WordNet
- (biochemistry) a drug that can combine with a receptor on a cell to produce a physiological reaction
- a muscle that contracts while another relaxes; "when bending the elbow the biceps are the agonist"
- someone involved in a contest or battle (as in an agon)
- releasing or activated by acetylcholine or a related compound
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- 1. 陣痛および分娩に対する硬膜外・脊椎麻酔：薬 neuraxial analgesia and anesthesia for labor and delivery drugs
- 2. 寝汗がみられる患者に対するアプローチ approach to the patient with night sweats
- 3. 頭頸部癌の初期治療中の合併症のマネージメントおよび予防 management and prevention of complications during initial treatment of head and neck cancer
- 4. シェーグレン症候群における口内乾燥およびその他の非眼結膜炎症状の治療 treatment of dry mouth and other non ocular sicca symptoms in sjogrens syndrome
- 5. 重症筋無力症の病因 pathogenesis of myasthenia gravis
English Journal
- The actions of Pasteurella multocida toxin on neuronal cells.
- Surguy SM1, Duricki DA1, Reilly JM2, Lax AJ3, Robbins J4.Author information 1Wolfson Centre for Age Related Diseases, King's College London, Guy's Campus, London SE1 1UL, UK.2Neuroscience, Physiology and Pharmacology, University College London, London WC1E 6BT, UK.3Department of Microbiology, Dental Institute, King's College London, Guy's Campus, London SE1 1UL, UK.4Wolfson Centre for Age Related Diseases, King's College London, Guy's Campus, London SE1 1UL, UK. Electronic address: jon.robbins@kcl.ac.uk.AbstractPasteurella multocida toxin (PMT) activates the G-proteins Gαi(1-3), Gαq, Gα11, Gα12 and Gα13 by deamidation of specific glutamine residues. A number of these alpha subunits have signalling roles in neurones. Hence we studied the action of this toxin on rat superior cervical ganglion (SCG) neurones and NG108-15 neuronal cells. Both Gαq and Gα11 could be identified in SCGs with immunocytochemistry. PMT had no direct action on Kv7 or Cav2 channels in SCGs. However PMT treatment enhanced muscarinic receptor mediated inhibition of M-current (Kv7.2 + 7. 3) as measured by a 19-fold leftward shift in the oxotremorine-M concentration-inhibition curve. Agonists of other receptors, such as bradykinin or angiotensin, that inhibit M-current did not produce this effect. However the amount of PIP2 hydrolysis could be enhanced by PMT for all three agonists. In a transduction system in SCGs that is unlikely to be affected by PMT, Go mediated inhibition of calcium current, PMT was ineffective whereas the response was blocked by pertussis toxin as expected. M1 muscarinic receptor evoked calcium mobilisation in transformed NG108-15 cells was enhanced by PMT. The calcium rises evoked by uridine triphosphate acting on endogenous P2Y2 receptors in NG108-15 cells were enhanced by PMT. The time and concentration dependence of the PMT effect was different for the resting calcium compared to the calcium rise produced by activation of P2Y2 receptors. PMT's action on these neuronal cells would suggest that if it got into the brain, symptoms of a hyperexcitable nature would be seen, such as seizures.
- Neuropharmacology.Neuropharmacology.2014 Feb;77:9-18. doi: 10.1016/j.neuropharm.2013.09.005. Epub 2013 Sep 18.
- Pasteurella multocida toxin (PMT) activates the G-proteins Gαi(1-3), Gαq, Gα11, Gα12 and Gα13 by deamidation of specific glutamine residues. A number of these alpha subunits have signalling roles in neurones. Hence we studied the action of this toxin on rat superior cervical ganglion (SCG) neur
- PMID 24055502
- GABAA receptors are located in cholinergic terminals in the nucleus pontis oralis of the rat: Implications for REM sleep control.
- Liang CL1, Marks GA2.Author information 1Department of Veterans Affairs, North Texas Health Care System, Dallas, TX 75216, USA; Department of Psychiatry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA.2Department of Veterans Affairs, North Texas Health Care System, Dallas, TX 75216, USA; Department of Psychiatry, University of Texas Southwestern Medical Center, Dallas, TX 75390, USA. Electronic address: gerald.marks@utsouthwestern.edu.AbstractThe oral pontine reticular formation (PnO) of rat is one region identified in the brainstem as a rapid eye movement (REM) sleep induction zone. Microinjection of GABAA receptor antagonists into PnO induces a long lasting increase in REM sleep, which is similar to that produced by cholinergic agonists. We previously showed that this REM sleep-induction can be completely blocked by a muscarinic antagonist, indicating that the REM sleep-inducing effect of GABAA receptor antagonism is dependent upon the local cholinergic system. Consistent with these findings, it has been reported that GABAA receptor antagonists microdialyzed into PnO resulted in increased levels of acetylcholine. We hypothesize that GABAA receptors located on cholinergic boutons in the PnO are responsible for the REM sleep induction by GABAA receptor antagonists through blocking GABA inhibition of acetylcholine release. Cholinergic, varicose axon fibers were studied in the PnO by immunofluorescence and confocal, laser scanning microscopy. Immunoreactive cholinergic boutons were found to be colocalized with GABAA receptor subunit protein γ2. This finding implicates a specific subtype and location of GABAA receptors in PnO of rat in the control of REM sleep.
- Brain research.Brain Res.2014 Jan 16;1543:58-64. doi: 10.1016/j.brainres.2013.10.019. Epub 2013 Oct 17.
- The oral pontine reticular formation (PnO) of rat is one region identified in the brainstem as a rapid eye movement (REM) sleep induction zone. Microinjection of GABAA receptor antagonists into PnO induces a long lasting increase in REM sleep, which is similar to that produced by cholinergic agonist
- PMID 24141149
- Metoclopramide does not increase gastric muscle contractility in newborn rats.
- Kasirer MY, Welsh C, Pan J, Shifrin Y, Belik J.Author information 1The Hospital for Sick Children.AbstractFeeding intolerance resulting from delayed gastric emptying is common in premature neonates. Metoclopramide (MCP), the most frequently used prokinetic drug in neonates, enhances gastric muscle contractility through inhibition of dopamine receptors. Although its therapeutic benefit is established in adults, limited data are available to support its clinical use in infants. Hypothesizing that developmentally-dependent differences are present, we comparatively evaluated the effect of MCP on fundus muscle contractility in newborn, juvenile and adult rats. The muscle strips were either contracted with electrical field stimulation (EFS) to induce cholinergic nerve-mediated acetylcholine release or carbachol, a cholinergic agonist acting directly on the muscarinic receptor. Although in adult rats MCP increased EFS induced contraction by 294±122% of control (P<0.01), no significant effect was observed in newborn fundic muscle. MCP had no effect on the magnitude of the carbachol-induced and/or bethanechol-induced gastric muscle contraction at any age. In response to dopamine, a 80.7± 5.3% relaxation of adult fundic muscle was observed, as compared with only a 8.4 ± 8.7%, response in newborn tissue (P<0.01). Dopamine D2 receptor expression was scant in neonates and significantly increased in adult gastric tissue (P<0.01). In conclusion the lack of MCP effect on the newborn fundic muscle contraction potential relates to developmental differences in dopamine D2 receptor expression. To the extent that this novel data can be extrapolated to neonates, the therapeutic value of MCP as a prokinetic agent early in life requires further evaluation.
- American journal of physiology. Gastrointestinal and liver physiology.Am J Physiol Gastrointest Liver Physiol.2014 Jan 9. [Epub ahead of print]
- Feeding intolerance resulting from delayed gastric emptying is common in premature neonates. Metoclopramide (MCP), the most frequently used prokinetic drug in neonates, enhances gastric muscle contractility through inhibition of dopamine receptors. Although its therapeutic benefit is established in
- PMID 24407589
Japanese Journal
- Selective M3 Muscarinic Receptor Antagonist Inhibits Small-Cell Lung Carcinoma Growth in a Mouse Orthotopic Xenograft Model
- Ami Nozomi,Koga Kazumi,Fushiki Hiroshi,Ueno Yoko,Ogino Yoshio,Ohta Hisashi
- Journal of Pharmacological Sciences 116(1), 81-88, 2011
- … In small cell lung carcinoma (SCLC), acetylcholine (ACh) is synthesized and secreted, and it acts as an autocrine growth factor through activation of its receptors, muscarinic receptor (mAChR) and nicotinic receptor (nAChR). … We used a highly selective M3 muscarinic antagonist, N-(2-[3-([3R]-1-(cyclohexylmethyl)-3-piperidinyl]methylamino)-3-oxopropyl]amino-2-oxoethyl)-3,3,3-triphenyl-propioamide (J-115311). …
- NAID 130000663531
- Histamine Develops Homologous Desensitization under Ca2+-free Conditions with Increase in Basal Tone in Smooth Muscle of Guinea Pig Taenia Caeci
- 菱沼 滋,庄司 優
- YAKUGAKU ZASSHI 130(3), 451-455, 2010
- … In contrast, histamine treatment reduced EC50 values for a muscarinic agonist, carbachol, and depolarizing high K+. … These results suggest that the failure of excess histamine to induce a normal Ca2+ response under Ca2+-free conditions may lead to homologous desensitization to histamine with apparent hyper-reactivity of smooth muscles to cholinergic and depolarizing stimuli. …
- NAID 130000259529
Related Links
- Definition: Drugs that bind to and activate muscarinic cholinergic receptors (RECEPTORS, MUSCARINIC). Muscarinic agonists are most commonly used when it is desirable to increase smooth muscle tone, especially in the GI tract ...
- Acetyicholine is a physiological neurotransmitter which acts on both muscarinic and nicotinic receptors. It is not useful as a drug being non-specific and
Related Pictures
★リンクテーブル★
| リンク元 | 「muscarinic agonist」「ムスカリン受容体刺激薬」「ムスカリン作動薬」「muscarinic receptor agonist」 |
| 関連記事 | 「muscarinic」「cholinergic agonist」「cholinergic」 |
「muscarinic agonist」
「ムスカリン受容体刺激薬」
- 英
- muscarinic agonist、muscarinic receptor agonist、muscarinic cholinergic agonist
- 関
- ムスカリン作動薬、ムスカリン作用薬、ムスカリンアゴニスト
「ムスカリン作動薬」
「muscarinic receptor agonist」
「muscarinic」
- adj.
- ムスカリン性の、ムスカリンの
- n.
- 関
- cholinergic、cholinergic agent、cholinergic drug、cholinomimetic、muscarine、muscarinic agent、muscarinic agonist
「cholinergic agonist」
「cholinergic」
- adj.
- コリン作動性の