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 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 Ca2+ 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.

• Publication year

  2013

• Venue

  PLoS ONE

• Publication date

  2013-05-31

• Fields of study

  Biology, Medicine

• Identifiers
  DOI 10.1371/journal.pone.0065052PMID 23741451PMCID 3669024
• External record

  Open on Semantic Scholar

• Source metadata

  Semantic Scholar, PubMed

• No claims are published for this paper.

• No concepts are published for this paper.

• Molecular and Pharmacological Characterization of Serotonin 5-HT2α and 5-HT7 Receptors in the Salivary Glands of the Blowfly Calliphora vicina

  2012cited by this paper
• Serotonin is Critical for Rewarded Olfactory Short-Term Memory in Drosophila

  2012cited by this paper
• Critical role for protein kinase A in the acquisition of gregarious behavior in the desert locust

  2011cited by this paper
• Inverse agonist and neutral antagonist actions of synthetic compounds at an insect 5‐HT1 receptor

  2010cited by this paper
• Evaluation of quantitative PCR reference genes for gene expression studies in Tribolium castaneum after fungal challenge.

  2010cited by this paper
• Characterization of the 5-HT1A receptor of the honeybee (Apis mellifera) and involvement of serotonin in phototactic behavior

  2010cited by this paper
• Serotonin Mediates Behavioral Gregarization Underlying Swarm Formation in Desert Locusts

  2009cited by this paper
• BeetleBase in 2010: revisions to provide comprehensive genomic information for Tribolium castaneum

  2009cited by this paper
• The expanded biology of serotonin.

  2009cited by this paper
• Conservation of structure, signaling and pharmacology between two serotonin receptor subtypes from decapod crustaceans, Panulirus interruptus and Procambarus clarkii

  2008cited by this paper
• The genome of the model beetle and pest Tribolium castaneum

  2008cited by this paper
• Serotonin is necessary for place memory in Drosophila

  2008cited by this paper
• Molecular biology of 5-HT receptors.

  2008cited by this paper
• Serotonin receptors.

  2008cited by this paper
• A genome-wide inventory of neurohormone GPCRs in the red flour beetle Tribolium castaneum.

  2008cited by this paper
• REVIEWS IN BASIC AND CLINICAL GASTROENTEROLOGY The Serotonin Signaling System: From Basic Understanding To Drug Development for Functional GI Disorders

  2007cited by this paper
• Serotonin and neuropeptide F have opposite modulatory effects on fly aggression

  2007cited by this paper
• The aminergic control of cockroach salivary glands.

  2006cited by this paper
• A sleep-promoting role for the Drosophila serotonin receptor 1A.

  2006cited by this paper
• Am5‐HT7: molecular and pharmacological characterization of the first serotonin receptor of the honeybee (Apis mellifera)

  2006cited by this paper
• A review of neurohormone GPCRs present in the fruitfly Drosophila melanogaster and the honey bee Apis mellifera.

  2006cited by this paper
• Serotonin modulates circadian entrainment in Drosophila.

  2005cited by this paper
• Molecular cloning and functional expression of a serotonin receptor from the Southern cattle tick, Boophilus microplus (Acari: Ixodidae)

  2004cited by this paper
• The association of serotonin with the alimentary canal of the African migratory locust, Locusta migratoria: distribution, physiology and pharmacological profile.

  2003cited by this paper
• Analysis of C-terminally substituted tachykinin-like peptide agonists by means of aequorin-based luminescent assays for human and insect neurokinin receptors.

  2002cited by this paper
• Molecular biology of serotonin receptors structure and function at the molecular level.

  2002cited by this paper
• The medical benefit of 5-HT research.

  2002cited by this paper
• Functional characterization of a novel serotonin receptor (5‐HTap2) expressed in the CNS of Aplysia californica

  2002cited by this paper
• A Drosophila dopamine 2-like receptor: Molecular characterization and identification of multiple alternatively spliced variants

  2002cited by this paper
• Accurate normalization of real-time quantitative RT-PCR data by geometric averaging of multiple internal control genes

  2002cited by this paper
• Molecular, pharmacological and functional diversity of 5-HT receptors.

  2002cited by this paper
• Cloning and expression analysis of a 5HT7‐like serotonin receptor cDNA from mosquito Aedes aegypti female excretory and respiratory systems

  2001cited by this paper
• Structure and function of invertebrate 5-HT receptors: a review.

  2001cited by this paper
• A highly conserved aspartic acid (Asp-155) anchors the terminal amine moiety of tryptamines and is involved in membrane targeting of the 5-HT(2A) serotonin receptor but does not participate in activation via a "salt-bridge disruption" mechanism.

  2000cited by this paper
• Uncovering molecular mechanisms involved in activation of G protein-coupled receptors.

  2000cited by this paper
• A highly conserved aspartic acid (Asp-155) anchors the terminal amine moiety of tryptamines and is involved in membrane targeting of the 5-HT(2A) serotonin receptor but does not participate in activation via a "salt-bridge disruption" mechanism.

  2000cited by this paper
• CCR5 binds multiple CC-chemokines: MCP-3 acts as a natural antagonist.

  1999cited by this paper
• Cloning and Functional Expression of an Aplysia 5-HT Receptor Negatively Coupled to Adenylate Cyclase

  1998cited by this paper
• Origin of the metazoan phyla: molecular clocks confirm paleontological estimates.

  1998cited by this paper
• Evaluation of a CRE-Directed Luciferase Reporter Gene Assay as an Alternative to Measuring cAMP Accumulation

  1997cited by this paper
• Molecular cloning and functional expression of a serotonin receptor fromCaenorhabditis elegans

  1997cited by this paper
• Functional characteristics of heterologously expressed 5-HT receptors.

  1997cited by this paper
• Identification of conserved aromatic residues essential for agonist binding and second messenger production at 5-hydroxytryptamine2A receptors.

  1997cited by this paper
• Evolution and overview of classical transmitter molecules and their receptors

  1996cited by this paper
• [19] Integrated methods for the construction of three-dimensional models and computational probing of structure-function relations in G protein-coupled receptors

  1995cited by this paper
• The family of G‐protein‐coupled receptors

  1995cited by this paper
• 5-hydroxytryptamine in the salivary glands of adult female Aedes aegypti and its role in regulation of salivation.

  1995cited by this paper
• Drosophila 5-HT2 serotonin receptor: coexpression with fushi-tarazu during segmentation.

  1995cited by this paper
• The high affinity state of the beta 2-adrenergic receptor requires unique interaction between conserved and non-conserved extracellular loop cysteines.

  1994cited by this paper
• The molecular evolution of G protein-coupled receptors: focus on 5-hydroxytryptamine receptors.

  1994cited by this paper
• Molecular biology of 5-HT receptors.

  1994cited by this paper
• International Union of Pharmacology classification of receptors for 5-hydroxytryptamine (Serotonin).

  1994cited by this paper
• A highly conserved tyrosine residue in G protein-coupled receptors is required for agonist-mediated beta 2-adrenergic receptor sequestration.

  1994cited by this paper
• Serotonin receptor cDNA cloned from Lymnaea stagnalis.

  1993cited by this paper
• A family of Drosophila serotonin receptors with distinct intracellular signalling properties and expression patterns.

  1992cited by this paper
• A sensorory input inhibiting heart rate in an insect,Rhodnius prolixus

  1992cited by this paper
• Serotoninergic elements in the stomatogastric nervous system of the stick insect, Carausius morosus, demonstrated by immunohistochemistry

  1991cited by this paper
• Cloning and characterization of a Drosophila serotonin receptor that activates adenylate cyclase.

  1990cited by this paper
• Physiological control of nutrient self-selection in Heliothis zea larvae: The role of serotonin

  1988cited by this paper
• The pharmacology of the isolated foregut of the locust schistocerca gregaria—I. the effect of a range of putative neurotransmitters

  1987cited by this paper
• Neurons reactive to antibodies against serotonin in the stomatogastric nervous system and in the alimentary canal of locust and crickets (Orthoptera, Insecta).

  1986cited by this paper
• Serotonin and the Control of Salivation in the Blowfly Calliphora

  1985cited by this paper
• The Schild regression in the process of receptor classification.

  1982cited by this paper
• Spontaneous activity of foregut and hindgut visceral muscle of the locust, Locusta migratoria—II. The effect of biogenic amines

  1982cited by this paper
• Comparative pharmacological properties of muscle function in the foregut and the hindgut of the cockroach Leucophaea maderae.

  1978cited by this paper
• Insect Salivary Glands: Stimulation of Fluid Secretion by 5-Hydroytryptamine and Adenosine-3',5'-monophosphate

  1968cited by this paper
• The effect of drugs on the alimentary canal of the African migratory locust Locusta migratoria.

  1966cited by this paper
• The Mode of Action of the Corpus Cardiacum on the Hind Gut in Periplaneta Americana

  1962cited by this paper

• Pharmacological characterization and functional roles of the 5‐HT7 receptor for pheromone sensitivity and mating in Helicoverpa armigera

  2025cites this paper
• Oxygen-dependent regulation of serotonin receptor 5-HT1A in hypoxic response and flight performance in bumblebees, Bombus terrestris

  2025cites this paper
• Deletion of the Serotonin Receptor 7 Gene Changed the Development and Behavior of the Mosquito, Aedes aegypti

  2022cites this paper
• Identification and Pharmacological Characterization of Two Serotonin Type 7 Receptor Isoforms from Mythimna separata

  2022cites this paper
• Involvement of Cis-Acting Elements in Molecular Regulation of JH-Mediated Vitellogenin Gene 2 of Female Periplaneta americana

  2021cites this paper
• Characterization of a new type of neuronal 5-HT G- protein coupled receptor in the cestode nervous system

  2021cites this paper
• Serotonin in Animal Cognition and Behavior

  2020cites this paper
• The stalk-eyed fly as a model for aggression – is there a conserved role for 5-HT between vertebrates and invertebrates?

  2020cites this paper
• Serotonergic Modulation Across Sensory Modalities.

  2020cites this paper
• Can BRET-based biosensors be used to characterize G-protein mediated signaling pathways of an insect GPCR, the Schistocerca gregaria CRF-related diuretic hormone receptor?

  2020cites this paper
• An insect serotonin receptor mediates cellular immune responses and its inhibition by phenylethylamide derivatives from bacterial secondary metabolites

  2019cites this paper
• Pharmacological characterization of the 5-HT1A receptor of Bombyx mori and its role in locomotion.

  2019cites this paper
• Phenylethylamides derived from bacterial secondary metabolites specifically inhibit an insect serotonin receptor

  2019cites this paper
• Exploring Neuromodulatory Effects of Adenosine Deaminase and Corazonin in Emerald Jewel Wasp Venom

  2019cites this paper
• Sex differences in aggression: Differential roles of 5-HT2, neuropeptide F and tachykinin

  2018cites this paper
• Dopamine signalling in locusts and other insects.

  2018cites this paper
• Molecular cloning and functional expression of the 5-HT7 receptor in Chinese mitten crab (Eriocheir sinensis).

  2018cites this paper
• Invertebrate serotonin receptors: a molecular perspective on classification and pharmacology

  2018cites this paper
• Parasitoid Jewel Wasp Mounts Multipronged Neurochemical Attack to Hijack a Host Brain*

  2018cites this paper
• Cloning and functional characterization of the DA2 receptor gene in Chinese mitten crab (Eriocheir sinensis)

  2018cites this paper
• 2.17 – Diverse Functions of Insect Biogenic Amines as Neurotransmitters, Neuromodulators, and Neurohormones

  2017cites this paper
• Molecular cloning and characterization of the SIFamide precursor and receptor in a hymenopteran insect, Bombus terrestris.

  2017cites this paper
• Characterization of three serotonin receptors from the small white butterfly, Pieris rapae.

  2017influential citation
• From Molecules to Management: Mechanisms and Consequences of Locust Phase Polyphenism

  2017cites this paper
• Identification, functional characterization, and pharmacological profile of a serotonin type-2b receptor in the medically important insect, Rhodnius prolixus

  2015cites this paper
• Bases comportementales et génétiques des apprentissages aversif et appétitif chez l'abeille, Apis mellifera

  2015cites this paper
• De novo assembly and characterization of central nervous system transcriptome reveals neurotransmitter signaling systems in the rice striped stem borer, Chilo suppressalis

  2015cites this paper
• Pharmacological and signalling properties of a D2-like dopamine receptor (Dop3) in Tribolium castaneum.

  2015cites this paper
• Serotonin, serotonin receptors and their actions in insects

  2014cites this paper
• Rapid behavioural gregarization in the desert locust, Schistocerca gregaria entails synchronous changes in both activity and attraction to conspecifics

  2014cites this paper
• Larvae of the small white butterfly, Pieris rapae, express a novel serotonin receptor

  2014cites this paper
• Signalling properties and pharmacology of a 5‐HT7‐type serotonin receptor from Tribolium castaneum

  2014cites this paper
• Pharmacological modulation of aversive responsiveness in honey bees

  2014cites this paper
• Signaling Properties and Pharmacological Analysis of Two Sulfakinin Receptors from the Red Flour Beetle, Tribolium castaneum

  2014cites this paper
• Mechanisms underlying dual effects of serotonin during development of Helisoma trivolvis (Mollusca)

  2014cites this paper
• Receptors for Neuronal or Endocrine Signalling Molecules as Potential Targets for the Control of Insect Pests

  2014cites this paper