کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
---|---|---|---|---|
5830412 | 1559037 | 2011 | 7 صفحه PDF | دانلود رایگان |
عنوان انگلیسی مقاله ISI
Synthesis and characterization of [3H]-SN56, a novel radioligand for the Ï1 receptor
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موضوعات مرتبط
علوم زیستی و بیوفناوری
علم عصب شناسی
علوم اعصاب سلولی و مولکولی
پیش نمایش صفحه اول مقاله
![عکس صفحه اول مقاله: Synthesis and characterization of [3H]-SN56, a novel radioligand for the Ï1 receptor Synthesis and characterization of [3H]-SN56, a novel radioligand for the Ï1 receptor](/preview/png/5830412.png)
چکیده انگلیسی
The study of the binding characteristics of Ï ligands in vivo and in vitro requires radiolabeled probes with high affinity and selectivity. The radioligand presently used for in vitro studies of the Ï1 receptor, [3H](+)-pentazocine, has significant limitations; it is difficult to synthesize, has limited chemical stability, and can be problematic to obtain. Evaluation of a series of novel 2(3H)-benzothiazolone compounds revealed SN56 to have sub-nanomolar and preferential affinity for the Ï1 subtype, relative to Ï2 and non-sigma, binding sites. The goal of this study was to characterize the binding of [3H]-SN56 to Ï1 receptors isolated from rat brain. Standard in vitro binding techniques were utilized to 1) determine the specificity and affinity of binding to Ï1 receptors, 2) confirm that [3H]-SN56 labels sites previously identified as Ï1 by comparing binding to sites labeled by [3H](+)-pentazocine, and 3) characterize the kinetics of binding. The results indicate that [3H]-SN56 exhibits 1) specific, saturable, and reversible binding to the Ï1 receptor, with Bmax = 340 ± 10 fmol/mg and Kd = 0.069 ± 0.0074 nM, 2) competitive displacement by classical sigma compounds, yielding Ï1 Ki values consistent with those reported in the literature, and 3) binding kinetics compatible with a 90 min incubation, and filtration for separation of free and bound radioligand. The results of these studies suggest that [3H]-SN56 may serve as a viable alternative to [3H](+)-pentazocine in radioligand binding assays.
ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: European Journal of Pharmacology - Volume 653, Issues 1â3, 25 February 2011, Pages 1-7
Journal: European Journal of Pharmacology - Volume 653, Issues 1â3, 25 February 2011, Pages 1-7
نویسندگان
James A. Fishback, Christophe Mesangeau, Jacques H. Poupaert, Christopher R. McCurdy, Rae R. Matsumoto,