Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor

Since most of our knowledge on pharmacological properties of brain 5-HT4 receptors have been discussed for mouse colliculi neurons, we cloned the corresponding receptor using the RT-PCR approach. As expected, the homology with the already cloned rat 5-HT(4L) receptor was high, revealing only 16 diff...

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Veröffentlicht in:FEBS letters 1996-11, Vol.398 (1), p.19-25
Hauptverfasser: Claeysen, S, Sebben, M, Journot, L, Bockaert, J, Dumuis, A
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container_issue 1
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container_title FEBS letters
container_volume 398
creator Claeysen, S
Sebben, M
Journot, L
Bockaert, J
Dumuis, A
description Since most of our knowledge on pharmacological properties of brain 5-HT4 receptors have been discussed for mouse colliculi neurons, we cloned the corresponding receptor using the RT-PCR approach. As expected, the homology with the already cloned rat 5-HT(4L) receptor was high, revealing only 16 differences at the amino-acid level. One of the differences, proline75 in mouse, alanine75 in the already published rat sequences was not confirmed. Therefore this proline is part of the consensus sequence present in all 5-HT receptor transmembrane domain II (LVMP). Comparing the affinities of 11 agonists and five antagonists for the cloned mouse receptor (5-HT(4L))expressed in LLCPK1 and the corresponding receptor in mouse colliculi shows an excellent correlation. The transfected mouse 5-HT(4L) receptor stimulated cAMP production. When expressed at high density, it exhibited intrinsic activity. In contrast to the previously described distribution, we found that mRNA encoding for both the short (5-HT(4S))and the long form (5-HT(4L)) of 5-HT4 receptors are expressed in all mouse and rat brain areas.
doi_str_mv 10.1016/s0014-5793(96)01132-5
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subjects Age Factors
Amino Acid Sequence
Animals
Animals, Newborn
Base Sequence
Binding Sites
Brain - anatomy & histology
Brain - growth & development
Brain - metabolism
Brain Chemistry
Cloning, Molecular
Inferior Colliculi - chemistry
Mice
Molecular Sequence Data
Rats
Rats, Inbred Strains
Receptors, Serotonin - drug effects
Receptors, Serotonin - genetics
Receptors, Serotonin - metabolism
Receptors, Serotonin, 5-HT4
Serotonin Antagonists - pharmacology
Serotonin Receptor Agonists - pharmacology
Species Specificity
Transfection
title Cloning, expression and pharmacology of the mouse 5-HT(4L) receptor
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