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Article
Neuromodulation Treatments for Mild Traumatic Brain Injury and Post-concussive Symptoms
Mild traumatic brain injury (mTBI) can result in prolonged post-concussive symptoms (e.g., depression, headaches, cognitive impairment) that are debilitating and difficult to treat. This article reviews recent...
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Article
Structure-based virtual screening, molecular docking and dynamics studies of natural product and classical inhibitors against human dihydrofolate reductase
Folate antagonists are classified as important and valuable therapeutic agents against infection, neoplastic, and inflammatory diseases. Dihydrofolate reductase (DHFR) is a biological target of two well-define...
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Article
Melatonin and Multiple Sclerosis: From Plausible Neuropharmacological Mechanisms of Action to Experimental and Clinical Evidence
Multiple sclerosis (MS) is a devastating chronic autoimmune demyelinating disease of the central nervous system (CNS), thought to affect more than 2.5 million people worldwide. Regulation of the sleep-wake cyc...
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Article
Open AccessOn resin click-chemistry-mediated synthesis of novel enkephalin analogues with potent anti-nociceptive activity
Here, we report the chemical synthesis of two DPDPE analogues 7a (NOVA1) and 7b (NOVA2). This entailed the solid-phase synthesis of two enkephalin precursor chains followed by a CuI-catalyzed azide-alkyne cycload...
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Article
Novel Fubinaca/Rimonabant hybrids as endocannabinoid system modulators
The discovery of novel modulators of the cannabinoid system is a current topic in medicinal chemistry. In this paper, we report nine novel carboxamides designed as hybrids of Fubinaca family compounds and Rimo...
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Article
In vitro and in silico approaches to unveil the mechanisms underlying the cytotoxic effect of juncunol on human hepatocarcinoma cells
Juncunol is a phenanthrene isolated from the halophyte species Juncus acutus, with selective cytotoxic activity towards human hepatocarcinoma (HepG2) cells. However, its mechanism of action is unknown.
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Article
Effects of central RVD-hemopressin(α) administration on anxiety, feeding behavior and hypothalamic neuromodulators in the rat
The endocannabinoid (eCB) system is strongly involved in the regulation of anxiety and feeding behavior. RVD-hemopressin(α) [RVD-hp(α)], a N-terminally extended form of hemopressin, is a negative allosteric mo...
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Article
Anorexigenic effects induced by RVD-hemopressin(α) administration
Hemopressin, VD-hemopressin(α) and RVD-hemopressin(α) are hemoglobin α chain derived-peptides which have been found in mouse brain, and where they modulate cannabinoid (CB) receptor function. The nonapeptide h...
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Article
Emotional disorders induced by Hemopressin and RVD-hemopressin(α) administration in rats
The endocannabinoid (eCB) system plays an important role in regulating emotional disorders, and is involved, directly or indirectly, in psychiatric diseases, such as anxiety and depression. Hemopressin, a hemo...
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Article
The Positive Regulation of eNOS Signaling by PPAR Agonists in Cardiovascular Diseases
Increasing evidence shows that activation of peroxisome proliferator-activated receptors (PPARs) plays an essential role in the regulation of vascular endothelial function through a range of mechanisms, includ...
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Article
CNS delivery of l-dopa by a new hybrid glutathione–methionine peptidomimetic prodrug
Parkinson’s disease (PD) is a neurodegenerative disorder associated primarily with loss of dopamine (DA) neurons in the nigrostriatal system. With the aim of increasing the bioavailability of l-dopa (LD) after or...
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Article
New potent biphalin analogues containing p-fluoro-l-phenylalanine at the 4,4′ positions and non-hydrazine linkers
We report the synthesis and the biological evaluation of two new analogues of the potent dimeric opioid peptide biphalin. The performed modification is based on the replacement of two key structural elements o...
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Chapter and Conference Paper
Development of μ Opioid Receptor Selective 4-Anilinidopiperidine Analogs