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Published February 27, 2002 | public
Journal Article

Voltage-dependent transient currents of human and rat 5-HT transporters (SERT) are blocked by HEPES and ion channel ligands

Abstract

The hyperpolarization‐activated transient current of mammalian 5‐hydroxytryptamine transporters (SERT) expressed in Xenopus oocytes was studied. Human (h) and rat (r) SERT transient currents are blocked by HEPES with changes in the waveform kinetics, and the blockade of hSERT has use‐dependent properties. HEPES also changes the time course of the prepriming step, especially for hSERT. Transient currents at hSERT and rSERT are also blocked by spermine and spermidine in the mM range, and by fluoxetine, cocaine, QX‐314, and QX‐222 in the μM range. These pharmacological and kinetic properties of transient current blockade emphasize the similarities between the transient current and phenomena at ion channels.

Additional Information

© 2015 Federation of European Biochemical Societies. Received 17 December 2001; revised 17 January 2002; accepted 17 January 2002. First published online 31 January 2002. We thank Chi‐Sung Chiu and Ken Philipson for helpful discussion. This work was supported by a grant from the National Institutes of Health (DA‐09121) and by an NRSA to M.L.

Additional details

Created:
August 21, 2023
Modified:
October 20, 2023