This title appears in the Scientific Report :
2010
Please use the identifier:
http://dx.doi.org/10.1111/j.1476-5381.2010.00638.x in citations.
Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5-HT1 receptor
Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5-HT1 receptor
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-HT(1) receptor of an insect model for neurobiology, physiology and pharmacology.A cDNA encoding for th...
Saved in:
Personal Name(s): | Troppmann, B. |
---|---|
Balfanz, S. / Baumann, A. / Blenau, W. | |
Contributing Institute: |
Zelluläre Biophysik; ISB-1 |
Published in: | British journal of pharmacology, 159 (2010) S. 1450 - 1462 |
Imprint: |
Malden, MA
Wiley
2010
|
Physical Description: |
1450 - 1462 |
DOI: |
10.1111/j.1476-5381.2010.00638.x |
PubMed ID: |
20233210 |
Document Type: |
Journal Article |
Research Program: |
BioSoft: Makromolekulare Systeme und biologische Informationsverarbeitung |
Series Title: |
British Journal of Pharmacology
158 |
Subject (ZB): | |
Publikationsportal JuSER |
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-HT(1) receptor of an insect model for neurobiology, physiology and pharmacology.A cDNA encoding for the Periplaneta americana 5-HT(1) 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.The P. americana 5-HT(1) receptor (Pea5-HT(1)) shares pronounced sequence and functional similarity with mammalian 5-HT(1) receptors. Activation with 5-HT reduced adenylyl cyclase activity in a dose-dependent manner. Pea5-HT(1) 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.This study marks the first pharmacological identification of an inverse agonist and a neutral antagonist at an insect 5-HT(1) receptor. The results presented here should facilitate further analyses of 5-HT(1) receptors in mediating central and peripheral effects of 5-HT in insects. |