Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions.

Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions. Research Abstract Details 

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Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions. Abstract Text:

Yosuke Yamauchi,Takaya Izumi,Kazuhiro Unemura,Yoshie Uenishi,Takayuki Nakagawa,Shuji Kaneko,Yosuke Yamauchi,Takaya Izumi,Kazuhiro Unemura,Yoshie Uenishi,Takayuki Nakagawa,Shuji Kaneko,Yosuke Yamauchi,Takaya Izumi,Kazuhiro Unemura,Yoshie Uenishi,Takayuki Nakagawa,Shuji Kaneko,

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 K(m) 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 K(i) 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.

Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions. Publishing Authors By Initials

Y Yamauchi,T Izumi,K Unemura,Y Uenishi,T Nakagawa,S Kaneko,Y Yamauchi,T Izumi,K Unemura,Y Uenishi,T Nakagawa,S Kaneko,Y Yamauchi,T Izumi,K Unemura,Y Uenishi,T Nakagawa,S Kaneko,

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Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions. Journal Published:

PUBLICATION TYPE: Journal Article

Journal: Neuroscience letters

VOLUME: 428

Page Numbers: 72-6

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ISSN: 0304-3940

DAY: 26

MONTH: 09

YEAR: 2007

Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions. Information

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LANGUAGE: eng

NlmUniqueID: 7600130

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Grant and Affiliation Information for Acceleration of serotonin transporter transport-associated current by 3,4-methylenedioxymethanphetamine (MDMA) under acidic conditions.

AFFILIATION: Department of Molecular Pharmacology, Graduate School of Pharmaceutical Sciences, Kyoto University, Sakyo-ku, Kyoto 606-8501, Japan.

Country: Ireland

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MEDLINETA: Neurosci Lett

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