The presence of adult human whole blood inhibited in vitro relaxations of rat aortic rings by the nitric oxide (NO) donor S-nitroso-N-acetyl-DL-penicillamine (SNAP). Incubation with foetal blood containing the same concentration of haemoglobin produced a shift to the right of the relaxation curve. SNAP-induced vasorelaxations were more inhibited by dialysed solutions of haemoglobin than by the presence of erythrocytes in the organ bath, but there were no differences between the effect of adult or foetal haemoglobins. The presence of plasma from adult or foetal blood did not modify the effects of SNAP. Relaxations induced by endogenous, endothelium-derived, NO were more inhibited by foetal t…
Systemic administration of D-penicillamine prevents the locomotor activation after intra-VTA ethanol administration in rats.
2010
Although recently published studies seem to confirm the important role displayed by acetaldehyde (ACH), the main metabolite of ethanol, in the behavioral effects of ethanol, the origin of ACH is still a matter of debate. While some authors confer more importance to the central (brain metabolism) origin of ACH, others indicate that the hepatic origin could be more relevant. In this study we have addressed this topic using an experimental approach that combines local microinjections of ethanol into the ventral tegmental area (VTA) (which guarantees the brain origin of the ACH) to induce motor activation in rats together with systemic administration (i.p.) of several doses (0, 12.5, 25 and 50 …
Binding of Tat Protein to TAR Region of Human Immunodeficiency Virus Type 1 Blocks TAR-Mediated Activation of (2′-5′)Oligoadenylate Synthetase
1990
The TAR sequence of the 5' leader of HIV-1 long terminal repeat-directed mRNA was found to be able to bind to and to activate double-stranded RNA-dependent (2'-5')A synthetase. Binding of TAR to the purified synthetase in vitro was abolished by addition of HIV-1 Tat protein, which binds to this sequence with a high affinity. Inhibition of TAR-mediated activation of (2'-5')A synthetase by Tat was prevented in the presence of the Zn2+ and Cd2+ chelators o-phenanthroline and penicillamine, which did not impair TAR-synthetase interaction. Transient expression assays of bacterial chloramphenicol acetyltransferase (CAT) gene in HeLa cells revealed that the levels of both CAT mRNA and CAT protein …
In situ generation of Co(II) by use of a solid-phase reactor in an FIA assembly for the spectrophotometric determination of penicillamine
2005
[EN] A flow injection analysis (FIA) manifold for the determination of penicillamine in pharmaceutical preparations is proposed. The manifold includes a solid-phase reactor for the in situ production of the derivatizing reagent, Co(II) ion, which forms a coloured complex with penicillamine in an alkaline medium. The reactor is prepared by natural immobilization of cobalt carbonate on a polymer matrix, which endows it with a high mechanical and microbiological stability. The cobalt released by passage of a 5 x 10(-4) Mol l(-1) sulphuric acid stream at a flow-rate of 2.3 ml min(-1) is merged with a volume of 314 mu l of sample containing penicillamine in ammonium-ammonia buffer at pH 9.5 to m…
P-77D-PENICILLAMINE, A POTENTIAL ETHANOL ANTI-RELAPSE DRUG, DOES NOT REDUCE THE VOLUNTARY ETHANOL INTAKE IN LONG-TERM EXPERIENCED RATS
2015
Experimental evidence has demonstrated that the reinforcing effects of ethanol crucially depend on the brain formation of acetaldehyde (ACD). Rationally supported by this basis, we previously evaluated a novel strategy to prevent relapse in alcoholism based on chemical ACD inactivation using D-Penicillamine (DP). Under our experimental …
Pre-Clinical Studies with D-Penicillamine as a Novel Pharmacological Strategy to Treat Alcoholism: Updated Evidences
2017
Ethanol, as other drugs of abuse, is able to activate the ventral tegmental area dopamine (VTA-DA) neurons leading to positively motivational alcohol-seeking behavior and use, and, ultimately to ethanol addiction. In the last decades, the involvement of brain-derived acetaldehyde (ACD) in the ethanol actions in the mesolimbic pathway has been widely demonstrated. Consistent published results have provided a mechanistic support to the use of ACD inactivating agents to block the motivational and reinforcing properties of ethanol. Hence, in the last years, several pre-clinical studies have been performed in order to analyze the effects of the sequestering ACD agents in the prevention of ethano…
P-76D-PENICILLAMINE, AN ACETALDEHYDE SEQUESTERING AGENT, REDUCES ETHANOL PREFERENCE IN ALCOHOL-NAÏVE RATS
2015
In previous investigations, we demonstrated that D-penicillamine (DP), a sulfhydryl aminoacid which has been studied as sequestration agent of acetaldehyde (ACD), is able to prevent the alcohol deprivation effect (ADE) but not voluntary ethanol consumption. Both results were obtained in long-term ethanol-experienced Wistar rats. Based on a previous …
P-78D-PENICILLAMINE PREVENTS THE ALCOHOL DEPRIVATION EFFECT IN THE OPERANT SELF-AMINISTRATION PARADIGM
2015
Although pharmacological treatments for relapse prevention have experienced some progress, their general effectiveness can be considered low and the problem could not be considered solved. In recent years, our group has explored the use of acetaldehyde (ACD) sequestering agents as a new and very promising strategy. These agents, such as …