Search results for "Benzylamines"
showing 10 items of 19 documents
Premature ejaculation: Pharmacotherapy vs group psychotherapy alone or in combination
2017
Objectives: Premature Ejaculation (PE), the commonest sexual dysfunction in males, is generally treated with local anesthetic and SSRI (Dapoxetine). The aim of our study was investigate Group Psychotherapy as an alternative treatment for PE and compare the efficacy of pharmacological treatment and psychotherapy, either alone or in combination, in terms of response and improved Quality of Life (QoL). From a male outpatient population screened for PE, those who received a diagnosis of PE were proposed for the study, enrolled and divided into 3 groups (A, B and C). Each group was treated with Dapoxetine, Group Psychotherapy alone and Dapoxetine and Group Psychotherapy, respectively. Materials …
Bis(5-tert-butyl-2-hydroxy-3-methylbenzyl)(6-hydroxyhexyl)ammonium chloride monohydrate, an anion receptor complex
2007
In the title compound, C(30)H(48)NO(3)(+) x Cl(-) x H(2)O, the cation acts with a water molecule as a chloride ion receptor. The chloride ion forms three strong intramolecular hydrogen bonds. The water molecule forms both an intramolecular bridge between one phenol H atom and the chloride ion, and an intermolecular link to the aliphatic alcohol O atom. Weak intermolecular C-H...Cl and C-H ...O hydrogen bonds provide additional packing interactions.
Synthesis and evaluation in rats of the dopamine D2/3 receptor agonist 18F-AMC20 as a potential radioligand for PET
2015
Dopamine D2/3 receptor (D2/3R) agonist PET tracers are better suited for the imaging of synaptic dopaminergic neurotransmission than D2/3R antagonists and may also offer the opportunity to study in vivo the high-affinity state of D2/3R (D2/3RHigh). With the aim to develop 18F-labeled D2/3R agonists suitable for widespread clinical application, we report here on the synthesis and in vitro and in vivo evaluation of a D2/3R agonist ligand from the aminomethyl chromane (AMC) class-(R)-2-[(4- 18Fluorobenzylamino)methyl]chroman-7-ol (18F-AMC20). Methods: In vitro affinities of AMC20 toward dopaminergic receptor subtypes were measured in membrane homogenates prepared from HEK293 cells expressing h…
Compliance to therapy with Dapoxetine in patients affected by Premature Ejaculation
2012
Introduction Premature ejaculation (PE) is a sexual dysfunction with high prevalence. According to some reports, it is present in about 20-30% of the male population. Since 2009 PE has been treated with a novel inhibitor of serotonin re-uptake, Dapoxetine, which has been reported to be specifically active for PE. Materials and Methods 59 patients have been selected among the patients affected by PE observed at the outpatient department of Urology and Andrology of the “Paolo Giaccone” University Policlinic Hospital of Palermo. Diagnosis was confirmed unequivocally in all patients, who were suitable for drug treatment and accepted to participate in the study. They were divided in 2 groups: on…
From attraction to repulsion : anion–π interactions between bromide and fluorinated phenyl groups
2011
Anion–π interactions in crystals of fluorobenzyl ammonium salts depend on the degree of fluorination at the aromatics.
Plerixafor with and without chemotherapy in poor mobilizers: results from the German compassionate use program.
2010
The CXCR4-inhibitor plerixafor mobilizes hematopoietic stem cells amplifying the effects of granulocyte-CSF (G-CSF). Before approval plerixafor was used in a compassionate use program (CUP) for patients who failed a previous mobilization. In the German CUP 60 patients from 23 centers (median age 56.5 years (2-75)) were given 240 μg/kg plerixafor SC 9-11 h before apheresis. A total of 78.3% (47/60) received G-CSF for 4 days before plerixafor administration; 76.6% of those (36/47) yielded at least 2.0 × 10(6) CD34(+) cells/μL. The median cell yield was 3.35 × 10(6) CD34+ cells/kg (0-29.53). Nine patients received plerixafor alone or with G-CSF for less than 4 days mobilizing a median of 3.30 …
(2S,3S)-2-(N,N-dibenzylamino)butane-1,3-diol refined using a multipolar atom model.
2008
The crystal structure of the title compound, C18H23NO2, was determined using the experimental library multipolar atom model. The refinement showed a significant improvement of crystallographic statistical indices when compared with a conventional spherical neutral atom refinement.
[11C]-DASB microPET imaging in the aged rat: Frontal and meso-thalamic increases in serotonin transporter binding
2011
Whereas molecular imaging studies in the aging human brain have predominantly demonstrated reductions in serotonin transporter (5-HTT) availability, the majority of the rodent studies, using autoradiographic methods, report increases in neural 5-HTT levels with age. To our knowledge, however, no previous rodent studies have assessed this topic in vivo, and therefore it remains unclear whether this discrepancy arises from methodological or inter-species differences. We performed an [(11)C]-DASB microPET study to evaluate the effects of aging on 5-HTT availability in the rat brain. To generate binding potential estimates, quantitative tracer kinetic modeling was applied using the simplified r…
Knock-down of the oxysterol receptor LXRα impairs cholesterol efflux in human primary macrophages: lack of compensation by LXRβ activation.
2012
Liver X Receptors (LXRs) α and β are oxysterol-activated nuclear receptors involved in the control of lipid metabolism and inflammation. Pharmacological activation of LXR is promising in the treatment of atherosclerosis since it can promote cholesterol efflux from macrophages and prevent foam cell formation. However, the development of LXR agonists has been limited by undesirable side-effects such as hepatic steatosis mediated by LXRα activation. Therefore, it has been proposed that targeting LXRα activators to extrahepatic tissues or using LXRβ-specific activators could be used as alternative strategies. It is not clear whether these molecules will retain the full atheroprotective potentia…
iNOS-derived nitric oxide mediates the increase in TFF2 expression associated with gastric damage: role of HIF-1.
2009
Trefoil (TFF) peptides are involved in gastrointestinal mucosal restitution. An hypoxia inducible factor 1 (HIF-1)-dependent induction of TFF genes has been reported in gastric epithelial cells. Nitric oxide (NO) is associated with mucosal damage and modulates HIF-1 activity. The aim of the present study was to analyze the role of iNOS-derived NO in HIF-1alpha stabilization and TFF gene expression in damaged gastric mucosa. Aspirin caused gastric injury that peaked 6 h after dosing and returned to normality at 24 h. iNOS mRNA expression occurs in the corpus in parallel with damage. Blockade of iNOS activity did not modify gastric lesions induced by aspirin but delayed mucosal healing. Aspir…