Evaluation of the Quality of Sleep, Endothelial Function, Cardiovascular Risk, Thyroid Function, a Function of Masticatory Muscles and Psycho-emotional State of Patients With Sleep Bruxism

Sleep apnea is a common and serious health problem in the Polish population. According to epidemiological data problem concerns about 7% of the adult population. The most common sleep disorder is obstructive sleep apnea (OSA). The consequence of episodes of airway obstruction and sleep fragmentation is an inefficient sleep, pathological daytime sleepiness, falling asleep involuntarily, awakening with feelings of shortness of breath or throttling. The direct consequences of sleep apnea are hypoxia, increased heart rate and increased blood pressure. Frequent complications of OSA are hypertension, stroke, cardiac arrhythmia, coronary artery disease and pulmonary hypertension. An additional problem in patients with sleep apnea is an increased incidence of bruxism. Bruxism is a common problem; reports of prevalence range from 8-31% in the general population. The most common symptoms of bruxism include: hypersensitive teeth, tooth wear, damage to dental restorations (e.g. crowns and fillings), damage to periodontal and oral mucosa, masticatory muscle pain and headaches. The etiology of bruxism is multifactorial and not fully understood. It can be caused by biologic, psychologic and exogenous factors. Arousals during the apnea episodes are considered to be a major cause of sleep bruxism in OSA patients. The relationship between OSA and sleep bruxism is still not clearly defined. Further research is needed to help explain the relationship between these two phenomena, which will enable further therapy in patients with coexisting OSA and sleep bruxism (SB).

Start Date20 Apr 2017

Sponsor / Collaborator

Akademia Medyczna

NCT03065998

/ Unknown statusEarly Phase 1IIT

Double Blind Placebo Control Opipramol-Baclofen Treatment for Addiction: Medical and Cognitive Effects

The aim of this study is examining the combination of two FDA approved drugs, Opipramol and baclofen, which may increase rehabilitation from psychoactive substances. Previous studies have indicated a connection of sigma-1 receptor to cocaine abuse and raised the possibility that these receptors as mediators of drug craving . However previous studies showed partial efficacy with no significant relapse in relapse rates. The same is true for the use of GABAb-1 receptor antagonist. Opipramol is a selective agonist for sigma-1 receptor. It is clinically used as an antidepressant and anxiolytic agent. Moreover, previous open and controlled trials indicated that the GABAb-1 antagonist baclofen partial efficacy in suppressing withdrawal symptoms in alcohol addicts and cocaine. Our studies in an animal model for addiction have shown a significant effect of the combine treatment of the indicated medications both in decreasing relapse and increase of -number of respondents.

Start Date01 Mar 2017

Sponsor / Collaborator

Israel Ministry of Health

100 Clinical Results associated with σ1 receptor x 5-HT2 receptor

100 Translational Medicine associated with σ1 receptor x 5-HT2 receptor

0 Patents (Medical) associated with σ1 receptor x 5-HT2 receptor

Literatures (Medical) associated with σ1 receptor x 5-HT2 receptor

01 Sep 2016·Pharmacology Biochemistry and BehaviorQ4 · PSYCHOLOGY

The effect of the sigma-1 receptor selective compound LS-1-137 on the DOI-induced head twitch response in mice

Q4 · PSYCHOLOGY

Article

Author: Luedtke, Robert R ; Mach, Robert H ; Malik, Maninder ; Rangel-Barajas, Claudia

Several receptor mediated pathways have been shown to modulate the murine head twitch response (HTR). However, the role of sigma receptors in the murine (±)-2,5-dimethoxy-4-iodoamphetamine (DOI)-induced HTR has not been previously investigated. We examined the ability of LS-1-137, a novel sigma-1 vs. sigma-2 receptor selective phenylacetamide, to modulate the DOI-induced HTR in DBA/2J mice. We also assessed the in vivo efficacy of reference sigma-1 receptor antagonists and agonists PRE-084 and PPCC. The effect of the sigma-2 receptor selective antagonist RHM-1-86 was also examined. Rotarod analysis was performed to monitor motor coordination after LS-1-137 administration. Radioligand binding techniques were used to determine the affinity of LS-1-137 at 5-HT2A and 5-HT2C receptors. LS-1-137 and the sigma-1 receptor antagonists haloperidol and BD 1047 were able to attenuate a DOI-induced HTR, indicating that LS-1-137 was acting in vivo as a sigma-1 receptor antagonist. LS-1-137 did not compromise rotarod performance within a dose range capable of attenuating the effects of DOI. Radioligand binding studies indicate that LS-1-137 exhibits low affinity binding at both 5-HT2A and 5-HT2C receptors. Based upon the results from these and our previous studies, LS-1-137 is a neuroprotective agent that attenuates the murine DOI-induced HTR independent of activity at 5-HT2 receptor subtypes, D2-like dopamine receptors, sigma-2 receptors and NMDA receptors. LS-1-137 appears to act as a sigma-1 receptor antagonist to inhibit the DOI-induced HTR. Therefore, the DOI-induced HTR can be used to assess the in vivo efficacy of sigma-1 receptor selective compounds.

01 Dec 2013·NeuropharmacologyQ2 · MEDICINE

Synergistic effect of 5-HT1A and σ1 receptor activation on prefrontal dopaminergic transmission under circulating steroid deficiency

Q2 · MEDICINE

Article

Author: Ago, Yukio ; Matsuda, Toshio ; Hasebe, Shigeru ; Hiramatsu, Naoki ; Mori, Kazuya ; Nishimura, Akira ; Takuma, Kazuhiro

Serotonin (5-HT)1A and σ1 receptors have been implicated in psychiatric disorders. We previously found that combined 5-HT reuptake inhibition and σ1 receptor activation has a synergistic effect on prefrontal dopaminergic transmission in adrenalectomized/castrated mice lacking circulating steroid hormones. In the present study, we examined the mechanisms underlying this neurochemical synergism. Systemic administration of fluvoxamine, a selective 5-HT reuptake inhibitor with agonistic activity towards the σ1 receptor, increased prefrontal dopamine (DA) levels, and adrenalectomy/castration potentiated this fluvoxamine-induced increase in DA. This enhancement of DA release was blocked by WAY100635 (a 5-HT1A receptor antagonist), but not by ritanserin (a 5-HT2 receptor antagonist), azasetron (a 5-HT3 receptor antagonist) or SB269970 (a 5-HT7 receptor antagonist). Individually, osemozotan (a 5-HT1A receptor agonist) and (+)-SKF-10,047 (a σ1 receptor agonist) did not alter prefrontal monoamine levels in adrenalectomized/castrated and sham-operated mice differentially. In contrast, co-administration of these drugs increased prefrontal DA levels to a greater extent in adrenalectomized/castrated mice than in sham-operated animals. Furthermore, co-administration of osemozotan and (+)-SKF-10,047 increased expression of the neuronal activity marker c-Fos in the ventral tegmental area of adrenalectomized/castrated mice, but not in sham-operated animals. These findings suggest that combined activation of 5-HT1A and σ1 receptors has a synergistic effect on prefrontal dopaminergic transmission under circulating steroid deficiency, and that this interaction may play an important role in the regulation of the prefrontal DA system.

01 Apr 1999·European Journal of PharmacologyQ3 · MEDICINE

Two novel σ receptor ligands, BD1047 and LR172, attenuate cocaine-induced toxicity and locomotor activity

Q3 · MEDICINE

Article

Author: Wayne D. Bowen ; Rae R. Matsumoto ; Kari A. McCracken ; Brian R. de Costa

The ability of cocaine to interact with sigma receptors indicates that these sites may mediate the negative properties associated with cocaine use, such as toxicity and addiction. Previous studies have shown that the novel sigma receptor ligand, BD1008 (N-[2-(3,4-dicholophenyl)ethyl]-N-methyl-2-(1-pyrrolidinyl)ethylam ine), effectively protects against cocaine-induced convulsions and locomotor activity in mice. Therefore, BD1047 ([2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(diamino)ethylamine) and LR172 (N-[2-(3,4-dichlorophenyl)ethyl]-N-methyl-2-(1-homopiperidinyl)eth ylamine), two analogs of BD1008, were tested to determine if they also have anti-cocaine properties. Receptor binding assays showed that BD1047 and LR172 both have high affinities for a receptors, but low to negligible affinities for dopamine, opioid, phencyclidine, and 5-HT2 sites. In behavioral studies, pretreatment of mice with BD1047 or LR172 reduced the convulsions, lethality, and locomotor activity produced by cocaine. The data indicates a possible role for sigma receptor ligands in the treatment of cocaine overdose and addiction.

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