PMID- 10521471
OWN - NLM
STAT- MEDLINE
DCOM- 19991123
LR  - 20190508
IS  - 0021-9258 (Print)
IS  - 0021-9258 (Linking)
VI  - 274
IP  - 43
DP  - 1999 Oct 22
TI  - The pharmacological and functional characteristics of the serotonin 5-HT(3A)
      receptor are specifically modified by a 5-HT(3B) receptor subunit.
PG  - 30799-810
AB  - 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.
FAU - Dubin, A E
AU  - Dubin AE
AD  - R. W. Johnson Pharmaceutical Research Institute, San Diego, California 92121,
      USA. audibin@prius.jnj.com
FAU - Huvar, R
AU  - Huvar R
FAU - D'Andrea, M R
AU  - D'Andrea MR
FAU - Pyati, J
AU  - Pyati J
FAU - Zhu, J Y
AU  - Zhu JY
FAU - Joy, K C
AU  - Joy KC
FAU - Wilson, S J
AU  - Wilson SJ
FAU - Galindo, J E
AU  - Galindo JE
FAU - Glass, C A
AU  - Glass CA
FAU - Luo, L
AU  - Luo L
FAU - Jackson, M R
AU  - Jackson MR
FAU - Lovenberg, T W
AU  - Lovenberg TW
FAU - Erlander, M G
AU  - Erlander MG
LA  - eng
SI  - GENBANK/AF169255
PT  - Journal Article
PL  - United States
TA  - J Biol Chem
JT  - The Journal of biological chemistry
JID - 2985121R
RN  - 0 (Biguanides)
RN  - 0 (Macromolecular Substances)
RN  - 0 (Receptors, Serotonin)
RN  - 0 (Receptors, Serotonin, 5-HT3)
RN  - 0 (Recombinant Proteins)
RN  - 0 (Serotonin Receptor Agonists)
RN  - 333DO1RDJY (Serotonin)
RN  - 910A4X901V (1-(3-chlorophenyl)biguanide)
RN  - SY7Q814VUP (Calcium)
SB  - IM
MH  - Amygdala/metabolism
MH  - Animals
MH  - Base Sequence
MH  - Biguanides/pharmacology
MH  - Brain/*metabolism
MH  - Calcium/metabolism
MH  - Cell Line
MH  - Cloning, Molecular
MH  - Entorhinal Cortex/metabolism
MH  - Female
MH  - *Gene Expression Regulation
MH  - Humans
MH  - Kinetics
MH  - Macromolecular Substances
MH  - Membrane Potentials/drug effects
MH  - Molecular Sequence Data
MH  - Neurons/*metabolism
MH  - Oocytes/drug effects/physiology
MH  - Open Reading Frames
MH  - Receptors, Serotonin/chemistry/genetics/*physiology
MH  - Receptors, Serotonin, 5-HT3
MH  - Recombinant Proteins/chemistry/metabolism
MH  - Serotonin/*pharmacology
MH  - Serotonin Receptor Agonists/*pharmacology
MH  - Telencephalon/metabolism
MH  - Transcription, Genetic
MH  - Transfection
MH  - Xenopus laevis
EDAT- 1999/10/16 00:00
MHDA- 1999/10/16 00:01
CRDT- 1999/10/16 00:00
PHST- 1999/10/16 00:00 [pubmed]
PHST- 1999/10/16 00:01 [medline]
PHST- 1999/10/16 00:00 [entrez]
AID - 10.1074/jbc.274.43.30799 [doi]
PST - ppublish
SO  - J Biol Chem. 1999 Oct 22;274(43):30799-810. doi: 10.1074/jbc.274.43.30799.