Although there is evidence for an important role of UGT2B10 in the N-glucuronidation of drugs and other xenobiotics, the inhibitor selectivity of this enzyme is poorly understood. This study sought primarily to characterize the inhibition selectivity of UGT2B10 by UDP-glucuronosyltransferase (UGT) enzyme-selective inhibitors used for reaction phenotyping, and 34 antidepressant and antipsychotic...

[3H]Doxepin, a tricyclic antidepressant, binds with high affinity to guinea pig brain membranes with a drug specificity indicating an association with H1 histamine receptors. The [3H]doxepin binding site has been solubilized, with digitonin being the only detergent able to maintain specific binding after solubilization. After solubilization, the kinetics and drug specificity of binding are virt...

We report a method for simultaneous measurement of five commonly used tricyclic antidepressant drugs (doxepin, desipramine, nortriptyline, imipramine, and amitriptyline) in serum by paired-ion high-performance liquid chromatography, with use of a reversed-phase column and ultraviolet detection at 254 nm. The drugs are extracted from 2 ml of serum at pH 14 into hexane/isoamyl alcohol (99/1 by vo...

GST pi, the main glutathione S-transferase isoform present in the human brain, was isolated from various regions of the brain and the in vitro effect of tricyclic antidepressants on its activity was studied. The results indicated that amitripyline and doxepin--derivatives of dibenzcycloheptadiene, as well as imipramine and clomipramine--derivatives of dibenzazepine, inhibit the activity of GST ...

Specific interventions included in the review Studies of RIMAs, i.e. MOC (18 to 600 mg) or BRO (93.1 to 150 mg/day) versus either placebo or another standard tricyclic antidepressant, selective serotonin re-uptake inhibitor (SSRI) or other class of antidepressant, were included. The active comparison groups included: diazepam, tranylcypromine, mianserin, isocarboxide, imipramine, amitriptyline,...

as contained in application WO8903692) Compositions useful in the treatment of disturbances of appetite, disturbances of mood, or both, associated with premenstrual syndrome, as well as methods of use therefor. The compositions include serotoninergic drugs, such as d-fenfluramine and fluoxetine. Claims 1. Use of one or more serotonin-mediated neurotransmission enhancing drugs for the manufactur...