Kooperativer Bibliotheksverbund

Berlin Brandenburg

and
and

Your email was sent successfully. Check your inbox.

An error occurred while sending the email. Please try again.

Proceed reservation?

Export
Filter
Type of Medium
Language
Year
  • 1
    In: Journal of Peptide Science, April 2013, Vol.19(4), pp.233-239
    Description: AM94 is a fluorinated analog of biphalin with non‐hydrazine linker that has an affinity for μ‐opioid and δ‐opioid receptors tenfold higher than biphalin. Furthermore, evaluation in rats showed that AM94 has in hot plate test – after both intracerebroventricular and intravenous administrations – a greater and more durable efficacy than biphalin. Here, the antinociceptive profile of AM94 is further evaluated by following two different administration routes, intrathecal and subcutaneous, and two different animal species, rats and mice. The analgesic potency of AM94 is compared with that of both the parent peptide biphalin and morphine. Results show that in rats (tail flick test) and in mice (formalin test), AM94 has a higher and more durable analgesic effect than biphalin after intrathecal and subcutaneous administrations. Conformational properties of biphalin and AM94 were also investigated by variable‐temperature H NMR and energy minimization. Copyright © 2012 European Peptide Society and John Wiley & Sons, Ltd. The antinociceptive profile of AM94 has been evaluated by in vivo nociception tests, in rats (tail flick test) and in mice (formalin test). Result have been compared with those of biphalin and morphine. Variable‐temperature H NMR experiments and energy minimization were also carried out.
    Keywords: Am94 ; Analgesic ; Antinociception ; Biphalin ; Formalin Test ; Molecular Modeling ; Opioids ; Tail Flick Test ; Variable‐Temperature H Nmr
    ISSN: 1075-2617
    E-ISSN: 1099-1387
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 2
    In: Medicine & Science in Sports & Exercise, 2013, Vol.45(1), pp.29-35
    Description: PURPOSE: Anabolic androgenic steroids (AAS) are synthetic androgen-like compounds that are abused in sport communities despite their adverse effects. Nerve growth factor (NGF) influences neuronal differentiation and survival, and it also mediates higher brain functions such as learning and memory. Changes in NGF expression have been implicated in neurodegenerative disorders, including Alzheimer disease. Hence, we decided to study the effect of chronic AAS exposure on brain NGF profile, NGF-dependent cholinergic function, and related behavioral performance. METHODS: Male Wistar rats were injected for 4 wk with either nandrolone or stanozolol at daily doses (5.0 mg·kg, s.c.) that are considered equivalent to those abused by humans. NGF levels and NGF receptor (TrkA and p75NTR) expression were measured in the hippocampus and in the basal forebrain. Choline acetyltransferase expression was evaluated in basal forebrain. Spatial learning and memory were assessed using the Morris water maze. RESULTS: AAS treatment caused region-specific changes in the expression of NGF and its receptors. Both nandrolone and stanozolol increased NGF levels in the hippocampus and reduced NGF levels in the basal forebrain, reduced p75NTR expression in the hippocampus, and failed to affect TrkA expression in the basal forebrain. Finally, AAS treatment reduced the expression of choline acetyltransferase in the basal forebrain and impaired the behavioral performance in the Morris water maze. CONCLUSION: The evidence that supraphysiological doses of AAS cause neurotrophic unbalance and related behavioral disturbances raises the concern that AAS abuse in humans may affect mechanisms that lie at the core of neuronal plasticity.
    Keywords: Anabolic Agents -- Adverse Effects ; Androgens -- Adverse Effects ; Hippocampus -- Drug Effects ; Nandrolone -- Adverse Effects ; Nerve Growth Factor -- Metabolism ; Performance-Enhancing Substances -- Adverse Effects ; Stanozolol -- Adverse Effects;
    ISSN: 0195-9131
    E-ISSN: 15300315
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 3
    Language: English
    In: Journal of controlled release, 2012, Vol.164(1), pp.17-25
    Description: Today there is a very great deal of interest among members of the global natural products community in investigating new plant constituents. Recent studies demonstrate that liquorice extracts are useful in the treatment of dermatitis, eczema, and psoriasis, with an efficacy comparable to that of corticosteroids. In this work, niosomes made up of surfactants (Tween 85 and Span 20) and cholesterol at various concentrations were prepared to investigate the potential application of niosomes for the delivery of ammonium glycyrrhizinate (AG), useful for the treatment of various inflammatory based diseases. Vesicles were characterized evaluating dimensions, ζ potential, anisotropy, drug entrapment efficiency, stability, cytotoxicity evaluation and skin tolerability. Release profiles of ammonium glycyrrhizinate/niosomes were evaluated in vitro using cellulose membranes. The best formulation was used to evaluate the in vitro/in vivo efficacy of the ammonium glycyrrhizinate/niosomes in murine and human models of inflammation. The AG-loaded non-ionic surfactant vesicles showed no toxicity, good skin tolerability and were able to improve the drug anti-inflammatory activity in mice. Furthermore, an improvement of the anti-inflammatory activity of the niosome delivered drug was observed on chemically induced skin erythema in humans. ; p. 17-25.
    Keywords: Zeta Potential ; Inflammation ; Anti-Inflammatory Agents ; Psoriasis ; Adrenal Cortex Hormones ; Animal Models ; Cytotoxicity ; Eczema ; Humans ; Cholesterol ; Licorice ; Anti-Inflammatory Activity ; Erythema ; Mice ; Cellulose ; Surfactants ; Niosomes
    ISSN: 0168-3659
    E-ISSN: 18734995
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 4
    Language: English
    In: Journal of Controlled Release, 28 November 2012, Vol.164(1), pp.17-25
    Description: Today there is a very great deal of interest among members of the global natural products community in investigating new plant constituents. Recent studies demonstrate that liquorice extracts are useful in the treatment of dermatitis, eczema, and psoriasis, with an efficacy comparable to that of corticosteroids. In this work, niosomes made up of surfactants (Tween 85 and Span 20) and cholesterol at various concentrations were prepared to investigate the potential application of niosomes for the delivery of ammonium glycyrrhizinate (AG), useful for the treatment of various inflammatory based diseases. Vesicles were characterized evaluating dimensions, ζ potential, anisotropy, drug entrapment efficiency, stability, cytotoxicity evaluation and skin tolerability. Release profiles of ammonium glycyrrhizinate/niosomes were evaluated using cellulose membranes. The best formulation was used to evaluate the efficacy of the ammonium glycyrrhizinate/niosomes in murine and human models of inflammation. The AG-loaded non-ionic surfactant vesicles showed no toxicity, good skin tolerability and were able to improve the drug anti-inflammatory activity in mice. Furthermore, an improvement of the anti-inflammatory activity of the niosome delivered drug was observed on chemically induced skin erythema in humans.
    Keywords: Niosomes ; Ammonium Glycyrrhizinate ; Toxicity ; Skin Tolerability ; Inflammation ; Pharmacy, Therapeutics, & Pharmacology
    ISSN: 0168-3659
    E-ISSN: 1873-4995
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 5
    Language: English
    In: Life Sciences, 2006, Vol.79(8), pp.791-800
    Description: Phosphodiesterase 4 (PDE4) inhibitors are effective anti-inflammatory drugs, although some adverse effects are observed in animals and humans. These effects have forced researchers to find new PDE4 inhibitors with less adverse effects. We recently reported the synthesis of novel heterocyclic-fused pyridazinones that inhibit PDE4. As a first step in the study of the anti-inflammatory properties of these compounds, we studied the effects of local administration of these pyridazinone derivatives in a mouse model of acute inflammation. We found that 6-Benzyl-3-methyl-4-phenylpyrazolo[3,4- ]pyridazin-7(6 )-one (CC4), ethyl 6,7-dihydro-6-ethyl-3-methyl-7-oxo-4-phenyl-thieno[2,3- ]pyridazine-2-carboxylate (CC6) and ethyl 6,7-dihydro-6-ethyl-3-methyl-4-phenyl-1 -pyrrolo[2,3- ]pyridazine-2-carboxylate (CC12) reduced the paw edema induced by zymosan in mice as rolipram (the PDE4 inhibitor prototype with anti-inflammatory activity) and indomethacin did. It is well known that rolipram locally administered induces some adverse effects such as hyperalgesia. Thus, we studied this effect after local administration of CC4, CC6 and CC12 in the formalin test. We found that CC6 induced hyperalgesic effects, whereas CC4 and CC12 did not change the nociceptive threshold. Furthermore, we found that rolipram and CC6 reduced locomotor activity, whereas CC4 and CC12 did not change locomotor performance of the mice. Since CC4 and CC12 neither affected the nociceptive threshold nor changed the locomotor performance of mice, they appear more suitable than CC6 for future studies on animals and could be developed as an anti-inflammatory drug for humans.
    Keywords: Pde2 ; Pde3 ; Pde4 ; Pde5 ; Phosphodiesterase Inhibitor ; Inflammation ; Pain ; Locomotor Activity ; Pyridazinone Derivatives ; Sciences (General) ; Biology
    ISSN: 0024-3205
    E-ISSN: 1879-0631
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 6
    Language: English
    In: Journal of medicinal chemistry, 25 April 2013, Vol.56(8), pp.3419-23
    Description: Natural residues of the dimeric opioid peptide Biphalin were replaced by the corresponding homo-β(3) amino acids. The derivative 1 containing hβ(3) Phe in place of Phe showed good μ- and δ-receptor affinities (Ki(δ) = 0.72 nM; Ki(μ) = 1.1 nM) and antinociceptive activity in vivo together with an increased enzymatic stability in human plasma.
    Keywords: Enkephalins -- Pharmacology
    ISSN: 00222623
    E-ISSN: 1520-4804
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 7
    Language: English
    In: Colloids and Surfaces B: Biointerfaces, 01 October 2017, Vol.158, pp.379-386
    Description: Given the poor bioavailability of curcumin, its antinociceptive effects are produced after chronic intravenous administration of high doses, while poly ( -lactide-co-glycolide)-loaded vesicles (PLGA) can improve drug delivery. This paper investigates the antinociceptive effects of curcumin-loaded PLGA nanovesicles (PLGA-CUR) administered via intravenous (i.v.) or intrathecal (i.t.) routes at low and high doses. The following models of pain were used: formalin test, zymosan-induced hyperalgesia and sciatic nerve ligation inducing neuropathic allodynia and hyperalgesia. PLGA-CUR administered intravenously was able to reduce the response to nociceptive stimuli in the formalin test and hyperalgesia induced by zymosan. Curcumin, instead, was inactive. Low-dose i.t. administration of PLGA-CUR significantly reduced allodynia produced by sciatic nerve ligation, whereas low doses of curcumin did not change the response to nociceptive stimuli. Long-lasting antinociceptive effects were observed when high doses of PLGA-CUR were administered intrathecally. At high doses, i.t. administration of curcumin only exerted rapid and transient antinociceptive effects. Measurement of cytokine and BDNF in the spinal cord of neuropathic mice demonstrate that the antinociceptive effects of PLGA-CUR depend on the reduction in cytokine release and BDNF in the spinal cord. The results demonstrate the effectiveness of PLGA-CUR and suggest that PLGA-CUR nanoformulation might be a new potential drug in the treatment of pain.
    Keywords: Curcumin ; Nociception ; Analgesia ; Plga ; Spinal Cord ; Engineering ; Chemistry ; Anatomy & Physiology
    ISSN: 0927-7765
    E-ISSN: 1873-4367
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 8
    Language: English
    In: Current Medicinal Chemistry, 2018, Vol.25(20), p.2353-2384
    Description: Nociceptin /Orphanin FQ Peptide” receptor (NOPr) is a G-protein-coupled receptor with the nociceptin/orphanin FQ peptide (N/OFQ) as endogenous agonist. It is expressed in the nervous system as well as in some non-neural tissues. Its activation has pronociceptive effect at the supraspinal level, whereas at the spinal level it produces nociceptive effects at low doses and antinociceptive effects at higher doses. NOPr is also involved in mood and blood pressure regulation, immunoregulation, airway constriction, feeding, urination, bowel motility, learning and memory. Selective NOPr agonists have been tested clinically as anxiolytics and antitussives, and the antagonists as analgesics, antidepressants and in the treatment of alcohol addiction. Two NOPr radioligands have also been tested in humans as neuroimaging agents. Furthermore, the partial agonist peptide SER100 and N/OFQ have been used in clinical trials, respectively for congestive heart failure and overactive bladder. The evidence of interactions between NOP and μ-opioid receptor (MOPr) receptors has been exploited in the use of mixed NOPr/MOPr modulators as analgesics and in the treatment of drug addiction. These drugs are devoid of typical opioid liabilities. In this review, we outline the latest advances in the structure-activity relationships (SAR) of NOPr agonists and antagonists, with emphasis on affinity, activity, selectivity and pharmacokinetic features.
    Keywords: Nociceptin Nop Receptor Ligands Opioids Structure-Activity Relationship G-Protein Coupled Receptors Pain.
    ISSN: 0929-8673
    E-ISSN: 1875-533X
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 9
    Language: English
    In: Brain Research, 2007, Vol.1131, pp.173-180
    Description: Reelin is an extracellular matrix protein, secreted by GABAergic interneurons, that provides a signal for neural plasticity. A downregulation of reelin may be a factor to be considered in the study of major psychiatric disorders. The heterozygous reeler mouse model, thus, may be important to reveal those alterations in behavioral phenotype produced by reduced neural plasticity. Heterozygous (HZ) and wild-type (WT) mice were tested for anxiety-related behavior, motor impulsivity, and morphine-induced analgesia. Heterozygous mice showed significantly lower levels of anxiety- and risk-assessment-related behaviors in the elevated plus-maze during adolescence, in the absence of basal changes in general locomotion. Adult mice were assessed for profiles of impulsive behavior in operant chambers, and HZ mice exhibited elevated levels of motor impulsivity. When mice were assessed in nociception tests, a genotype difference in morphine-induced analgesia was found, and these results were confirmed by measurement of μ-receptors in the midbrain. The basal behavioral profile of the HZ genotype reveals important differences, consistent with decreased behavioral inhibition and emotionality, which can be revealed as early as in adolescence, together with slight increment of impulsive behavior and altered pain threshold and at the adult age. The HZ genotype can thus represent a useful animal model for the study of behavioral disorders consequent to reduced neural plasticity.
    Keywords: Reelin ; Antipsychotic ; Adolescence ; Impulsivity ; Nociception ; Neuropsychiatric Disorder ; Anatomy & Physiology
    ISSN: 0006-8993
    E-ISSN: 1872-6240
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
  • 10
    In: Lab Animal, 2014, Vol.43(9), p.321
    Description: Evaluating the behavior of mice and rats has substantially contributed to the progress of research in many scientific fields. Researchers commonly observe recorded video of animal behavior and manually record their observations for later analysis, but this approach has several limitations. The authors developed an automated system for tracking and analyzing the behavior of rodents that is based on radio frequency identification (RFID) in an ultra-high-frequency bandwidth. They provide an overview of the system's hardware and software components as well as describe their technique for surgically implanting passive RFID tags in mice. Finally, the authors present the findings of two validation studies to compare the accuracy of the RFID system versus commonly used approaches for evaluating the locomotor activity and object exploration of mice.
    Keywords: Rfid Equipment -- Research ; Rfid Equipment -- Usage ; Animal Behavior -- Analysis ; Neuropsychological Tests -- Research;
    ISSN: 0093-7355
    E-ISSN: 15484475
    Library Location Call Number Volume/Issue/Year Availability
    BibTip Others were also interested in ...
Close ⊗
This website uses cookies and the analysis tool Matomo. Further information can be found on the KOBV privacy pages