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Molecular, pharmacological, and signaling properties of octopamine receptors from honeybee ( Apis mellifera ) brain
Author(s) -
Balfanz Sabine,
Jordan Nadine,
Langenstück Teresa,
Breuer Johanna,
Bergmeier Vera,
Baumann Arnd
Publication year - 2014
Publication title -
journal of neurochemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.75
H-Index - 229
eISSN - 1471-4159
pISSN - 0022-3042
DOI - 10.1111/jnc.12619
Subject(s) - octopamine (neurotransmitter) , receptor , biogenic amine , second messenger system , biology , g protein coupled receptor , adenylyl cyclase , signal transduction , biochemistry , pharmacology , serotonin
G protein‐coupled receptors are important regulators of cellular signaling processes. Within the large family of rhodopsin‐like receptors, those binding to biogenic amines form a discrete subgroup. Activation of biogenic amine receptors leads to transient changes of intracellular Ca 2+ ‐([Ca 2+ ] i ) or 3′,5′‐cyclic adenosine monophosphate ([ cAMP ] i ) concentrations. Both second messengers modulate cellular signaling processes and thereby contribute to long‐lasting behavioral effects in an organism. In vivo pharmacology has helped to reveal the functional effects of different biogenic amines in honeybees. The phenolamine octopamine is an important modulator of behavior. Binding of octopamine to its receptors causes elevation of [Ca 2+ ] i or [ cAMP ] i . To date, only one honeybee octopamine receptor that induces Ca 2+ signals has been molecularly and pharmacologically characterized. Here, we examined the pharmacological properties of four additional honeybee octopamine receptors. When heterologously expressed, all receptors induced cAMP production after binding to octopamine with EC 50s in the nanomolar range. Receptor activity was most efficiently blocked by mianserin, a substance with antidepressant activity in vertebrates. The rank order of inhibitory potency for potential receptor antagonists was very similar on all four honeybee receptors with mianserin >> cyproheptadine > metoclopramide > chlorpromazine > phentolamine. The subroot of octopamine receptors activating adenylyl cyclases is the largest that has so far been characterized in arthropods, and it should now be possible to unravel the contribution of individual receptors to the physiology and behavior of honeybees.The biogenic amine octopamine is an important modulator of behavior and physiology in arthropods. Binding of octopamine to specific G protein‐coupled receptors causes elevation of [Ca 2+ ] i or [cAMP] i . Only one honeybee octopamine receptor inducing Ca 2+ signals has been experimentally characterized, yet. Here, we present the pharmacological properties of four additional members of the honeybee octopamine receptor family causing cAMP production.