L-798,106

Depression and anxiety disorders in chronic hemodialysis patients and their quality of life: A cross-sectional study about 106 cases in the northeast of morocco.[Pubmed:28352018]

Saudi J Kidney Dis Transpl. 2017 Mar-Apr;28(2):341-348.

Hemodialysis (HD) has a severe impact on the life of HD patients. The aim of this work was to assess the prevalence of depression and anxiety disorders, suicidal ideation, and the quality of life among HD patients. Associated factors were also studied. A cross-sectional study was carried out among 103 HD patients treated at the HD Center of Al Farabi Hospital of Oujda during a period of six months in 2015. The Mini-International Neuropsychiatric Interview and European Quality of Life-5 Dimensions (EQ-5D) were used for the assessment. Major depressive episode (MDE) was found in 34% of our patients, whereas anxiety disorder was observed in 25.2%. Suicidal ideation was found in 16.5% and 1.9% of our patients planned their suicide. The EQ-5D index was 0.41 +/- 0.36 and the EQ-Visual Analog Scale score was 45.73 +/- 14. Multivariate analysis showed that MDEs were associated with three factors: marital status, pain, and anxiety disorder. There was also an association between anxiety disorder and age and EQ-Visual Analog Scale score. Suicidal ideation was associated with marital status and anxiety disorders. Together, these results underline the importance of the collaboration between nephrologists and psychiatrists for a better care of HD patients.

Technical Note: Monte Carlo study of (106) Ru/(106) Rh ophthalmic plaques including the (106) Rh gamma spectrum.[Pubmed:28370303]

Med Phys. 2017 Jun;44(6):2581-2585.

PURPOSE: To assess the influence of the (106) Rh gamma spectrum on the Monte Carlo simulation of (106) Ru/(106) Rh ophthalmic plaques, which has been neglected without a quantitative estimation in all previous publications. METHODS: Simulations were run with the penelope 2014 Monte Carlo code for radiation transport. Depth-dose distributions in water were simulated for the plaque models CCA, CCC, CCX and CIA. In addition to the (106) Rh beta spectrum, all gamma components from the (106) Rh gamma spectrum were included in the simulations. Depth-dose curves were compared with those obtained without considering the (106) Rh gamma spectrum. Moreover, half-value (HVL) and tenth-value layers (TVL) were estimated for the (106) Rh gamma spectrum in water, PMMA, stainless steel and lead. Some practical radiation protection applications were discussed. Parallel computing was implemented to reduce computing time. RESULTS: The contribution of the (106) Rh gamma spectrum on the depth-dose curves is negligible at depths of clinical interest. The HVL and TVL of the (106) Rh gamma spectrum were found to be similar to those of (137) Cs. The air-kerma rate at 1 m for a CCA plaque in typical clinical conditions was about 0.4muGym2h-1, resulting in equivalent doses at that point elow 0.05 mSv during a treatment. The air-kerma rate would be underestimated by a factor of 5 if the (106) Rh gamma spectrum were not considered. Also, a freely available software tool was developed to ease parallelization of penelope 2014 simulations that use penmain as steering main program. CONCLUSIONS: The influence of the (106) Rh gamma spectrum is not relevant for clinical purposes, thus validating the common assumption from the literature. However, for simulations at large distances from the plaques, such as for radiation shielding assessment and estimation of dose to personnel, the gamma spectrum from (106) Rh must be taken into account to obtain accurate results.

Transbronchial cryobiopsy in interstitial lung disease: experience in 106 cases - how to do it.[Pubmed:28344982]

ERJ Open Res. 2017 Mar 22;3(1). pii: 00148-2016.

Transbronchial biopsy using forceps (TBB) is the first diagnostic technique performed on patients with interstitial lung disease (ILD). However, the small size of the samples and the presence of artefacts in the tissue obtained make the yield variable. Our objectives were 1) to attempt to reproduce transbronchial cryobiopsy under the same conditions with which we performed conventional TBB, that is, in the bronchoscopy unit without intubating the patient and without fluoroscopy or general anaesthesia; 2) to describe the method used for its execution; and 3) to analyse the diagnostic yield and its complications. We carried out a prospective study that included 106 patients with clinical and radiological features suggestive of ILD who underwent cryo-transbronchial lung biopsy (cryo-TBB) under moderate sedation without endotracheal intubation, general anaesthesia or use of fluoroscopy. We performed the procedure using two flexible bronchoscopes connected to two video processors, which we alternated until obtaining the number of desired samples. A definitive diagnosis was obtained in 91 patients (86%). As for complications, there were five pneumothoraces (4.7%) and in no case was there severe haemorrhage or exacerbation of the underlying interstitial disease. Cryo-TBB following our method is a minimally invasive, rapid, safe and economic technique that can be performed in a bronchoscopy suite under moderate sedation without the need for intubating the patient or using fluoroscopy and without requiring general anaesthesia.

Simultaneous determination of 106 pesticides in nuts by LC-MS/MS using freeze-out combined with dispersive solid-phase extraction purification.[Pubmed:28374572]

J Sep Sci. 2017 Jun;40(11):2398-2405.

As a result of the low water content and high fat matrices in nuts, it is very difficult to simultaneously determine multi-pesticides in trace levels. Here, a sample pretreatment method was developed in which, microwave-assisted solvent extraction was firstly used to extract pesticides, and then a two-step cleanup method was conducted combining freeze-out with dispersive solid-phase extraction to remove the lipidic matrix. By this way, 106 pesticides were simultaneously determined in the complicated nut sample by using an ultra-high pressure liquid chromatography coupled with a tandem mass spectrometer. Average recoveries were 75.3-119.3% with relative standard deviations < 14% at three concentration levels. The limits of detection and quantification were in the ranges of 0.3-3.0 and 1.0-10.0 mug/kg, respectively. Furthermore, the method was successfully applied to the determination of pesticides in 180 commercial nut samples.

Activation of prostaglandin EP receptors by lubiprostone in rat and human stomach and colon.[Pubmed:18332851]

Br J Pharmacol. 2008 May;154(1):126-35.

BACKGROUND AND PURPOSE: Lubiprostone (Amitiza), a possible ClC-2 channel opener derived from prostaglandin E(1) and indicated for the treatment of constipation, increases chloride ion transport and fluid secretion into the intestinal lumen. As lubiprostone may also directly modulate gastrointestinal motility, we investigated its actions and the possible involvement of prostaglandin EP receptor activation on rat and human isolated gastrointestinal preparations. EXPERIMENTAL APPROACH: Rat and human isolated preparations were mounted in tissue baths for isometric recording. The effects of lubiprostone on muscle tension and on electrically stimulated, neuronal contractions were investigated in the absence and presence of EP receptor antagonists. KEY RESULTS: In rat and human stomach longitudinal muscle, lubiprostone induced a contraction (pEC(50) of 7.0+/-0.0, n=4 and 6.4+/-0.2, n=3, respectively), which was inhibited by pretreatment with the EP(1) receptor antagonist, EP(1)A 300 nM (pEC(50) reduced to 6.2+/-0.2, n=6), but not by the EP(3) or EP(4) receptor antagonists (L-798106 and GW627368X, respectively, 1 microM, P>0.05). Lubiprostone also reduced electrically stimulated, neuronal contractions in rat and human colon circular muscle preparations (pIC(50) of 8.9+/-0.4, n=7 and 8.7+/-0.9, n=6, respectively), an effect mediated pre-junctionally. This effect was reduced by the EP(4) receptor antagonist (pIC(50) of 6.7+/-1.1, n=7 and 7.7+/-0.4, n=6, respectively) but not by EP(1) or EP(3) receptor antagonists. CONCLUSIONS AND IMPLICATIONS: In rats and humans, lubiprostone contracts stomach longitudinal muscle and inhibits neuronally mediated contractions of colon circular muscle. Experiments are now needed to determine if this additional activity of lubiprostone contributes to its clinical efficacy and/or side-effect profile.

E-ring 8-isoprostanes inhibit ACh release from parasympathetic nerves innervating guinea-pig trachea through agonism of prostanoid receptors of the EP3-subtype.[Pubmed:14744812]

Br J Pharmacol. 2004 Feb;141(4):600-9.

1. In the present study, we examined the effect of E-ring 8-isoprostanes on cholinergic neurotransmission in guinea-pig trachea and identified the receptor(s) involved. As isoprostanes are isomeric with prostaglandins, PGE(2) and sulprostone (a selective EP(3)-receptor agonist) were examined in parallel. 2. 8-Iso-PGE(1), 8-iso-PGE(2) (0.1 nm-1 microM), sulprostone (1 nm-1 microM) and PGE(2) (1 microM) suppressed EFS-evoked [(3)H]ACh release from guinea-pig trachea in a concentration-dependent manner, producing 39.5, 53.9, 61.2 and 59.9% inhibition, respectively, at 1 microM. It should be noted that an established maximum effective concentration was not determined. 3. Neither SQ 29,548 (1 microm; a TP-receptor antagonist) nor AH 6809 (10 microM; an EP(1)-/EP(2)-/DP-receptor antagonist) reversed the inhibitory effect of these compounds. 4. L-798,106, a novel and highly selective EP(3)-receptor antagonist, produced a parallel shift to the right of the concentration-response curves that described the inhibitory action of sulprostone on EFS-evoked contractile responses in guinea-pig vas deferens (an established EP(3)-receptor-expressing tissue), from which a mean pA(2) of 7.48 was derived. On guinea-pig trachea, L-798,106 also antagonised sulprostone-induced inhibition of EFS-induced twitch responses, with similar potency (mean pA(2)=7.82). 5. The inhibitory effects of 8-iso-PGE(1), 8-iso-PGE(2), sulprostone and PGE(2) on EFS-induced [(3)H]ACh release was blocked by L-798,106 at a concentration (10 microM) that binds only weakly to human recombinant EP(1)-, EP(2)- and EP(4)-receptor subtypes expressed in HEK 293 cells. 6. These data suggest that E-ring 8-isoprostanes, PGE(2) and sulprostone inhibit EFS-evoked [(3)H]ACh release from cholinergic nerves innervating guinea-pig trachea, by interacting with prejunctional prostanoid receptors of the EP(3)-subtype.

Structure-activity relationship of cinnamic acylsulfonamide analogues on the human EP3 prostanoid receptor.[Pubmed:11504634]

Bioorg Med Chem. 2001 Aug;9(8):1977-84.

Potent and selective antagonists of the human EP3 receptor have been identified. The structure-activity relationship of the chemical series was conducted and we found several analogues displaying sub-nanomolar K(i) values at the EP3 receptor and micromolar activities at the EP1, EP2 and EP4 receptors. The effect of added human serum albumin (HSA) on the binding affinity at the EP3 receptor was also investigated.

L-798106 is potent and highly selective prostanoid EP3 receptor antagonist (Ki=0.3 nM), it also has micromolar activities at the EP4, EP1 and EP2 receptors with Ki values of 916 nM, >5000 nM and >5000 nM at EP4, EP1 and EP2, respectively.

L-798,106,244101-02-8,Natural Products,Prostanoid Receptors, buy L-798,106 , L-798,106 supplier , purchase L-798,106 , L-798,106 cost , L-798,106 manufacturer , order L-798,106 , high purity L-798,106