Journal: RSC medicinal chemistry

Article Title: Stereochemical optimization of N ,2-substituted cycloalkylamines as norepinephrine reuptake inhibitors.

doi: 10.1039/d4md00521j

Figure Lengend Snippet: Fig. 2 (a) Concentration–inhibition curves of inhibitors 32a, 32b with a (1R,2R)- and (1S,2R)-cyclopentyl orientation, respectively, and (b) 33b, 33d with a trans- and cis-aminocyclohexanol orientation, respectively, in the NET TRACT assay. Cells are pretreated for 1 h with vehicle or one of six increasing concentrations of inhibitor, then stimulated with 1 μM NE or vehicle. NE-induced cellular response is shown as percentage enhancement. Data were normalized to the average top and bottom values of the nisoxetine concentration–inhibition curve. Data are shown as mean ± SEM of three to four individual experiments performed in duplicate.

Article Snippet: Nisoxetine hydrochloride was purchased from Santa Cruz biotechnology (Dallas, TX, USA).

Techniques: Concentration Assay, Inhibition

Journal: The Journal of Pharmacology and Experimental Therapeutics

Article Title: Dopamine Receptor Agonist Treatment of Idiopathic Dystonia: A Reappraisal in Humans and Mice

doi: 10.1124/jpet.117.246348

Figure Lengend Snippet: Effects of enhanced monoaminergic transmission on dystonia induced by cerebellar microinjection of kainate. (A) Peripheral administration of amphetamine, which nonselectively increases the extracellular concentrations of the monoamines dopamine, norepinephrine, and serotonin, dose-dependently reduced the severity of dystonia induced by microinjection of kainate to the cerebellum (one-way ANOVA; F3,28 = 4.813, P < 0.01, n = 8/dose). (B) The selective norepinephrine reuptake inhibitor nisoxetine did not affect the disability score (one-way ANOVA; F3,27 = 0.468, NS, n = 7 to 8/dose). (C) Citalopram, a selective serotonin reuptake inhibitor, did not affect the disability score (one-way ANOVA; F3,26 = 0.317, NS, n = 7 to 8/dose). (D) The selective dopamine reuptake inhibitor GBR-12909 dose-dependently reduced the severity of dystonia (one-way ANOVA; F3,28 = 3.853, P < 0.05, n = 8/dose). Disability scores lower than 10 (dashed lines) suggest abnormal motor behavior, such as an unsteady gait, but not overt dystonia. Values represent the mean of the cumulative disability score in 1 hour ± S.E.M. *P < 0.05; **P < 0.01 compared with vehicle, Holm-Sidak multiple comparisons test. NS, not statistically significant.

Article Snippet: Nisoxetine, citalopram, GBR-12909 (1-[2-[ Bis -(4-fluorophenyl)methoxy]ethyl]-4-(3-phenylpropyl)piperazine dihydrochloride), and apomorphine were purchased from Tocris and dissolved in water.

Techniques: Transmission Assay, Microinjection

Journal:

Article Title: Degradation of Triphenyltin by a Fluorescent Pseudomonad

doi:

Figure Lengend Snippet: Biodegradation of TPT by ATCC strains of fluorescent pseudomonads in SG medium supplemented with TPT. The concentrations of DPT produced by TPT (130 μM) degradation were determined by post-column HPLC analysis. Similar results were obtained in three independent experiments. Symbols: ●, P. chlororaphis ATCC 9446; ▴, P. fluorescens ATCC 13525; ⧫, P. putida ATCC 12633; ■, P. aeruginosa ATCC 15692.

Article Snippet: However, it should be noted that the pyoverdines produced by P. aeruginosa ATCC 15692, P. fluorescens ATCC 13525, and P. chlororaphis ATCC 9446 that exhibit TPT-DF activity have a closely related structure and cross-reactivity to the iron transport system, whereas P. putida ATCC 12633 produces a strain-specific pyoverdine ( 10 , 18 , 27 ).

Techniques: Produced