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Differential Membrane Targeting and Pharmacological Characterization of Chimeras of Rat Serotonin 5‐HT~1A~ and 5‐HT~1B~ Receptors Expressed in Epithelial LLC‐PK1 Cells by Michèle Darmon; Xavier Langlois; Laurent Suffisseau; Claude-Michelle Fattaccini; Michel Hamon is a scholarly article available to read on EtoBox.

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Abstract: The serotonin 5‐HT~1A~ and 5‐HT~1B~ receptors are two structurally related but pharmacologically distinguishable 5‐HT receptor types. In brain, the 5‐HT~1A~ receptor is localized on the soma and dendrites of neurons, whereas the 5‐HT~1B~ receptor is targeted to the axon terminals. We previously showed that these two receptors are targeted in different membrane compartments when stably expressed in the epithelial LLC‐PK1 cell line. Further investigations on the mechanisms responsible for their differential targeting were done by constructing chimeras of 5‐HT~1A~ and 5‐HT~1B~ receptors still able to bind specifically [^3^H]lysergic acid diethylamide and selective agonists and antagonists. Their cellular localization examined by confocal microscopy suggests that the third intracellular domain of the 5‐HT~1B~ receptor was responsible for its Golgi‐like localization in transfected LLC‐PK1 cells. In contrast, the third intracellular domain of the 5‐HT~1A~ receptor apparently allowed the sorting of the chimeras to the plasma membrane. Further inclusion of the C‐terminal domain of the 5‐HT~1A~ receptor in their sequence led to a basolateral localization, whereas that of the 5‐HT~

Author

Michèle Darmon; Xavier Langlois; Laurent Suffisseau; Claude-Michelle Fattaccini; Michel Hamon

Publisher

John Wiley and Sons; Wiley (Blackwell Publishing); Blackwell Publishing Inc.; Wiley (ISSN 0022-3042)

Published

1998

Language

EN