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PubMed Journals Articles About "Effects Of A CRF1 Receptor Antagonist On Human Startle In Normal Female Volunteers" RSS

19:55 EDT 25th March 2019 | BioPortfolio

Effects Of A CRF1 Receptor Antagonist On Human Startle In Normal Female Volunteers PubMed articles on BioPortfolio. Our PubMed references draw on over 21 million records from the medical literature. Here you can see the latest Effects Of A CRF1 Receptor Antagonist On Human Startle In Normal Female Volunteers articles that have been published worldwide.

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Showing "Effects CRF1 Receptor Antagonist Human Startle Normal Female" PubMed Articles 1–25 of 49,000+

Psychophysiological treatment outcomes: Corticotropin-releasing factor type 1 receptor antagonist increases inhibition of fear-potentiated startle in PTSD patients.

After exposure to a traumatic event, a subset of people develop post-traumatic stress disorder (PTSD). One of the key deficits in PTSD is regulation of fear, and impaired inhibition of fear-potentiated startle (FPS) has been identified as a potential physiological biomarker specific to PTSD. As part of a larger clinical trial, this study investigated the effects of a CRF receptor 1 antagonist, GSK561679, on inhibition of fear-potentiated startle during a conditional discrimination fear-conditioning paradigm...


The Neuroprotective Effect of Histamine H4 Receptor Antagonist on Dopaminergic Neurons in Parkinson's Disease.

This research was aimed to explore the neuroprotective effects of histamine H3 and H4 receptor antagonists on dopaminergic (DA) neurons in Parkinson's disease (PD) model rats induced by 6-hydroxydopamine (6-OHDA) and their mechanism. The changes of the level of monoamine neurotransmitters, the number and morphology of TH-positive cells, and inflammatory factors in the striatum were used to evaluate the protective effects of H3 and H4 receptor antagonists on PD rats. The effects of histamine H4 receptor anta...

Fibronectin modulates the endocannabinoid system through the cAMP/PKA pathway during human sperm capacitation.

Fibronectin (Fn) enhances human sperm capacitation via the cAMP/PKA pathway, and the endocannabinoid system participates in this process. Moreover, Fn has been linked to endocannabinoid system components in different cellular models, even though no evidence of such interactions in human sperm is available. Normal semen samples were evaluated over a four-year period. Our findings suggest that (i) the capacitating effects of Fn were reversed by pre-incubating the sperm with a cannabinoid receptor 1 (CB1) or t...


Dopamine D and D Receptor Antagonism During Development Alters Later Behavior in Zebrafish.

This study sought to examine the long-term behavioral impacts of dopamine D and D receptor antagonism during development in zebrafish (Danio rerio). Zebrafish embryos of both the AB* and 5D strains were exposed via immersion to either the D receptor antagonist SCH-23390 or the D receptor antagonist haloperidol, at either 0.5 or 1.5-µM, from 5 h post-fertilization to 5 days post-fertilization. Aquarium water served as a control. Fish were then either tested as larvae on day 6 post-fertilization on a light...

Histamine H receptor mediates chemotaxis of human lung mast cells.

The diverse effects of histamine are mediated by discrete histamine receptors. The principal repository of histamine in the body is the mast cell. However, the effects of histamine on mast cells, especially those of human origin, have not been fully elucidated. In this study, the expression of histamine receptors in human lung mast cells was evaluated. Moreover, the effects of histamine receptor engagement on both mediator release and chemotaxis were investigated. Mast cells were isolated and purified from ...

Blockade of Serotonin 2C Receptors with SB-242084 Moderates Reduced Locomotor Activity and Rearing by Cannabinoid 1 Receptor Antagonist AM-251.

The endocannabinoid and serotonin (5-HT) systems have key roles in the regulation of several physiological functions such as motor activity and food intake but also in the development of psychiatric disorders. Here we tested the hypothesis, whether blockade of serotonin 2C (5-HT2C) receptors prevents the reduced locomotor activity and other behavioral effects caused by a cannabinoid 1 (CB1) receptor antagonist. As a pretreatment, we administered SB-242084 (1 mg/kg, ip.), a 5-HT2C receptor antagonist or vehi...

Spironolactone depletes the XPB protein and inhibits DNA damage responses in UVB-irradiated human skin.

UVB wavelengths of light induce the formation of photoproducts in genomic DNA that are potentially mutagenic and detrimental to epidermal cell function. Interestingly, the mineralocorticoid and androgen receptor antagonist spironolactone (SP) was recently identified as an inhibitor of UV photoproduct removal in human cancer cells in vitro via its ability to promote the rapid proteolytic degradation of the DNA repair protein XPB (xeroderma pigmentosum group B). Using normal human keratinocytes in vitro and s...

Effect of a novel nonsteroidal selective mineralocorticoid receptor antagonist, esaxerenone (CS-3150), on blood pressure and renal injury in high salt-treated type 2 diabetic mice.

Although beneficial antihypertensive and antialbuminuric effects of steroidal mineralocorticoid receptor (MR) antagonists have been shown, the use of these drugs has been clinically limited in diabetic kidney disease (DKD) because of the high incidence of side effects. Here, we aimed to examine the effect of a novel nonsteroidal selective mineralocorticoid receptor antagonist, esaxerenone, on blood pressure and renal injury in high salt-treated type 2 diabetic KK-A mice, a model of human hypertensive DKD. K...

The mineralocorticoid receptor antagonist spironolactone reduces alcohol self-administration in female and male rats.

Cortisol/corticosterone and the hypothalamic-pituitary-adrenal (HPA) axis serve an important role in modulating alcohol drinking behaviors. To date most alcohol research has focused on the functional involvement of corticosterone and the glucocorticoid receptor (GR), the primary receptor for corticosterone. Recent studies have indicated that the related mineralocorticoid receptor (MR), which binds both corticosterone and aldosterone, may also play a role in alcohol drinking. Therefore, the purpose of the pr...

Potential roles of 5-HT receptor (5-HTR) antagonists in modulating the effects of nicotine.

5-HTR antagonists such as ondansetron, granisetron and tropisetron have been clinically used to treat nausea and vomiting in chemotherapy patients. However, current study and research revealed novel potentials of these ligands in other diseases like inflammation, Alzheimer's, and drug abuse. Towards utilising these drugs as anti-smoking agents to treat nicotine dependence problem, there are conflicting reports regarding the potential of these ligands in modulating the effects of nicotine in both human and a...

Multiple-Dose Pharmacokinetics, Pharmacodynamics, and Safety of the Urotensin-II Receptor Antagonist Palosuran in Healthy Male Subjects.

To investigate the multiple-dose pharmacokinetics (PK), pharmacodynamics (PD), and tolerability of palosuran, a selective, potent antagonist of the human UT receptor.

Leptin Receptor as a Potential Target to Inhibit Human Testicular Seminoma Growth.

Although in the last decades, the adipokine leptin and its own receptor have been considered as significant cancer biomarkers, their potential involvement in human testicular seminoma growth and progression remains unexplored. Here, we demonstrated that the expression of leptin and its receptor was significantly higher in human testicular seminoma compared to normal adult testis. Human seminoma cell line TCam-2 also expressed leptin along with the long and the short isoforms of leptin receptor and in respon...

Effect of the Fexofenadine on the expression of HRH-1 and HRH-4 receptor in Peripheral Blood Mononuclear Cell isolated from children with diagnosed allergy - in vitro study Short communication.

Fexofenadine (FXF) is the active metabolite of terfenadine with selective peripheral H1 receptor antagonist activity. FXF is a third-generation antihistamine, non-sedating, rapid and very long acting used in symptoms associated with allergic diseases such as allergic rhinitis, asthma and dermatitis. The pleiotropic effects of histamine are mediated by four types of receptors that belong to the G-protein-coupled receptor family: histamine H1 receptor (HRH-1), histamine H2 receptor, histamine H3 receptor, an...

The basic helix-loop-helix transcription factor Crf1 is required for development and pathogenicity of the rice blast fungus by regulating carbohydrate and lipid metabolism.

Pyricularia oryzae is a plant pathogen causing rice blast, a serious disease spreading in cultivated rice globally. Transcription factors play important regulatory roles in fungal development and pathogenicity. Here, we characterized the biological functions of Crf1, a basic helix-loop-helix (bHLH) transcription factor, in the development and pathogenicity of P. oryzae with functional genetics, molecular, and biochemical approaches. We found that CRF1 is necessary for virulence and plays an indispensable ro...

5-HT receptor signaling in serotonin transporter knockout rats: a female sex specific animal model of visceral hypersensitivity.

The irritable bowel syndrome (IBS) is a functional gastrointestinal motor and visceral sensation disorder that is more common in women than men. Female serotonin transporter (SERT) gene knockout (KO) rats exhibit hypersensitivity to colorectal balloon distention (CRD) that mimics colonic hypersensitivity occurring in female IBS patients. Alosetron, (5-HT receptor antagonist), is used to treat diarrhea-predominant IBS in female patients. Other 5-HT receptor antagonists are ineffective in treating IBS symptom...

Enrichment-induced differences in methamphetamine drug discrimination in male rats.

Rats raised in an enriched environment show a decrease in sensitivity to the subjective effects of the psychostimulant d-amphetamine. The purpose of the present study was to determine if environmental enrichment during development alters the subjective effects of the more commonly abused drug methamphetamine. Male Sprague-Dawley rats were raised in either an enriched (EC) or an isolated condition (IC). EC and IC rats were trained on a two-lever operant procedure to discriminate 1.0 mg/kg (i.p.) methamphet...

The Effects of Neurokinin-1 Receptor Antagonist in an Experimental Autoimmune Cystitis Model Resembling Bladder Pain Syndrome/Interstitial Cystitis.

To identify the effects of the neurokinin-1 receptor (NK1R) antagonist aprepitant in treating pelvic pain, micturition symptoms, and bladder inflammation in mice with experimental autoimmune cystitis (EAC) similar to bladder pain syndrome/interstitial cystitis (BPS/IC). Female C57BL/6 mice were divided into the following three groups: normal control, EAC, and EAC plus aprepitant. EAC was induced in mice by duplicate immunization with bladder homogenate. In the EAC model group, EAC mice were given PBS by gav...

Characterization of the antagonist actions of 5-BDBD at the rat P2X4 receptor.

P2X receptors (P2XRs) are a family of ATP-gated ionic channels that are expressed in numerous excitable and non-excitable cells. Despite the great advance on the structure and function of these receptors in the last decades, there is still lack of specific and potent antagonists for P2XRs subtypes, especially for the P2 × 4R. Here, we studied in detail the effect of the P2 × 4R antagonist 5-(3-bromophenyl)-1,3-dihydro-2H-benzofuro[3,2-e]-1,4-diazepin-2-one (5-BDBD) on ATP-induced currents mediated...

Chemical manipulations on the 1,4-dioxane ring of 5-HT receptor agonists lead to antagonists endowed with antitumor activity in prostate cancer cells.

A series of derivatives obtained by moving the aromatic moiety on the 1,4-dioxane ring of compounds 1-3 from position 6 to position 2 or 3 was prepared and evaluated for the affinity for 5-HT receptor (5-HTR) and α-adrenoceptor (α-AR) subtypes. Moreover, the flexible 2-ethanolamine linker of the most interesting compounds was replaced by the more conformationally constrained piperazine ring. In vitro functional studies performed on derivatives showing the highest affinities for 5-HTR highlighted that the...

Startle, pre-pulse sensitization, and habituation in zebrafish.

The startle response, pre-pulse presentation of startle, and habituation in adult zebrafish (danio rerio) have not been formerly characterized using the same motion detection equipment within an integrated procedure.

Flumazenil but not bicuculline counteract the impairing effects of anesthetic ketamine on recognition memory in rats. Evidence for a functional interaction between the GABA-benzodiazepine receptor and ketamine?

Experimental evidence indicates that anesthetic doses of the non-competitive NMDA receptor antagonist ketamine impair memory abilities in rodents. The mechanism by which anesthetic ketamine produces its adverse behavioural effects is not yet clarified. In this context, it has been proposed that the effects of anesthetic ketamine on memory might be attributed to its agonistic properties on the GABA type A receptor. The present study was designed to address this issue. Thus, we investigated the ability of the...

Orexin-A signaling in the paraventricular nucleus modulates spontaneous firing of glucose-sensitive neurons and promotes food intake via the NPY pathway in rats.

Understanding the mechanisms regulating feeding is crucial to unraveling the pathogenesis of obesity. The study primary explored the effects of orexin-A and neuropeptide Y (NPY) signaling in the hypothalamic paraventricular nucleus (PVN) on feeding and glucose-sensitive (GS) neuron activity in rats. Microinjection of orexin-A into the PVN promoted feeding and modulated the spontaneous firing of GS neurons. Those effects were eliminated by pre-injection of the orexin-A receptor-1 (OX1R) antagonist SB-334867 ...

Effects of long-term oral nitrate administration on adiposity in normal adult female rats.

Nitric oxide (NO) deficiency is associated with obesity. Nitrate could act as a substrate for production of NO and is a novel therapeutic agent in obesity. This study aims at determining effects of long-term nitrate administration on obesity indices in normal adult female rats.

Dependency of prepulse inhibition deficits on baseline startle reactivity in a mouse model of the human 22q11.2 microdeletion syndrome.

Hemizygous microdeletion at the chromosomal locus 22q11.2 is a copy number variation with strong genetic linkage to schizophrenia and related disorders. This association, along with its phenotypic overlap with the 22q11.2 microdeletion syndrome, has motivated the establishment of Df[h22q11]/+ mice, in which the human 22q11.2 orthologous region is deleted. Previous investigations using this model revealed the presence of reduced prepulse inhibition (PPI) of the acoustic startle reflex, a form of sensorimotor...

Possible involvement of the μ opioid receptor in the antinociception induced by sinomenine on formalin-induced nociceptive behavior in mice.

Sinomenine, an alkaloid originally isolated from the roots and the rhizome of Sinomenium acutum is used as a traditional Chinese herbal medicines for rheumatoid arthritis and neuralgia. The aims of this study were to investigate the effects of oral administration of shinomenine on formalin-induced nociceptive behavior in mice and the opioid receptor subtypes involved in the antinociceptive effects of sinomenine. Our findings showed that a single dose of oral-administrated sinomenine inhibited the formalin i...


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