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Cited by 281

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The Pharmacological and Functional Characteristics of the Serotonin 5-HT3A Receptor Are Specifically Modified by a 5-HT3B Receptor Subunit

Open access
Dubin, Adrienne E., Huvar, Rene, D'Andrea, Michael R., Pyati, Jayashree, Zhu, Jessica Y., Joy, K.C., Wilson, Sandy J., Galindo, Jose E., Glass, Charles A., Luo, Lin, Jackson, Michael R., Lovenberg, Timothy W., Erlander, Mark G.·1999·Journal of Biological Chemistry

Abstract

While homomers containing 5-HT(3A) subunits form functional ligand-gated serotonin (5-HT) receptors in heterologous expression systems (Jackson, M. B., and Yakel, J. L. (1995) Annu. Rev. Physiol. 57, 447-468; Lambert, J. J., Peters, J. A., and Hope, A. G. (1995) in Ligand-Voltage-Gated Ion Channels (North, R., ed) pp. 177-211, CRC Press, Inc., Boca Raton, FL), it has been proposed that native receptors may exist as heteromers (Fletcher, S., and Barnes, N. M. (1998) Trends Pharmacol. Sci. 19, 212-215). We report the cloning of a subunit 5-HT(3B) with approximately 44% amino acid identity to 5-HT(3A) that specifically modified 5-HT(3A) receptor kinetics, voltage dependence, and pharmacology. Co-expression of 5-HT(3B) with 5-HT(3A) modified the duration of 5-HT(3) receptor agonist-induced responses, linearized the current-voltage relationship, increased agonist and antagonist affinity, and reduced cooperativity between subunits. Reverse transcriptase-polymerase chain reaction in situ hybridization revealed co-localization of both 5-HT(3B) and 5-HT(3A) in a population of neurons in the amygdala, telencephalon, and entorhinal cortex. Furthermore, 5-HT(3A) and 5-HT(3B) mRNAs were expressed in spleen and intestine. Our data suggest that 5-HT(3B) might contribute to tissue-specific functional changes in 5-HT(3)-mediated signaling and/or modulation.

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Metadata

Authors
Dubin, A. E., Huvar, R., D'Andrea, M. R., Pyati, J., Zhu, J. Y., Joy, K. C., Wilson, S. J., Galindo, J. E., Glass, C. A., Luo, L., Jackson, M. R., Lovenberg, T. W., & Erlander, M. G.
Venue
Journal of Biological Chemistry
Publisher
Elsevier BV
Published
1999-10
Volume
274
Issue
43
Pages
30799-30810
ISSN
0021-9258 (ISSN-L)
OpenAlex
W2096091943
Cited by
281
References
1
FWCI
3.55
Type
journal article
Language
en
Open access
hybrid

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CoChat. (2026). Citation check: The Pharmacological and Functional Characteristics of the Serotonin 5-HT3A Receptor Are Specifically Modified by a 5-HT3B Receptor Subunit. https://app.cochat.ai/papers/10.1074/jbc.274.43.30799
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Dubin, A. E., Huvar, R., D'Andrea, M. R., Pyati, J., Zhu, J. Y., Joy, K. C., Wilson, S. J., Galindo, J. E., Glass, C. A., Luo, L., Jackson, M. R., Lovenberg, T. W., & Erlander, M. G. (1999). The Pharmacological and Functional Characteristics of the Serotonin 5-HT3A Receptor Are Specifically Modified by a 5-HT3B Receptor Subunit. Journal of Biological Chemistry. https://doi.org/10.1074/jbc.274.43.30799

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Contains information from the Semantic Scholar Academic Graph Datasets, made available under the ODC Attribution License (ODC-BY 1.0).

Semantic Scholar’s data is described in: Kinney, R., et al. (2023). The Semantic Scholar Open Data Platform. arXiv:2301.10140.