代謝型受容体、代謝型レセプター

WordNet

a cellular structure that is postulated to exist in order to mediate between a chemical agent that acts on nervous tissue and the physiological response

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=sense organ / 受信装置

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出典(authority):フリー百科事典『ウィキペディア（Wikipedia）』「2013/03/24 14:19:02」(JST)

wiki en

A metabotropic receptor is a type of membrane receptors of eukaryotic cells that acts through a secondary messenger. It may be located at the surface of the cell or in vesicles.

Based on their structural and functional characteristics, neurotransmitter receptors can be classified into two broad categories: metabotropic and ionotropic receptors. Ionotropic receptors form an ion channel pore. In contrast, metabotropic receptors are indirectly linked with ion channels on the plasma membrane of the cell through signal transduction mechanisms, often G proteins. Hence, G protein-coupled receptors are inherently metabotropic. Other examples of metabotropic receptors include tyrosine kinases or guanylyl cyclase receptors.

Both receptor types are activated by specific neurotransmitters. When an ionotropic receptor is activated, it opens a channel that allows ions such as Na⁺, K⁺, or Cl^- to flow. In contrast, when a metabotropic receptor is activated, a series of intracellular events are triggered that can also result in ion channels opening but must involve a range of second messenger chemicals.

Examples

This class of receptors includes the metabotropic glutamate receptors, muscarinic acetylcholine receptors, GABA_B receptors, and most serotonin receptors, as well as receptors for norepinephrine, epinephrine, histamine, dopamine, neuropeptides^[1]^[2] and endocannabinoids.

Structure

The G protein-coupled receptors have seven hydrophobic transmembrane domains. Most of them are monomeric proteins, although GABA_B receptors require heterodimerization to function properly. The protein's N terminus is located on the extracellular side of the membrane and its C terminus is on the intracellular side.^[2]

The 7 transmembrane spanning domains, with an external amino terminus, is often claimed as being alpha helix shaped, and the polypeptide chain is said to be composed of ~ 450-550 amino acids.

Function

Metabotropic receptors have neurotransmitters as ligands, which, when bound to the receptors, initiate cascades that can lead to channel-opening or other cellular effects. When a ligand (the neurotransmitter) binds to the receptor (the transducer) the latter activates a primary effector via the G-protein, which can go on to activate secondary messengers or have other effects. Since opening channels by metabotropic receptors involves activating a number of molecules in turn, channels associated with these receptors take longer to open than ionotropic receptors do, and they are thus not involved in mechanisms that require quick responses.^[3]^:240 However, metabotropic receptors also remain open from seconds to minutes.^[3]^:250–1 Thus they have a much longer-lasting effect than ionotropic receptors, which open quickly but only remain open for a few milliseconds.^[1] While ionotropic channels have an effect only in the immediate region of the receptor, the effects of metabotropic receptors can be more widespread through the cell.

Metabotropic receptors can both open and close channels. They can make a membrane more excitable by closing K⁺ channels, retaining positive charge within the cell and thus reducing the amount of current necessary to cause an action potential.^[3]^:242–3 Metabotropic receptors on the presynaptic membrane can inhibit or, more rarely, facilitate neurotransmitter release from the presynaptic neuron.^[4] These receptors can be further classified into receptor tyrosine kinases and G protein-coupled receptors, or GPCRs.^[3]^:229

References

^ ^a ^b Hoehn K, Marieb EN (2007). "Fundamentals of the nervous system and nervous". Human Anatomy & Physiology. San Francisco: Pearson Benjamin Cummings. ISBN 0-8053-5910-9. http://wps.aw.com/bc_marieb_happlace_7_oa/42/10967/2807754.cw/index.html.
^ ^a ^b Williams, S. J.; Purves, Dale (2001). Neuroscience. Sunderland, Mass: Sinauer Associates. ISBN 0-87893-742-0.
^ ^a ^b ^c ^d Jessell TM, Kandel ER, Schwartz JH (2000). Principles of Neural Science. New York: McGraw-Hill. ISBN 0-8385-7701-6.
^ Schmitz D, Mellor J, Nicoll RA (March 2001). "Presynaptic kainate receptor mediation of frequency facilitation at hippocampal mossy fiber synapses". Science 291 (5510): 1972–6. doi:10.1126/science.1057105. PMID 11239159.

UpToDate Contents

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English Journal

Regulation of mGluR7 trafficking by SUMOylation in neurons.

Choi JH1, Park JY1, Park SP2, Lee H2, Han S2, Park KH1, Suh YH3.
Neuropharmacology.Neuropharmacology.2016 Mar;102:229-35. doi: 10.1016/j.neuropharm.2015.11.021. Epub 2015 Nov 26.
SUMOylation is a post-translational modification by which Small Ubiquitin-like MOdifier (SUMO) proteins are covalently linked to the lysine residues of target proteins via an enzymatic cascade. SUMOylation at the synapse plays an important regulatory role in a wide variety of neuronal function such
PMID 26631532

Allosteric modulation of metabotropic glutamate receptor 4 activates IDO1-dependent, immunoregulatory signaling in dendritic cells.

Volpi C1, Mondanelli G1, Pallotta MT1, Vacca C1, Iacono A1, Gargaro M1, Albini E1, Bianchi R1, Belladonna ML1, Celanire S2, Mordant C2, Heroux M2, Royer-Urios I2, Schneider M2, Vitte PA2, Cacquevel M2, Galibert L2, Poli SM2, Solari A3, Bicciato S4, Calvitti M1, Antognelli C1, Puccetti P1, Orabona C1, Fallarino F1, Grohmann U5.
Neuropharmacology.Neuropharmacology.2016 Mar;102:59-71. doi: 10.1016/j.neuropharm.2015.10.036. Epub 2015 Oct 30.
Metabotropic glutamate receptor 4 (mGluR4) possesses immune modulatory properties in vivo, such that a positive allosteric modulator (PAM) of the receptor confers protection on mice with relapsing-remitting experimental autoimmune encephalomyelitis (RR-EAE). ADX88178 is a newly-developed, one such
PMID 26522434

Influence of MPEP (a selective mGluR5 antagonist) on the anticonvulsant action of novel antiepileptic drugs against maximal electroshock-induced seizures in mice.

Zolkowska D1, Kondrat-Wrobel MW2, Florek-Luszczki M3, Luszczki JJ4.
Progress in neuro-psychopharmacology & biological psychiatry.Prog Neuropsychopharmacol Biol Psychiatry.2016 Feb 4;65:172-8. doi: 10.1016/j.pnpbp.2015.10.005. Epub 2015 Oct 21.
The aim of this study was to determine the effects of 2-methyl-6-(phenylethynyl)pyridine (MPEP - a selective antagonist for the glutamate metabotropic receptor subtype mGluR5) on the protective action of some novel antiepileptic drugs (lamotrigine, oxcarbazepine, pregabalin and topiramate) against m
PMID 26478256

Japanese Journal

Intracellular calcium level is an important factor influencing ion channel modulations by PLC-coupled metabotropic receptors in hippocampal neurons

Sugawara Yuto,Echigo Ryousuke,Kashima Kousuke,Minami Hanae,Watanabe Megumi,Nishikawa Yuiko,Muranishi Miho,Yoneda Mitsugu,Ohno-Shosaku Takako
Brain Research 1512, 9-21, 2013-00-00
… Previous studies demonstrated that receptor-driven PLCβ activation depends on intracellular Ca2+ concentration ([Ca2+]i), suggesting the possibility that PLCβ-dependent cellular responses are basically Ca 2+ dependent. … To test this possibility, we examined whether modulations of ion channels driven by PLC-coupled metabotropic receptors are sensitive to [Ca2+]i using cultured hippocampal neurons. …
NAID 120005302294

Stimulation of Metabotropic Glutamate (mGlu) 2 Receptor and Blockade of mGlu1 Receptor Improve Social Memory Impairment Elicited by MK-801 in Rats

Hikichi Hirohiko,Kaku Ayaka,Karasawa Jun-ichi,Chaki Shigeyuki
Journal of Pharmacological Sciences, 2013
… Both the stimulation of the metabotropic glutamate (mGlu) 2/3 receptor and the blockade of the mGlu1 receptor have been shown to be effective in a number of animal models of schizophrenia. … The present study evaluated the effects of an mGlu2/3-receptor agonist and an mGlu1-receptor antagonist on social memory impairment in rats. …
NAID 130003362702

グループII代謝型グルタミン酸受容体をターゲットとした新規統合失調症治療薬の創製

日吉哲明,茶木茂之,奥山茂
日本薬理學雜誌 = Folia pharmacologica Japonica 140(3), 111-115, 2012-09-01
NAID 10031072050

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