Search results for "RECEPTORS"
showing 10 items of 3254 documents
Effects of indomethacin on muscarinic inhibition of endogenous noradrenaline release from rat isolated trachea
1993
The release of endogenous noradrenaline from rat isolated tracheae was evoked by electrical field stimulation (3 Hz, 540 pulses) in the presence of yohimbine, desipramine and tyrosine. The muscarine receptor agonist oxotremorine concentration-dependently inhibited the evoked release of noradrenaline by 95% at 1 μmol/l, EC50 values in two series of experiments 41 and 57 nmol/l, respectively. The effect of oxotremorine was antagonized by the non-selective muscarine receptor antagonist scopolamine (10–1000 nmol/l) in a manner suggesting a simple competitive interaction (slope of Schild plot −0.94; pA2 value 8.88). However, the M2 selective muscarine receptor antagonist methoctramine (0.1–10 μm…
From structural biochemistry to expression profiling: Neuroprotective activities of estrogen
2005
Abstract Estrogens are neuromodulatory and neuroprotective hormones. Chemically, estrogens are steroid compounds and unfold most of their activities through the activation of nuclear receptors that bind to specific target genes and control their transcription. Two subtypes of estrogen receptors are known (estrogen receptor α and estrogen receptor β) and they are expressed throughout the body including the CNS and in particular the brain. We employed large scale DNA-chip-analysis to display the gene expression pattern differentially regulated by both estrogen receptor subtypes in human neuronal cells. We identified different gene families regulated by estrogen receptors that complement the k…
Estrogen receptor agonists and immune system in ovariectomized mice.
2006
Several data implicate the immune system in bone lost after estrogen deficiency, however, some of the effects on the immune system of estrogen deficiency or of estrogen receptor (ER) modulation are not well established. In this study, the effect of ER agonists on the immune system in ovariectomized mice is analyzed. Mice were ovariectomized and were administered 17β-estradiol (E2), raloxifene (RAL) or genistein (GEN). The effect of a 4-week treatment on bone turnover and on several parameters that reflect the status of the immune system was studied. Results show that ovariectomy provoked both uterine atrophy and thymic hypertrophy. Although RAL corrected thymic hypertrophy, only E2 correct…
Constitutive androstane receptor activation stimulates faecal bile acid excretion and reverse cholesterol transport in mice.
2010
The constitutive androstane receptor (CAR) is a nuclear receptor expressed in the liver and involved in xenobiotic metabolism. The aim of this study was to assess whether pharmacological CAR activation could affect neutral sterol and bile acid elimination under conditions of cholesterol overload.Wild type, Car-/-, ApoE-/-, and low-density lipoprotein receptor (Ldlr)-/- mice fed a western-type diet were treated with the CAR agonist TCPOBOP.CAR activation was associated with a decrease in faecal cholesterol output related to the repression of the Abcg5/g8 cholesterol transporters. In contrast, TCPOBOP treatment induced a marked increase (up to three fold, p0.01) in the elimination of faecal b…
Selective RAR agonists for acne vulgaris: A narrative review.
2019
Background Acne vulgaris is a chronic disfiguring inflammatory disease of adolescents and adults affecting up to 90% of the population around the world. The sequence of etiopathogenesis in acne is not completely understood but involves abnormalities in sebum production, follicular plugging, proliferation of propionibacterium acnes, and chronic inflammation. Aims This review aims to summarize the features of the topical selective RAR agonists in treating acne vulgaris with a special emphasis on the 4th generation topical retinoid trifarotene. Methods Studies were identified by searching electronic databases (MEDLINE and PubMed) till August 2019 and reference lists of respective articles. Onl…
Activation of mGlu3 Receptors Stimulates the Production of GDNF in Striatal Neurons
2009
Metabotropic glutamate (mGlu) receptors have been considered potential targets for the therapy of experimental parkinsonism. One hypothetical advantage associated with the use of mGlu receptor ligands is the lack of the adverse effects typically induced by ionotropic glutamate receptor antagonists, such as sedation, ataxia, and severe learning impairment. Low doses of the mGlu2/3 metabotropic glutamate receptor agonist, LY379268 (0.25-3 mg/kg, i.p.) increased glial cell line-derived neurotrophic factor (GDNF) mRNA and protein levels in the mouse brain, as assessed by in situ hybridization, real-time PCR, immunoblotting, and immunohistochemistry. This increase was prominent in the striatum, …
Effect of Soluble Interleukin-6 Receptor on Interleukin-6 Synthesis in Human Skin Fibroblasts
1996
Abstract In this study the ability of soluble interleukin-6 receptor (sIL-6R) to stimulate interleukin-6 (IL-6) synthesis in human fibroblasts is described. It was found that sIL-6R, in combination with endogenous or exogenous IL-6, markedly upregulated IL-6 synthesis. These data suggest that increased IL-6 production after stimulation by either interleukin-1 or tumor necrosis factor-α would result in complex formation with sIL-6R, rapid uptake, and further synthesis of this cytokine. Furthermore, it would explain the decrease in sIL-6R plasma levels observed in patients suffering from sepsis.
Cholesterol as stabilizer of the oxytocin receptor
2002
AbstractThe function of the oxytocin receptor system is strongly dependent on steroids as demonstrated by several physiological studies. One key element of this dependence on steroids may be the interaction of cholesterol and the oxytocin receptor. In this study, we show that cholesterol stabilizes the solubilized human oxytocin receptor against thermal inactivation and proteolytic degradation. In the absence of additional cholesterol, the soluble receptor inactivates within minutes. Maximal stabilization of the oxytocin receptor requires a continuous supply with cholesterol from a cholesterol-rich environment. A structure–activity analysis of various cholesterol analogues and their effect …
Individualized analysis of skin thermosensory thresholds and sensitivity in heat-sensitive people with multiple sclerosis
2020
We investigated whether and how multiple sclerosis (MS) alters thresholds for perceiving increases and decreases in local skin temperature, as well as the sensitivity to progressively greater temperature stimuli, amongst heat-sensitive people with MS. Eleven MS patients (5 M/6 F; 51.1 ± 8.6 y, EDSS 5.7 ± 1.9) and 11 healthy controls (CTR; 7 M/4 F; 50.3 ± 9.0 y) performed warm and cold threshold tests on a hairy skin site, on both sides of the body. They also underwent a thermosensitivity test where they rated (visual analogue scale) perceived magnitude of 4 local skin stimuli (i.e. 22, 26, 34, 38°C). Individual thresholds and slopes of linear regression for thermosensitivity were z-transfor…
Molecular and Translational Classifications of DAMPs in Immunogenic Cell Death
2015
The immunogenicity of malignant cells has recently been acknowledged as a critical determinant of efficacy in cancer therapy. Thus, besides developing direct immunostimulatory regimens, including dendritic cell-based vaccines, checkpoint-blocking therapies, and adoptive T-cell transfer, researchers have started to focus on the overall immunobiology of neoplastic cells. It is now clear that cancer cells can succumb to some anticancer therapies by undergoing a peculiar form of cell death that is characterized by an increased immunogenic potential, owing to the emission of the so-called "damage-associated molecular patterns" (DAMPs). The emission of DAMPs and other immunostimulatory factors by…