Interactions between the presynaptic alpha2-autoreceptor and presynaptic inhibitory heteroreceptors on noradrenergic neurones. 1998

E Schlicker, and M Göthert
Institut für Pharmakologie und Toxikologie, Rheinische Friedrich-Wilhelms-Universität Bonn, Germany.

The noradrenergic neurones of the autonomic nervous system (postganglionic sympathetic neurones) and of the central nervous system are endowed with presynaptic receptors by which noradrenaline release is inhibited by noradrenaline itself (via the alpha2-autoreceptor) and by other transmitters and mediators (via heteroreceptors). Frequently, but not consistently, inhibitory interactions exist between auto- and heteroreceptors. This holds true for the following heteroreceptors: adenosine A1, cannabinoid CB1, dopamine D2/D3, histamine H3, 5-hydroxytryptamine (serotonin) 5-HT(1B), imidazoline, muscarine M2, delta opioid, kappa opioid, mu opioid, orphan opioid (ORL1), prostaglandin EP3, and somatostatin SRIF1. Such interactions (which have also been obtained in human tissue) may, if not considered, prevent the identification of a putative heteroreceptor or the quantitative estimation of the effect mediated by this receptor, and they may explain drug interactions in humans in vivo; many ligands at the alpha2-autoreceptor and at the heteroreceptors may be simultaneously used for therapeutic reasons (e.g., carbachol, clonidine, dopamine, sumatriptan, mianserin, and misoprostol) or abused (e.g., heroin, LSD, and delta9-tetrahydrocannabinol in hashish or marijuana).

UI MeSH Term Description Entries
D009433 Neural Inhibition The function of opposing or restraining the excitation of neurons or their target excitable cells. Inhibition, Neural
D009474 Neurons The basic cellular units of nervous tissue. Each neuron consists of a body, an axon, and dendrites. Their purpose is to receive, conduct, and transmit impulses in the NERVOUS SYSTEM. Nerve Cells,Cell, Nerve,Cells, Nerve,Nerve Cell,Neuron
D009638 Norepinephrine Precursor of epinephrine that is secreted by the ADRENAL MEDULLA and is a widespread central and autonomic neurotransmitter. Norepinephrine is the principal transmitter of most postganglionic sympathetic fibers, and of the diffuse projection system in the brain that arises from the LOCUS CERULEUS. It is also found in plants and is used pharmacologically as a sympathomimetic. Levarterenol,Levonorepinephrine,Noradrenaline,Arterenol,Levonor,Levophed,Levophed Bitartrate,Noradrenaline Bitartrate,Noradrénaline tartrate renaudin,Norepinephrin d-Tartrate (1:1),Norepinephrine Bitartrate,Norepinephrine Hydrochloride,Norepinephrine Hydrochloride, (+)-Isomer,Norepinephrine Hydrochloride, (+,-)-Isomer,Norepinephrine d-Tartrate (1:1),Norepinephrine l-Tartrate (1:1),Norepinephrine l-Tartrate (1:1), (+,-)-Isomer,Norepinephrine l-Tartrate (1:1), Monohydrate,Norepinephrine l-Tartrate (1:1), Monohydrate, (+)-Isomer,Norepinephrine l-Tartrate (1:2),Norepinephrine l-Tartrate, (+)-Isomer,Norepinephrine, (+)-Isomer,Norepinephrine, (+,-)-Isomer
D006801 Humans Members of the species Homo sapiens. Homo sapiens,Man (Taxonomy),Human,Man, Modern,Modern Man
D000818 Animals Unicellular or multicellular, heterotrophic organisms, that have sensation and the power of voluntary movement. Under the older five kingdom paradigm, Animalia was one of the kingdoms. Under the modern three domain model, Animalia represents one of the many groups in the domain EUKARYOTA. Animal,Metazoa,Animalia
D017660 Autoreceptors Transmitter receptors on or near presynaptic terminals (or varicosities) which are sensitive to the transmitter(s) released by the terminal itself. Receptors for the hormones released by hormone-releasing cells are also included. Autoreceptor
D017729 Presynaptic Terminals The distal terminations of axons which are specialized for the release of neurotransmitters. Also included are varicosities along the course of axons which have similar specializations and also release transmitters. Presynaptic terminals in both the central and peripheral nervous systems are included. Axon Terminals,Nerve Endings, Presynaptic,Synaptic Boutons,Synaptic Terminals,Axon Terminal,Bouton, Synaptic,Boutons, Synaptic,Ending, Presynaptic Nerve,Endings, Presynaptic Nerve,Nerve Ending, Presynaptic,Presynaptic Nerve Ending,Presynaptic Nerve Endings,Presynaptic Terminal,Synaptic Bouton,Synaptic Terminal,Terminal, Axon,Terminal, Presynaptic,Terminal, Synaptic,Terminals, Axon,Terminals, Presynaptic,Terminals, Synaptic
D017981 Receptors, Neurotransmitter Cell surface receptors that bind signalling molecules released by neurons and convert these signals into intracellular changes influencing the behavior of cells. Neurotransmitter is used here in its most general sense, including not only messengers that act to regulate ion channels, but also those which act on second messenger systems and those which may act at a distance from their release sites. Included are receptors for neuromodulators, neuroregulators, neuromediators, and neurohumors, whether or not located at synapses. Neurohumor Receptors,Neuromediator Receptors,Neuromodulator Receptors,Neuroregulator Receptors,Receptors, Neurohumor,Receptors, Synaptic,Synaptic Receptor,Synaptic Receptors,Neuromediator Receptor,Neuromodulator Receptor,Neuroregulator Receptor,Neurotransmitter Receptor,Receptors, Neuromediators,Receptors, Neuromodulators,Receptors, Neuroregulators,Receptors, Neurotransmitters,Neuromediators Receptors,Neuromodulators Receptors,Neuroregulators Receptors,Neurotransmitter Receptors,Neurotransmitters Receptors,Receptor, Neuromediator,Receptor, Neuromodulator,Receptor, Neuroregulator,Receptor, Neurotransmitter,Receptor, Synaptic,Receptors, Neuromediator,Receptors, Neuromodulator,Receptors, Neuroregulator
D020239 Receptor Cross-Talk The simultaneous or sequential binding of multiple cell surface receptors to different ligands resulting in coordinated stimulation or suppression of signal transduction. Receptor Cross Talk,Cross Talk, Receptor,Cross-Talk, Receptor

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