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Octopamine enhances dark-adaptation in Limulus ventral photoreceptors.

Limulus ventral photoreceptors receive synaptic input from fibers that emerge from the brain and that appear to use octopamine as a transmitter. Exogenous application of octopamine has been shown to increase levels of intracellular cAMP in ventral photoreceptors, but the resulting physiological effects have been unclear. In this report, we show that octopamine increases the rate of dark-adaptation following a bright light. Since a similar increase in the rate of dark-adaptation is produced by IBMX (1 mM) and forskolin (100 microM), drugs shown previously to raise the concentration of cAMP, the octopamine effect may be mediated by cAMP. Our results suggest that dark-adaptation, a fundamental process of photoreceptors, is under efferent neural control.

1-Methyl-3-isobutylxanthine↗

Comparison of o-octopamine and related phenylethanolamines as substrates for norepinephrine N-methyltransferase.

o-Octopamine was a substrate for rabbit adrenal norepinephrine N-methyltransferase with lower affinity than the position isomers m-octopamine and p-octopamine. The order of substrate affinity for monochloro or monohydroxy phenylethanolamines was para greater than meta greater than ortho. With phenylethanolamine and ring-hydroxylated phenylethanolamines, primary amines were better substrates than were N-methyl secondary amines. N-Methylation might be a metabolic pathway for o-octopamine, reported to occur in mammalian tissues.

Adrenal Glands↗

[Specific stimulation of adipose tissue adrenergic beta 3 receptors by octopamine].

A new subtype of beta-adrenoceptor (beta 3) has been recently characterized in human and rodent genome. This receptor can be stimulated with catecholamines or selective pharmacological beta 3-adrenoceptor agonists and it fulfils similar function of norepinephrine in rodent and dog adipose tissue. Octopamine but not tyramine or phenylethylamine activated lipolysis in dog fat cells as well as BRL 37344 (a beta 3-adrenoceptor agonist) or norepinephrine. In human fat cells, norepinephrine was lipolytic whereas BRL 37344 or octopamine were without effect. The lipolytic effect of octopamine did not depend on beta 1-/beta 2-adrenoceptor stimulation since it was not suppressed by beta 1- or beta 2-antagonists. These results suggest that octopamine is a specific endogenous ligand for beta 3-adrenoceptors in mammals.

Adipose Tissue↗

Stress-induced release of octopamine in the American cockroach Periplaneta americana L.

After stress, changes of octopamine content were observed in the antennal heart and the retrocerebral complex of cockroaches. Only individually handled animals exposed to short and extreme stress showed an alteration in the haemolymph octopamine levels. The removal of the retrocerebral complex resulted in an elevation of the octopamine content in the haemolymph. We suppose that the corpora cardiaca are not the only source for the octopamine released into haemolymph in stress situations.

Animals↗

Octopamine in the developing nervous system of the pond snail, Lymnaea stagnalis L.

Development of the octopaminergic system in the pond snail, Lymnaea stagnalis, was investigated by means of immunocytochemistry and radioenzymatic assay. The earliest octopamine-immunoreactive neurons appear at a late embryonic stage (E85) of development following metamorphosis. At this moment of development, the adult-like pattern of distribution and projection (arborization) characteristics of octopamine-immunoreactive neurone can already be observed. During hatching and postembryonic (juvenile) development the number of labelled neurons increases only within the ventro-medial cell groups of the cerebral ganglia, whereas the extent of varicose axon arborization of the labelled neurons increases gradually. No peripheral projections of the embryonic and postembryonic octopamine-immunoreactive neurons were observed. The postembryonic increase in number of immunoreactive neurons and development of axonal arborization is accompanied by a rapid, exponential enhancement of octopamine content of Lymnaea CNS, as detected radioenzymatically. A possible role of the octopaminergic neurons in the regulation of certain physiological function(s), active only from a late stage of embryonic development, is suggested.

Animals↗

High-affinity antagonists of the locust neuronal octopamine receptor.

The pharmacological antagonistic properties of the invertebrate specific octopamine receptor were investigated using a conventional radio-receptor assay with [3H]octopamine as the radioligand. Among the antagonists with highest affinity of the locust (Locusta migratoria L.) neuronal octopamine receptor were tetracyclic substances like mianserin (K1 = 1.2 nM), some of its derivatives (8-hydroxymianserin; K1 = 1.68 nM), and maroxepine, which is the antagonist with the highest affinity ever reported (K1 = 1.02 nM) to this octopamine receptor class. Among the other antagonists tested only phentolamine (K1 = 19 nM) and promethazine (K1 = 31.2 nM) had high-affinity properties.

Animals↗

Second messengers of octopamine receptors in the snail Lymnaea.

We describe octopamine responses of 3 large buccal neurons of Lymnaea and test the hypothesis that these are cAMP-dependent. The B1 neuron is excited by octopamine and the depolarisation is significantly enlarged (P < 0.05) by application of the blocker of cAMP breakdown, 3-isobutyl-1-methylxanthine (IBMX). The B1 neuron is also depolarised by forskolin, an activator of adenylyl cyclase. The B2 and B3 neurons are inhibited by octopamine, and the response is not affected by IBMX. Both cells are excited by forskolin. We conclude that the B1 neuron response to octopamine is likely to be mediated by cAMP, while the B2 and B3 responses are cAMP-independent.

1-Methyl-3-isobutylxanthine↗

Cytoarchitecture of histamine-, dopamine-, serotonin- and octopamine-containing neurons in the cricket ventral nerve cord.

The present article provides a comparative neuroanatomical description of the cellular localization of the biogenic amines histamine, dopamine, serotonin and octopamine in the ventral nerve cord of an insect, namely the cricket, Gryllus bimaculatus. Generally, different immunocytochemical staining techniques reveal a small number of segmentally distributed immunoreactive (-IR) amine-containing neurons allowing single cell reconstruction of prominent elements. Aminergic neurons share common morphological features in that they innervate large portions of neurophil and often connect different neuromeres by intersegmental 'wide-field' projections of varicose appearance. In many cases aminergic terminals are also found on the surface of peripheral nerves suggesting additional neurohemal release sites. Despite such morphological similarities histological analysis demonstrates for any given amine functionally distinct neuron types with specific innervation patterns establishing discrete pathways. Histamine-IR interneurons are characterized by both ascending and descending projections forming central and peripheral terminals. The descending branches from dopamine-IR cells mainly converge within the terminal ganglion, whereas serotonin-IR interneurons with ascending projections often terminate within the brain. Serotonin is also present in sensory and motor neurons. In contrast to other aminergic neurons, most octopamine-IR cells represent unpaired neurons projecting through motor nerves of the soma-containing neuromere. Octopamine-IR cells with intersegmental branches are only rarely found. Based on these findings, a colocalization of different amines within the same neuron seems to be unlikely to occur in the cricket ventral nerve cord. With respect to the neuroanatomical description of amine-containing neurons known physiological effects of biogenic amines and their possible neuromodulatory functions in insects are discussed.

Animals↗

Octopamine in the locust brain: cellular distribution and functional significance in an arousal mechanism.

This review summarizes the distribution of octopamine-like immunoreactive neurons in the brain of the locust and the functional significance of a subset of them in an arousal mechanism in the visual system. A small set of identifiable octopamine-immunoreactive neurons lies in the ventromedial brain. Their cell bodies are large and readily accessible, which allows their removal and analysis of their biogenic amine content using gas-chromatography mass-spectrometry to confirm that they are genuinely octopaminergic. The neurons project from the central brain to the optic lobes where they arborize extensively in the medulla and lobula. There they release octopamine in response to multimodal input in the central brain. This evokes dishabitution in the locust's movement-detection system, suggesting an arousal mechanism.

Animals↗

Tyramine and octopamine: antagonistic modulators of behavior and metabolism.

The phenolamines tyramine and octopamine are decarboxylation products of the amino acid tyrosine. Although tyramine is the biological precursor of octopamine, both compounds are independent neurotransmitters, acting through various G-protein coupled receptors. Especially, octopamine modulates a plethora of behaviors, peripheral and sense organs. Both compounds are believed to be homologues of their vertebrate counterparts adrenaline and noradrenaline. They modulate behaviors and organs in a coordinated way, which allows the insects to respond to external stimuli with a fine tuned adequate response. As these two phenolamines are the only biogenic amines whose physiological significance is restricted to invertebrates, the attention of pharmacologists was focused on the corresponding receptors, which are still believed to represent promising targets for new insecticides. Recent progress made on all levels of octopamine/tyramine research enabled us to better understand the molecular events underlying the control of complex behaviors.

Animals↗

Evidence for the lack of a carrier effect in the solvent extraction and determination of octopamine by gas chromatography mass spectrometry.

It has been shown that there is no significant carrier effect when low levels of [3H]octopamine (100 pg) are extracted by ethyl acetate from aqueous solutions containing a 10(3) or 10(6) times excess of unlabelled octopamine. It is also shown that there is no carrier effect when low levels of octopamine as the tetrakis-TMS derivative are injected with 100 times the amount of the [2H3] analogue on an SE 30 column.

Chromatography, Gas↗

Octopamine: presence in firefly lantern suggests a transmitter role.

The lantern of the adult firefly is innervated by a nerve supply with endings similar to other known monoaminergic nerves. However, catecholamines could not be detected in the nerve endings and noradrenaline and adrenaline were relatively weak agonists in eliciting a flash of light when applied to the lantern in vitro. Firefly lanterns were assayed for octopamine using a sensitive, specific enzymatic assay in which octopamine is enzymatically converted to 3H-synephrine and quantitated by liquid scintillation counting. The presence of substantial amounts (125 ng/g tissue) of octopamine was demonstrated and confirmed by thin layer chromatography. On the basis of this and earlier work, it is suggested that the nerves to the firefly lantern are octopaminergic.

Animals↗

Biochemistry and ultrastructure of serotonergic nerve endings in the lobster: serotonin and octopamine are contained in different nerve endings.

In this article we report that the distribution of serotonin in the lobster nervous system parallels the distribution of octopamine and that the same tissues that contain endogenous serotonin can synthesize it from tryptophan. Octopamine and serotonin are highly concentrated in a neurosecretory region of the second thoracic roots in association with a group of neurosecretory cells. The roots possess separate high-affinity uptake systems for both serotonin and tryptophan. Radioactive serotonin, accumulated in tissues during incubations with either tritiated serotonin or tritiated tryptophan, can be released, in a calcium-dependent manner, by depolarization with potassium. A detailed morphological examination of the second thoracic roots shows four distinct categories of nerve endings in the vicinity of the neurosecretory cells. Octopamine is synthesized in one of these types of endings and serotonin in another. The high-affinity uptake systems for serotonin and tryptophan are found only in association with the endings that make serotonin. These endings and all the biochemical parameters of serotonin metabolism in the roots are selectively destroyed by previous injection of animals with the neurotoxin 5,7-dihydroxytryptamine.

Animals↗

Is octopamine a transmitter mediating hormone release in insects?

The release of hyperlipemic hormone from the glandular cells of the corpus cardiacum (CC) of Locusta migratoria is under the synaptic control of axons in nervus corpus cardiacum II (NCC II). The effects of aminergic agonists and antagonists on the release of the hyperlipemic hormone induced by electrical stimulation of NCC II have been examined. CC isolated from reserpine-injected locusts did not release hormone when subjected to electrical stimulation of NCC II but continued to release hormone in response to high-potassium saline. The electrically stimulated release of hormone from isolated CC was abolished by the alpha-adrenergic blocking agent, phenoxybenzamine, but potentiated by the beta-adrenergic blocking agent, propranolol. Phenoxybenzamine did not interfere with release induced by high-potassium saline. It is suggested that the postsynaptic receptors on the glandular cells are similar to the alpha-adrenergic receptors of vertebrates. Octopamine was found to be present in the glandular lobe of the CC at concentrations of 0.62 pmole per gland pair. Reserpine depleted the content to 0.3 pmole per pair. Bathing the CC in 10(-7) M octopamine resulted in the release of hyperlipemic hormone, and this release was blocked by phenoxybenzamine. It is concluded that the neurotransmitter involved in the synapse between axons of NCC II and the cells releasing hyperlipemic hormone is aminergic, possibly octopaminergic. Octopamine may well be a transmitter mediating hormone release in insects.

Animals↗

Octopamine and chlordimeform enhance sensory responsiveness and production of the flight motor pattern in developing and adult moths.

Octopamine and an agonist, chlordimeform, increase the responsiveness of adult and pharate adult Manduca sexta to gentle mechanical stimulation of the wing. Higher doses of chlordimeform elicit almost continuous production of the flight motor pattern in both adults and pharate adults, and the effect persists for more than 24 h. The dose of chlordimeform necessary for this effect increases with age. Mechanical stimulation of the wing of pharate adults elicits several cycles of flight motor pattern, but with repeated stimulation the animal habituates. Habituation is slower in chlordimeform-treated animals than in controls. Injection of octopamine (1-8 X 10(-8) mol) or chlordimeform (3 X 10(-9) mol) into the mesothoracic ganglion elicits the flight motor pattern. The excitatory actions of both compounds can be blocked by cyproheptidine. Chlordimeform (5 X 10(-8) mol) in acetone applied to the wing does not cause a noticeably greater increase in teh electrical activity of sensory neurons than does acetone applied alone; this result suggests that chlordimeform does not act on these peripheral sites or on axonal membranes in general. We suggest that chlordimeform and octopamine act on the thoracic ganglia to alter the level of excitation or effectiveness of synaptic transmission among central neurons, including those involved in producing the flight motor pattern.

Amidines↗

Octopamine mediates rapid stimulation of protein kinase A in the antennal lobe of honeybees.

In the honeybee octopamine mediates mechanisms of arousal that interfere with the appetitive proboscis extension response to food-indicating chemosensory stimuli. This study demonstrates that injections of octopamine or cyclic adenosine monophosphate (cAMP) into the primary chemosensory neuropil of the honeybee, the antennal lobe, evokes a rapid and transient activation of cAMP-dependent protein kinase (PKA). Other monoamines detectable in the antennal lobe, dopamine and serotonin, do not affect the level of PKA activity. Stimulation of the bees' antenna with the appetitive stimulus water or sucrose solution in vivo also causes a short-term activation of PKA in the antennal lobe. The increased PKA activity can be detected immediately (0.5 s) after stimulation but reverts to the basal level within 3 s. This effect can be abolished by monoamine depletion with reserpine. Since octopamine is the only monoamine that stimulates PKA, it appears to mediate the PKA activation after sucrose stimulus and may contribute to the processing of this chemosensory input.

Animals↗

Histochemical localization of octopamine- and proctolin-sensitive adenylate cyclase activity in a locust skeletal muscle.

A histochemical technique for the localization of adenylate cyclase activity has been applied to the extensor-tibiae muscle of the hindleg of the locust, Schistocerca gregaria to localise the sites of action of the modulatory compounds octopamine and proctolin. Octopamine-sensitive adenylate cyclase activity can be demonstrated in fast and intermediate type muscle fibres but not in the limited number of purely slow muscle fibres (3-6) in the fan region at the proximal end of the muscle. In contrast the latter fibres are the only ones in the muscle to exhibit proctolin-sensitive adenylate cyclase activity. In both cases the bulk of the reaction product is localised in the sarcoplasmic reticulum component of the dyads, with lesser amounts occurring beneath the sarcolemmal membrane, in the non-dyad sarcoplasmic reticulum and in the T-tubule system. The results are consistent with physiological data suggesting that proctolin, but not octopamine, mediates its effects on the myogenic rhythm of contraction and relaxation in this muscle by changing the levels of cyclic AMP in the small group of slow muscle fibres which act as the pacemaker for this rhythm.

Adenylyl Cyclases↗

Bioavailability of m-octopamine in man related to its metabolism.

The diminished sympathomimetic pressor activity of monohydroxylated phenylalkylamines after oral administration has been attributed to incomplete enteric absorption. Therefore, urinary excretion of the unchanged drug and its metabolites has been compared after intravenous and oral administration of 3H-m-octopamine to eight patients. Identical amounts of 3H-activity (80% of the dose) were excreted after the two routes of dosing, so enteric absorption has been assumed to be complete. Significant differences were found in the fraction of free urinary m-octopamine, which amounted to 10.5% of the dose after infusion and 0.58% after oral administration. The only metabolic pathways for m-octopamine are deamination and conjugation. Following oral administration the percentage of conjugates was considerably higher than after intravenous infusion. This metabolic pattern appears typical of all phenylalkylamines with a hydroxyl group in the meta position. Ring hydroxylation to catecholamines was not observed. The enzymes mainly responsible for conjugation after oral administration are located in the gut wall. The resulting ""first pass effect'', i.e. metabolism prior to the access to the central compartment, can account for the diminished pharmacodynamic effect after dosing by this route.

Administration, Oral↗