serotonin uptake inhibitor

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5-HT uptake inhibitorserotonin reuptake inhibitor

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出典(authority):フリー百科事典『ウィキペディア(Wikipedia)』「2013/01/27 21:27:53」(JST)

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英文文献

  • Behavioural and transcriptional changes in the amphipod Echinogammarus marinus exposed to two antidepressants, fluoxetine and sertraline.
  • Bossus MC1, Guler YZ1, Short SJ1, Morrison ER2, Ford AT3.Author information 1Institute of Marine Sciences, School of Biological Sciences, University of Portsmouth, Ferry Road, Portsmouth, Hampshire PO4 9LY, UK.2Higher Education Academy Psychology, Department of Psychology, University of Portsmouth, Hampshire PO1 2DY, UK.3Institute of Marine Sciences, School of Biological Sciences, University of Portsmouth, Ferry Road, Portsmouth, Hampshire PO4 9LY, UK. Electronic address: alex.ford@port.ac.uk.AbstractIn the past decade, there have been increasing concerns over the effects of pharmaceutical compounds in the aquatic environment, however very little is known about the effects of antidepressants such as the selective serotonin re-uptake inhibitors (SSRIs). Many biological functions within invertebrates are under the control of serotonin, such as reproduction, metabolism, moulting and behaviour. The effects of serotonin and fluoxetine have recently been shown to alter the behaviour of the marine amphipod, Echinogammarus marinus (Leach, 1815). The purpose of this study was to observe behavioural and transcriptional modifications in this crustacean exposed to the two most prescribed SSRIs (fluoxetine and sertraline) and to develop biomarkers of neurological endocrine disruption. The animals were exposed to both drugs at environmentally relevant concentrations from 0.001 to 1μg/L during short-term (1h and 1day) and medium-term (8 days) experiments. The movement of the amphipods was tracked using the behavioural analysis software during 12min alternating dark/light conditions. The behavioural analysis revealed a significant effect on velocity which was observed after 1h exposure to sertraline at 0.01μg/L and after 1 day exposure to fluoxetine as low as 0.001μg/L. The most predominant effect of drugs on velocity was recorded after 1 day exposure for the 0.1 and 0.01μg/L concentrations of fluoxetine and sertraline, respectively. Subsequently, the expression (in this article gene expression is taken to represent only transcription, although it is acknowledged that gene expression can also be regulated at translation, mRNA and protein stability levels) of several E. marinus neurological genes, potentially involved in the serotonin metabolic pathway or behaviour regulation, were analysed in animals exposed to various SSRIs concentrations using RT-qPCR. The expression of a tryptophan hydroxylase (Ph), a neurocan core protein (Neuc), a Rhodopsin (Rhod1) and an Arrestin (Arr) were measured following exposure to fluoxetine or sertraline for 8 days. The levels of Neuc, Rhod1 and Arr were significantly down-regulated to approximately 0.5-, 0.29- and 0.46-fold, respectively, for the lower concentrations of fluoxetine suggesting potential changes in the phototransduction pathway. The expression of Rhod1 tended to be up-regulated for the lower concentration of sertraline but not significantly. In summary, fluoxetine and sertraline have a significant impact on the behaviour and neurophysiology of this amphipod at environmentally relevant concentrations with effects observed after relatively short periods of time.
  • Aquatic toxicology (Amsterdam, Netherlands).Aquat Toxicol.2014 Jun;151:46-56. doi: 10.1016/j.aquatox.2013.11.025. Epub 2013 Dec 12.
  • In the past decade, there have been increasing concerns over the effects of pharmaceutical compounds in the aquatic environment, however very little is known about the effects of antidepressants such as the selective serotonin re-uptake inhibitors (SSRIs). Many biological functions within invertebra
  • PMID 24373616
  • An exploratory investigation of various modes of action and potential adverse outcomes of fluoxetine in marine mussels.
  • Franzellitti S1, Buratti S2, Capolupo M2, Du B3, Haddad SP3, Chambliss CK4, Brooks BW3, Fabbri E5.Author information 1University of Bologna, Interdepartment Centre for Environmental Science Research, via S. Alberto 163, 48123 Ravenna, Italy; University of Bologna, Department of Biological, Geological, and Environmental Sciences, via Selmi 3, 40100 Bologna, Italy. Electronic address: silvia.franzellitti@unibo.it.2University of Bologna, Interdepartment Centre for Environmental Science Research, via S. Alberto 163, 48123 Ravenna, Italy.3Department of Environmental Science, Baylor University, Waco, TX 76798, USA.4Department of Chemistry and Biochemistry, Baylor University, Waco, TX 76798, USA.5University of Bologna, Interdepartment Centre for Environmental Science Research, via S. Alberto 163, 48123 Ravenna, Italy; University of Bologna, Department of Biological, Geological, and Environmental Sciences, via Selmi 3, 40100 Bologna, Italy.AbstractThe present study investigated possible adverse outcome pathways (AOPs) of the antidepressant fluoxetine (FX) in the marine mussel Mytilus galloprovincialis. An evaluation of molecular endpoints involved in modes of action (MOAs) of FX and biomarkers for sub-lethal toxicity were explored in mussels after a 7-day administration of nominal FX concentrations encompassing a range of environmentally relevant values (0.03-300ng/L). FX bioaccumulated in mussel tissues after treatment with 30 and 300ng/L FX, resulting in bioconcentration factor (BCF) values ranging from 200 to 800, which were higher than expected based solely on hydrophobic partitioning models. Because FX acts as a selective serotonin (5-HT) re-uptake inhibitor increasing serotonergic neurotransmission at mammalian synapses, cell signaling alterations triggered by 5-HT receptor occupations were assessed. cAMP levels and PKA activities were decreased in digestive gland and mantle/gonads of FX-treated mussels, consistent with an increased occupation of 5-HT1 receptors negatively coupled to the cAMP/PKA pathway. mRNA levels of a ABCB gene encoding the P-glycoprotein were also significantly down-regulated. This membrane transporter acts in detoxification towards xenobiotics and in altering pharmacokinetics of antidepressants; moreover, it is under a cAMP/PKA transcriptional regulation in mussels. Potential stress effects of FX were investigated using a battery of biomarkers for mussel health status that included lysosomal parameters, antioxidant enzyme activities, lipid peroxidation, and acetylcholinesterase activity. FX reduced the health status of mussels and induced lysosomal alterations, as suggested by reduction of lysosomal membrane stability in haemocytes and by lysosomal accumulation of neutral lipids in digestive gland. No clear antioxidant responses to FX were detected in digestive gland, while gills displayed significant increases of catalase and glutathione-s-transferase activities and a significant decrease of acetylcholinesterase activity. Though AOPs associated with mammalian therapeutic MOAs remain important during assessments of pharmaceutical hazards in the environment, this study highlights the importance of considering additional MOAs and AOPs for FX, particularly in marine mussels.
  • Aquatic toxicology (Amsterdam, Netherlands).Aquat Toxicol.2014 Jun;151:14-26. doi: 10.1016/j.aquatox.2013.11.016. Epub 2013 Dec 7.
  • The present study investigated possible adverse outcome pathways (AOPs) of the antidepressant fluoxetine (FX) in the marine mussel Mytilus galloprovincialis. An evaluation of molecular endpoints involved in modes of action (MOAs) of FX and biomarkers for sub-lethal toxicity were explored in mussels
  • PMID 24361074
  • Design of novel multiple-acting ligands towards SERT and 5-HT2C receptors.
  • Eliás O1, Agai-Csongor E2, Domány G2, Keserű GM2, Gere A2, Kiss B2, Hellinger E2, Vastag M2, Gyertyán I2.Author information 1Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary. Electronic address: elias@richter.hu.2Gedeon Richter Plc, Budapest 10, PO Box 27, H-1475, Hungary.AbstractThis Letter describes our attempts to elaborate dually acting compounds possessing serotonin re-uptake transporter inhibitor and serotonin 5-HT2C receptor antagonist properties. A novel series of 1,3-diphenylureas and N-phenylbenzamides have thus been prepared and evaluated. Based on its in vitro and in vivo activities, as well as pharmacokinetic profile, compound 16a was identified as a lead compound. The synthesis and structure-activity relationship of this series of compounds is presented herein.
  • Bioorganic & medicinal chemistry letters.Bioorg Med Chem Lett.2014 May 1;24(9):2118-22. doi: 10.1016/j.bmcl.2014.03.043. Epub 2014 Mar 24.
  • This Letter describes our attempts to elaborate dually acting compounds possessing serotonin re-uptake transporter inhibitor and serotonin 5-HT2C receptor antagonist properties. A novel series of 1,3-diphenylureas and N-phenylbenzamides have thus been prepared and evaluated. Based on its in vitro an
  • PMID 24717153

和文文献

  • Antiallodynic Action of 1-(3-(9H-Carbazol-9-yl)-1-propyl)-4-(2-methyoxyphenyl)-4-piperidinol (NNC05-2090), a Betaine/GABA Transporter Inhibitor
  • , , [他], , , , , ,
  • Journal of Pharmacological Sciences 125(2), 217-226, 2014
  • … 1-(3-(9H-Carbazol-9-yl)-1-propyl)-4-(2-methyoxyphenyl)-4-piperidinol (NNC05-2090), an inhibitor that displays moderate selectivity for BGT-1, had an antiallodynic action on model mice treated through both intrathecally and intravenous administration routes. … On the other hand, SKF89976A, a selective GAT-1 inhibitor, had a weak antiallodynic action, and (S)-SNAP5114, an inhibitor that displays selectivity for GAT-3, had no antiallodynic action. …
  • NAID 130004438625
  • Protective Effects of Fluvoxamine against Ischemia/Reperfusion Injury in Isolated, Perfused Guinea-Pig Hearts
  • , , , , , , , , , ,
  • Biological and Pharmaceutical Bulletin 37(5), 731-739, 2014
  • Serotonin (5-hydroxytryptamine; … Here, the beneficial effects of the selective serotonin reuptake inhibitor (SSRI) fluvoxamine was demonstrated on ischemia–reperfusion injury in guinea-pig hearts perfused using the Langendorff technique. …
  • NAID 130004147319
  • Effects of Paroxetine and Milnacipran on Pain Disorder
  • Sanada Kenji,Mimura Masaru,Uchida Eiji,Kato Nobumasa,Iwanami Akira,Sanada Kenji,Mimura Masaru,Uchida Eiji,Kato Nobumasa,Iwanami Akira
  • The Showa University Journal of Medical Sciences 24(4), 293-300, 2012-12
  • … The results of the present study suggest that both paroxetine (a selective serotonin re-uptake inhibitor) and milnacipran (a selective serotonin-noradrenaline re-uptake inhibitor) may decrease pain in individuals with pain disorder. …
  • NAID 120005536456

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Since the introduction of Blue Cross' GenericSelect(R) incentive program in the fourth quarter of 2002, members have nearly doubled the use of generic selective serotonin uptake inhibitors (anti-depressants), increased their use of ...

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Selective Serotonin Reuptake Inhibitors Sertralin side effects - ManVsOcdSerotonin reuptake inhibitor, selective  inhibitors; Dopamine Reuptake InhibitorsAnti-psychotic drugs cause permanent brain Selective Serotonin Reuptake Inhibitors In


★リンクテーブル★
リンク元セロトニン取り込み抑制薬」「セロトニン取り込み阻害剤」「serotonin reuptake inhibitor」「セロトニン取り込み阻害薬」「セロトニン取り込み抑制剤
関連記事inhibit」「uptake」「inhibitor」「serotonin

セロトニン取り込み抑制薬」

  [★]

serotonin uptake inhibitor5-HT uptake inhibitor
セロトニン再取り込み阻害薬セロトニン取り込み阻害剤セロトニン取り込み阻害薬セロトニン再取り込み阻害剤セロトニン取り込み抑制剤


セロトニン取り込み阻害剤」

  [★]

serotonin uptake inhibitor
セロトニン再取り込み阻害薬セロトニン取り込み阻害薬セロトニン取り込み抑制薬セロトニン再取り込み阻害剤セロトニン取り込み抑制剤


serotonin reuptake inhibitor」

  [★]

5-HT uptake inhibitorserotonin uptake inhibitor

セロトニン取り込み阻害薬」

  [★]

serotonin uptake inhibitor5-HT uptake inhibitor
セロトニン取り込み阻害剤セロトニン取り込み抑制薬セロトニン取り込み抑制剤


セロトニン取り込み抑制剤」

  [★]

serotonin uptake inhibitor
セロトニン取り込み阻害剤セロトニン取り込み阻害薬セロトニン取り込み抑制薬

inhibit」

  [★]

  • v.
  • 抑制する、阻害する、阻止する
abrogateblockdepressdepressiondeterinhibitioninterdictpreventpreventionrepressrepressionrestrainrestraintsuppresssuppression

WordNet   license wordnet

「limit, block, or decrease the action or function of; "inhibit the action of the enzyme"; "inhibit the rate of a chemical reaction"」

PrepTutorEJDIC   license prepejdic

「〈感情・欲望・行動・作用など〉‘を'抑制する / (…しないように)〈人〉‘を'抑制する,妨げる《+『名』+『from』+『名』(do『ing』)》」

WordNet   license wordnet

「control and refrain from showing; of emotions, desires, impulses, or behavior」
bottle up, suppress

WordNet   license wordnet

「limit the range or extent of; "Contact between the young was inhibited by strict social customs"」

uptake」

  [★]

  • n.
  • v.
incorporateincorporation

WordNet   license wordnet

「a process of taking up or using up or consuming; "they developed paper napkins with a greater uptake of liquids"」

PrepTutorEJDIC   license prepejdic

「〈U〉《the up. take》《話》理解,予解 / 〈C〉(鉱山などで空気や煙の)吸い上げパイプ」


inhibitor」

  [★]

  • n.
blockerdepressantsuppressant

WordNet   license wordnet

「a substance that retards or stops an activity」

PrepTutorEJDIC   license prepejdic

「抑制する人(物) / 化学反応抑制剤」

serotonin」

  [★] セロトニン 5-HT 5HT

WordNet   license wordnet

「a neurotransmitter involved in e.g. sleep and depression and memory」
5-hydroxytryptamine




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