کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
10838677 | 1067174 | 2005 | 8 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Neurochemical, pharmacokinetic, and behavioral effects of the novel selective serotonin reuptake inhibitor BMS-505130
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کلمات کلیدی
CmaxNPGTail suspension test - آزمون تعلیق دمmaximum plasma concentration - حداکثر غلظت پلاسماSerotonin transporter (SERT) - حمل کننده سروتونین (SERT)Premature ejaculation - زود انزالی، انزال زودرسSelective serotonin reuptake inhibitor - مهار کننده بازجذب سروتونین انتخابیSelective serotonin reuptake inhibitor (SSRI) - مهارکننده بازجذب سروتونین (SSRI)SSRI - مهارکنندههای بازجذب سروتونینmicrodialysis - میکرو دیالیزNucleus paragigantocellularis - هسته paragigantocellularis
موضوعات مرتبط
علوم زیستی و بیوفناوری
بیوشیمی، ژنتیک و زیست شناسی مولکولی
زیست شیمی
پیش نمایش صفحه اول مقاله

چکیده انگلیسی
BMS-505130 is a potent and selective serotonin transport inhibitor; Ki for binding to the serotonin transporter=0.18 nM (Ki values for binding to the norepinephrine and dopamine transporters=4.6 and 2.1 μM, respectively). In platelet serotonin uptake studies BMS-505130 (5 mg/kg, p.o.) produced a robust inhibition of serotonin uptake. In microdialysis studies oral dosing with BMS-505130 produced a dose-dependent increase in cortical serotonin levels that reached a maximal effect of 200% above baseline at a dose of 1 mg/kg, p.o.; the peak serotonin response was transient in nature. Following oral administration, peak plasma concentrations of BMS-505130 reached Tmax at 1.6±0.7 h and then declined to concentrations <10% of Cmax within the following 6 h; plasma half-life following i.v. dosing was 0.46±0.02 h. Parallel microdialysis and pharmacokinetic studies revealed that changes in serotonin levels in the cortex mirrored changes in the brain concentration of BMS-505130. In a behavioral assay known to be sensitive to selective serotonin reuptake inhibitors (SSRIs), mouse tail suspension, BMS-505130 produced a robust response after either oral or intraperitoneal dosing. BMS-505130 exhibits a pharmacological, neurochemical and behavioral profile consistent with a potent SSRI. Moreover, BMS-505130's short half-life may be advantageous for the treatment of premature ejaculation where an acute effect to delay ejaculation followed by a relatively rapid fall in SSRI plasma concentrations might be desirable.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Pharmacology Biochemistry and Behavior - Volume 80, Issue 3, March 2005, Pages 521-528
Journal: Pharmacology Biochemistry and Behavior - Volume 80, Issue 3, March 2005, Pages 521-528
نویسندگان
Matthew T. Taber, Robert N. Wright, Thaddeus F. Molski, Wendy J. Clarke, Patrick J. Brassil, Derek J. Denhart, Ronald J. Mattson, Nicholas J. Lodge,