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J Biol Chem, Vol. 274, Issue 43, 30799-30810, October 22, 1999

The Pharmacological and Functional Characteristics of the Serotonin 5-HT_3A Receptor Are Specifically Modified by a 5-HT_3B Receptor Subunit

From the R. W. Johnson Pharmaceutical Research Institute, San Diego, California 92121 and the ^§ R. W. Johnson Pharmaceutical Research Institute, Spring House, Pennsylvania 19477-0776

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 ~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-HT₃ 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-HT₃-mediated signaling and/or modulation.

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