Home About us Contact
|
Home About us Contact | ||
|
|
||
Reuptake Inhibition (reuptake + inhibition)
Selected AbstractsNovel 2-N,N-Dimethylaminomethyl-2,3,3a,12b-tetrahydrodibenzo[b,f]furo [2,3-d]oxepin Derivatives Displaying Combined Norepinephrine Reuptake Inhibition and 5-HT2A/2C Receptor Antagonism.CHEMINFORM, Issue 40 2005Jose M. Bartolome Abstract For Abstract see ChemInform Abstract in Full Text. [source] Synthesis of new 5-substitutedbenzo[b]thiophene derivativesJOURNAL OF HETEROCYCLIC CHEMISTRY, Issue 5 2001S. Pérez-Silanes Previous works of our group have dealt with the synthesis of 1-(aryl)-3-[4-(aryl)piperazin-1-yl]propane derivatives in the search for new and efficient antidepressants with a dual mode of action: serotonin reuptake inhibition and 5-HT1A receptor afinity [1-4]. From these studies we concluded that the 3-[4-(aryl)piperazin-1-yl]-1-(benzo[b]thiophen-3-yl)propane derivatives led to the best results. The continuation of this research project required the preparation of some new 3-acyl-5-substituted benzo[b]thiophenes with a wide variety of substituents at the 5 position, ranging from nitro to hydroxyl derivatives. To obtain these derivatives we acylated the corresponding 5-substituted benzo[b]thiophenes when it was possible. [source] Hemorrhagic stroke associated with antidepressant use in patients with depression: does degree of serotonin reuptake inhibition matter?PHARMACOEPIDEMIOLOGY AND DRUG SAFETY, Issue 3 2009Yan Chen MD Abstract Objective This study aimed to determine whether the degree of serotonin (5-HT) reuptake inhibition affects risk of hemorrhagic stroke associated with antidepressant use in patients with depression. Method A population-based, nested case-control study was performed using a managed care medical claims database. Ninety two depressed patients with a diagnosis of hemorrhagic stroke were identified and matched with 552 controls by age, sex, and year of index date of depression (IDD). Diagnoses of depression, hemorrhagic stroke, and other medical comorbidities were identified using ICD-9 codes. Antidepressants were classified as high, medium, or low reuptake inhibition based on their affinities for the 5-HT reuptake transporter, determined using their respective equilibrium dissociation constants (KD; high: KD,<,1,nM; medium: 1,,,KD,<,10,nM; low: KD,,,10,nM). Conditional logistic regression analysis was performed to estimate the crude and adjusted odds ratios (ORs) with 95% confidence intervals (CIs) of the risk of hemorrhagic stroke. Results Compared to non-users of antidepressants, risk of hemorrhagic stroke did not significantly differ between patients who had ever used antidepressants with high (OR,=,0.82; 95% CI,=,0.44,1.55), medium (OR,=,0.93; 95% CI,=,0.37,2.31), or low (OR,=,0.38; 95% CI,=,0.11,1.41) 5-HTT inhibition. Conclusion Risk of hemorrhagic stroke associated with antidepressant use may not be related to an antidepressant's degree of 5-HT reuptake inhibition. Given the limitations of this study, additional studies are needed to confirm these findings. Copyright © 2009 John Wiley & Sons, Ltd. [source] Ef,ciency of antidepressant drugs as monoamine reuptake inhibitors: analysis of the hydrophobicity in,uence using biopartitioning micellar chromatographic dataBIOMEDICAL CHROMATOGRAPHY, Issue 7 2004C. Quiñones-Torrelo Abstract The reuptake blockade of biogenic amines by antidepressants is related not only to their therapeutics effects, but also to their side effects and potential drug,drug interactions. As an alternative to classical quantitative structure,activity relationships studies, in this work we propose different quantitative retention,activity relationships (QRAR) models that are able to describe the monoamine reuptake inhibition by antidepressants. The retention of compounds is measured using a biopartitioning micellar chromatography (BMC) system that can simulate the same hydrophobic, electronic and steric molecular interactions as those that condition drug activity. Since all the compounds considered in this work are structurally related because all of them share the same molecular features as the corresponding basic pharmacophore, the results obtained show that there is a retention range in which antidepressants present the highest monoamine reuptake inhibitor potency. Copyright © 2003 John Wiley & Sons, Ltd. [source] | ||||||||||