Pharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.

Serotonin (5-hydroxytryptamine, 5-HT) is known for its key role in modulating diverse physiological processes and behaviors by binding various 5-HT receptors. However, a lack of pharmacological knowledge impedes studies on invertebrate 5-HT receptors. Moreover, pharmacological information is urgentl...

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Autores principales:	Rut Vleugels, Cynthia Lenaerts, Arnd Baumann, Jozef Vanden Broeck, Heleen Verlinden
Formato:	article
Lenguaje:	EN
Publicado:	Public Library of Science (PLoS) 2013
Materias:	Medicine R Science Q
Acceso en línea:	https://doaj.org/article/d040e53dc2d941ad9715370b34910923
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spelling	oai:doaj.org-article:d040e53dc2d941ad9715370b349109232021-11-18T07:43:28ZPharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.1932-620310.1371/journal.pone.0065052https://doaj.org/article/d040e53dc2d941ad9715370b349109232013-01-01T00:00:00Zhttps://www.ncbi.nlm.nih.gov/pmc/articles/pmid/23741451/?tool=EBIhttps://doaj.org/toc/1932-6203Serotonin (5-hydroxytryptamine, 5-HT) is known for its key role in modulating diverse physiological processes and behaviors by binding various 5-HT receptors. However, a lack of pharmacological knowledge impedes studies on invertebrate 5-HT receptors. Moreover, pharmacological information is urgently needed in order to establish a reliable classification system for invertebrate 5-HT receptors. In this study we report on the molecular cloning and pharmacological characterization of a 5-HT1 receptor from the red flour beetle, Tribolium castaneum (Trica5-HT1). The Trica5-HT1 receptor encoding cDNA shows considerable sequence similarity with members of the 5-HT1 receptor class. Real time PCR showed high expression in the brain (without optic lobes) and the optic lobes, consistent with the role of 5-HT as neurotransmitter. Activation of Trica5-HT1 in mammalian cells decreased NKH-477-stimulated cyclic AMP levels in a dose-dependent manner, but did not influence intracellular Ca(2+) signaling. We studied the pharmacological profile of the 5-HT1 receptor and demonstrated that α-methylserotonin, 5-methoxytryptamine and 5-carboxamidotryptamine acted as agonists. Prazosin, methiothepin and methysergide were the most potent antagonists and showed competitive inhibition in presence of 5-HT. This study offers important information on a 5-HT1 receptor from T. castaneum facilitating functional research of 5-HT receptors in insects and other invertebrates. The pharmacological profiles may contribute to establish a reliable classification scheme for invertebrate 5-HT receptors.Rut VleugelsCynthia LenaertsArnd BaumannJozef Vanden BroeckHeleen VerlindenPublic Library of Science (PLoS)articleMedicineRScienceQENPLoS ONE, Vol 8, Iss 5, p e65052 (2013)
institution	DOAJ
collection	DOAJ
language	EN
topic	Medicine R Science Q
spellingShingle	Medicine R Science Q Rut Vleugels Cynthia Lenaerts Arnd Baumann Jozef Vanden Broeck Heleen Verlinden Pharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.
description	Serotonin (5-hydroxytryptamine, 5-HT) is known for its key role in modulating diverse physiological processes and behaviors by binding various 5-HT receptors. However, a lack of pharmacological knowledge impedes studies on invertebrate 5-HT receptors. Moreover, pharmacological information is urgently needed in order to establish a reliable classification system for invertebrate 5-HT receptors. In this study we report on the molecular cloning and pharmacological characterization of a 5-HT1 receptor from the red flour beetle, Tribolium castaneum (Trica5-HT1). The Trica5-HT1 receptor encoding cDNA shows considerable sequence similarity with members of the 5-HT1 receptor class. Real time PCR showed high expression in the brain (without optic lobes) and the optic lobes, consistent with the role of 5-HT as neurotransmitter. Activation of Trica5-HT1 in mammalian cells decreased NKH-477-stimulated cyclic AMP levels in a dose-dependent manner, but did not influence intracellular Ca(2+) signaling. We studied the pharmacological profile of the 5-HT1 receptor and demonstrated that α-methylserotonin, 5-methoxytryptamine and 5-carboxamidotryptamine acted as agonists. Prazosin, methiothepin and methysergide were the most potent antagonists and showed competitive inhibition in presence of 5-HT. This study offers important information on a 5-HT1 receptor from T. castaneum facilitating functional research of 5-HT receptors in insects and other invertebrates. The pharmacological profiles may contribute to establish a reliable classification scheme for invertebrate 5-HT receptors.
format	article
author	Rut Vleugels Cynthia Lenaerts Arnd Baumann Jozef Vanden Broeck Heleen Verlinden
author_facet	Rut Vleugels Cynthia Lenaerts Arnd Baumann Jozef Vanden Broeck Heleen Verlinden
author_sort	Rut Vleugels
title	Pharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.
title_short	Pharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.
title_full	Pharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.
title_fullStr	Pharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.
title_full_unstemmed	Pharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.
title_sort	pharmacological characterization of a 5-ht1-type serotonin receptor in the red flour beetle, tribolium castaneum.
publisher	Public Library of Science (PLoS)
publishDate	2013
url	https://doaj.org/article/d040e53dc2d941ad9715370b34910923
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Pharmacological characterization of a 5-HT1-type serotonin receptor in the red flour beetle, Tribolium castaneum.

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