31506
2010
2010
eng
article
1
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Characterization of the 5-HT1A receptor of the honeybee (Apis mellifera) and involvement of serotonin in phototactic behavior
Serotonin plays a key role in modulating various physiological and behavioral processes in both protostomes and deuterostomes. The vast majority of serotonin receptors belong to the superfamily of G-protein-coupled receptors. We report the cloning of a cDNA from the honeybee (Am5-ht1A) sharing high similarity with members of the 5-HT1 receptor class. Activation of Am5-HT1A by serotonin inhibited the production of cAMP in a dose-dependent manner (EC50 = 16.9 nM). Am5-HT1A was highly expressed in brain regions known to be involved in visual information processing. Using in vivo pharmacology, we could demonstrate that Am5-HT1A receptor ligands had a strong impact on the phototactic behavior of individual bees. The data presented here mark the first comprehensive study-from gene to behavior-of a 5-HT1A receptor in the honeybee, paving the way for the eventual elucidation of additional roles of this receptor subtype in the physiology and behavior of this social insect.
http://www.springerlink.com/content/101193
10.1007/s00018-010-0350-6
1420-682X
allegro:1991-2014
10107821
Cellular and molecular life sciences. - ISSN 1420-682X. - 67 (2010), 14, S. 2467 - 2479
Markus Thamm
Sabine Balfanz
Richarda Scheiner
Arnd Baumann
Wolfgang Blenau
Institut für Biochemie und Biologie
Referiert
4427
2010
eng
postprint
1
2010-08-30
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Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5-HT1 receptor
Background and purpose: 5-Hydroxytryptamine (5-HT) has been shown to control and modulate many physiological and behavioural functions in insects. In this study, we report the cloning and pharmacological properties of a 5-HT1 receptor of an insect model for neurobiology, physiology and pharmacology. Experimental approach: A cDNA encoding for the Periplaneta americana 5-HT1 receptor was amplified from brain cDNA. The receptor was stably expressed in HEK 293 cells, and the functional and pharmacological properties were determined in cAMP assays. Receptor distribution was investigated by RT-PCR and by immunocytochemistry using an affinity-purified polyclonal antiserum. Key results: The P. americana 5-HT1 receptor (Pea5-HT1) shares pronounced sequence and functional similarity with mammalian 5-HT1 receptors. Activation with 5-HT reduced adenylyl cyclase activity in a dose-dependent manner. Pea5-HT1 was expressed as a constitutively active receptor with methiothepin acting as a neutral antagonist, and WAY 100635 as an inverse agonist. Receptor mRNA was present in various tissues including brain, salivary glands and midgut. Receptor-specific antibodies showed that the native protein was expressed in a glycosylated form in membrane samples of brain and salivary glands. Conclusions and implications: This study marks the first pharmacological identification of an inverse agonist and a neutral antagonist at an insect 5-HT1 receptor. The results presented here should facilitate further analyses of 5-HT1 receptors in mediating central and peripheral effects of 5-HT in insects.
urn:nbn:de:kobv:517-opus-44346
4434
British journal of pharmacology 159 (2010), 7, S. 1450 - 1462, DOI 10.1111/j.1476-5381.2010.00638.x
<hr>The definitive version is available at www3.interscience.wiley.com:
<br><a href="http://www3.interscience.wiley.com/journal/121548564/home">
British journal of pharmacology</a>. - 159 (2010), 7, S. 1450-1462<br>
ISSN 0007-1188<br>
DOI <a href="http://dx.doi.org/10.1111/j.1476-5381.2010.00638.x"> 10.1111/j.1476-5381.2010.00638.x</a>
Keine öffentliche Lizenz: Unter Urheberrechtsschutz
Britta Troppmann
Sabine Balfanz
Arnd Baumann
Wolfgang Blenau
eng
uncontrolled
Biogenic amine
eng
uncontrolled
constitutive activity
eng
uncontrolled
cellular signalling
eng
uncontrolled
G-protein-coupled receptor
eng
uncontrolled
insect
Biowissenschaften; Biologie
Institut für Biochemie und Biologie
Universität Potsdam