کد مقاله کد نشریه سال انتشار مقاله انگلیسی نسخه تمام متن
4348972 1615182 2007 5 صفحه PDF دانلود رایگان
عنوان انگلیسی مقاله ISI
Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions
موضوعات مرتبط
علوم زیستی و بیوفناوری علم عصب شناسی علوم اعصاب (عمومی)
پیش نمایش صفحه اول مقاله
Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions
چکیده انگلیسی

3,4-Methylenedioxymethamphetamine (MDMA) selectively releases serotonin (5-HT) from neurons after uptake by the serotonin transporter (SERT) and causes psychostimulant effects accompanied by hyperthermia. Since rapid increases in CNS lactate levels are suggested in response to MDMA, we investigated the effects of the physiologically-relevant increase in H+ concentration on the two conducting states of SERT expressed in Xenopus oocytes. Perfusion with SERT substrates at pH 7.4 dose-dependently evoked a transport-associated inward current response with the following rank order of potency: 5-HT > MDMA > dopamine ≫ norepinephrine. In the absence of transport substrates, a step hyperpolarization pulse activated a transient Na+ leak current, which was inhibited by SERT substrates with the same rank, as well as by a SERT inhibitor, citalopram. At pH 6.4, the Km values of 5-HT and dopamine for the transport-associated current were not altered, while that of MDMA was three-fold lower. In contrast, the Ki values of all these substrates for transient leak current were unchanged at pH 6.4, suggesting that the affinities to SERT binding sites are not influenced. These results suggest that the effect of MDMA on SERT is enhanced by acidic conditions.

ناشر
Database: Elsevier - ScienceDirect (ساینس دایرکت)
Journal: Neuroscience Letters - Volume 428, Issues 2–3, 27 November 2007, Pages 72–76
نویسندگان
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