153 results on '"Filip, P."'
Search Results
2. Further proof on the role of accumbal nNOS in cocaine-seeking behavior in rats
3. Molecular pattern of a decrease in the rewarding effect of cocaine after an escalating-dose drug regimen
4. KM-408, a novel phenoxyalkyl derivative as a potential anticonvulsant and analgesic compound for the treatment of neuropathic pain
5. The effects of the recurrent social isolation stress on fear extinction and dopamine D2 receptors in the amygdala and the hippocampus
6. Evaluation of the 5-HT2C receptor drugs RO 60-0175, WAY 161503 and mirtazepine in a preclinical model of comorbidity of depression and cocaine addiction
7. Treatment with dopamine β-hydroxylase (DBH) inhibitors prevents morphine use and relapse-like behavior in rats
8. N-acetylcysteine in substance use disorder: a lesson from preclinical and clinical research
9. Maternal feeding patterns affect the offspring’s brain: focus on serotonin 5-HT2C and 5-HT2A receptors
10. The coming together of allosteric and phosphorylation mechanisms in the molecular integration of A2A heteroreceptor complexes in the dorsal and ventral striatal-pallidal GABA neurons
11. Acute cocaine treatment enhances the antagonistic allosteric adenosine A2A-dopamine D2 receptor–receptor interactions in rat dorsal striatum without increasing significantly extracellular dopamine levels
12. Adaptive mechanisms following antidepressant drugs: Focus on serotonin 5-HT2A receptors
13. Extinction training following cocaine or MDMA self-administration produces discrete changes in D2-like and mGlu5 receptor density in the rat brain
14. Oral administration of BDNF and/or GDNF normalizes serum BDNF level in the olfactory bulbectomized rats: A proof of concept study
15. Assessment of metabolic and hormonal profiles and striatal dopamine D2 receptor expression following continuous or scheduled high-fat or high-sucrose diet in rats
16. Correction to: The coming together of allosteric and phosphorylation mechanisms in the molecular integration of A2A heteroreceptor complexes in the dorsal and ventral striatal-pallidal GABA neurons
17. Correction to: Extinction training following cocaine or MDMA self-administration produces discrete changes in D2-like and mGlu5 receptor density in the rat brain
18. Neuroadaptive changes in metabotropic glutamate mGlu2/3R expression during different phases of cocaine addiction in rats
19. Manganese neurotoxicity and protective effects of resveratrol and quercetin in preclinical research
20. Working memory deficits and alterations of ERK and CREB phosphorylation following withdrawal from cocaine self-administration
21. Oxidative stress as an etiological factor and a potential treatment target of psychiatric disorders. Part 2. Depression, anxiety, schizophrenia and autism
22. Oxidative stress as an etiological factor and a potential treatment target of psychiatric disorders. Part 1. Chemical aspects and biological sources of oxidative stress in the brain
23. Binge eating in pre-clinical models
24. Cocaine exposure alters H2S tissue concentrations in peripheral mouse organs
25. Context-controlled nicotine-induced changes in the labeling of serotonin (5-HT)2A and 5-HT2C receptors in the rat brain
26. Integrated workflow for quantitative phosphoproteomic analysis of the selected brain structures in development of morphine dependence
27. The effect of active and passive intravenous cocaine administration on the extracellular signal-regulated kinase (ERK) activity in the rat brain
28. Inhibitory actions of mGlu4 receptor ligands on cocaine-, but not nicotine-, induced sensitizing and conditioning locomotor responses in rats
29. Cocaine-induced glutamate receptor trafficking is abrogated by extinction training in the rat hippocampus
30. Kynurenic acid inhibits proliferation and migration of human glioblastoma T98G cells
31. Preclinical studies on comorbidity between depression and psychostimulant addiction
32. The effects of the recurrent social isolation stress on fear extinction and dopamine D2receptors in the amygdala and the hippocampus
33. Effects of the histamine H3 receptor antagonist ABT-239 on cognition and nicotine-induced memory enhancement in mice
34. LC/MS/MS evaluation of cocaine and its metabolites in different brain areas, peripheral organs and plasma in cocaine self-administering rats
35. Neonatal serotonin (5-HT) depletion does not affect spatial learning and memory in rats
36. Effects of the histamine (H)3 receptor antagonist ABT-239 on acute and repeated nicotine locomotor responses in rats
37. Role of serotonin (5-HT)1B receptors in psychostimulant addiction
38. Neonatal serotonin (5-HT) depletion does not disrupt prepulse inhibition of the startle response in rats
39. Effects of serotonin (5-HT)6 receptor ligands on responding for cocaine reward and seeking in rats
40. Effects of ethylene glycol ethers on cell viability in the human neuroblastoma SH-SY5Y cell line
41. Nicotine dependence — human and animal studies, current pharmacotherapies and future perspectives
42. Overview on 5-HT receptors and their role in physiology and pathology of the central nervous system
43. KM-408, a novel phenoxyalkyl derivative as a potential anticonvulsant and analgesic compound for the treatment of neuropathic pain
- Abstract
Background: Epilepsy frequently coexists with neuropathic pain. Our approach is based on the search for active compounds with multitarget profiles beneficial in terms of potential side effects and on the implementation of screening for potential multidirectional central activity. Methods: Compounds were synthesized by means of chemical synthesis. After antiseizure and neurotoxicity screening in vivo, KM-408and its enantiomers were chosen for analgesic activity evaluations. Further safety studies included acute toxicity in mice, the effect on normal electrocardiogram and on blood pressure in rats, whole body plethysmography in rats, and in vitro and biochemical assays. Pharmacokinetics has been studied in rats after ivand poadministration. Metabolism has been studied in vivo in rat serum and urine. Radioligand binding studies were performed as part of the mechanism of action investigation. Results: Selected results for KM-408: K
i sigma = 7.2*10–8 ; Ki 5-HT1A = 8.0*10–7 ; ED50 MES (mice, ip) = 13.3 mg/kg; formalin test (I phase, mice, ip)—active at 30 mg/kg; SNL (rats, ip)—active at 6 mg/kg; STZ-induced pain (mice, ip)—active at 1 mg/kg (von Frey) and 10 mg/kg (hot plate); hot plate test (mice, ip)—active at 30 mg/kg; ED50 capsaicin test (mice, ip) = 18.99 mg/kg; tail immersion test (mice)—active at 0.5%; corneal anesthesia (guinea pigs)—active at 0.125%; infiltration anesthesia (guinea pigs)—active at 0.125%. Conclusions: Within the presented study a novel compound, R,S-2-((2-(2-chloro-6-methylphenoxy)ethyl)amino)butan-1-ol hydrochloride (KM-408) with dual antiseizure and analgesic activity has been developed for potential use in neuropathic pain treatment. Graphical abstract:
44. Evaluation of the 5-HT2Creceptor drugs RO 60-0175, WAY 161503 and mirtazepine in a preclinical model of comorbidity of depression and cocaine addiction
- Abstract
Background: Epidemiological data indicate a high rate of comorbidity of depression and cocaine use disorder (CUD). The role of serotonin 2C (5-HT
2C ) receptors in the mechanisms responsible for the coexistence of depression and CUD was not investigated. Methods: We combined bilateral olfactory bulbectomy (OBX), an animal model of depression, with intravenous cocaine self-administration and extinction/reinstatement in male rats to investigate two 5-HT2C receptor agonists (Ro 60-0175 (RO) and WAY 161503 (WAY)) and the 5-HT2C -receptor preferring antagonist mirtazapine (MIR; an antidepressant), with the goal of determining whether these drugs alter cocaine-induced reinforcement and seeking behaviors. Additionally, neurochemical analyses were performed following cocaine self-administration and its abstinence period in the brain structures in OBX rats and SHAM-operated controls. Results: Acute administration of RO reduced, while WAY non-significantly attenuated cocaine reinforcement in both rat phenotypes. Moreover, RO or WAY protected against cocaine-seeking behavior after acute or after repeated drug administration during extinction training in OBX and SHAM rats. By contrast, acutely administered MIR did not alter cocaine reinforcement in both rat phenotypes, while it’s acute (but not repeated) pretreatment reduced cocaine-seeking in OBX and SHAM rats. In neurochemical analyses, cocaine reinforcement increased 5-HT2C receptor levels in the ventral hippocampus; a preexisting depression-like phenotype enhanced this effect. The 10-daily cocaine abstinence reduced 5-HT2C receptor expression in the dorsolateral striatum, while the coexistence of depression and CUD enhanced local receptor expression. Conclusion: The results support a key role of 5-HT2C receptors for treating CUD and comorbid depression and CUD. They may be backs the further research of pharmacological strategies with drug targeting receptors. Graphical abstract:
45. Effect of active and passive cocaine intravenous administration on the extracellular signal-regulated kinase (ERK) activity in rat brain
46. Changes in the level of endocannabinoids and endocannabinoidlike molecules after acute and repeated administration of escitalopram or FAAH inhibitor in rat brain structures
47. Evaluation of the thermographic analysis in rat models of obesity
48. Horse chestnut saponins as a source of new materials for exploratory medicinal chemistry
49. Effects of adenosine A2A receptor ligands on cocaine self-administration and relapse in rats
50. Effects of acute and repeated administration of imipramine and N-acetylcysteine on the level of endocannabinoids in different rat brain structures
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