SB-242084 (BioDeep_00000794670)
代谢物信息卡片
化学式: C21H19ClN4O2 (394.1196464)
中文名称: SB 242084
谱图信息:
最多检出来源 () 0%
分子结构信息
SMILES: CC1=CC2=C(C=C1Cl)N(CC2)C(=O)NC3=CN=C(C=C3)OC4=C(N=CC=C4)C
InChI: InChI=1S/C21H19ClN4O2/c1-13-10-15-7-9-26(18(15)11-17(13)22)21(27)25-16-5-6-20(24-12-16)28-19-4-3-8-23-14(19)2/h3-6,8,10-12H,7,9H2,1-2H3,(H,25,27)
描述信息
SB 242084 is a selective, competitive and high-affinity (pKi=9.0) 5-HT2C receptor antagonist (crosses the blood-brain barrier). SB 242084 increases basal activity of dopaminergic neurons in the ventral tegmental area (VTA) of the midbrain and dopamine release in the vomeronasal nucleus. SB 242084 also increases mitochondrial gene expression and oxidative metabolism via 5-HT2A receptor. SB 242084 has good research potential in the negative symptoms of anxiety, depression and schizophrenia, as well as in acute organ damage[1][2][3].
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在这里通过桑基图来展示出与当前的这个代谢物在我们的BioDeep知识库中具有相关联信息的其他代谢物。在这里进行关联的信息来源主要有：
- PubMed: 来源于PubMed文献库中的文献信息，我们通过自然语言数据挖掘得到的在同一篇文献中被同时提及的相关代谢物列表，这个列表按照代谢物同时出现的文献数量降序排序，取前10个代谢物作为相关研究中关联性很高的代谢物集合展示在桑基图中。
- NCBI Taxonomy: 通过文献数据挖掘，得到的代谢物物种来源信息关联。这个关联信息同样按照出现的次数降序排序，取前10个代谢物作为高关联度的代谢物集合展示在桑吉图上。
- Chemical Taxonomy: 在物质分类上处于同一个分类集合中的其他代谢物
- Chemical Reaction: 在化学反应过程中，存在为当前代谢物相关联的生化反应过程中的反应底物或者反应产物的关联代谢物信息。
点击图上的相关代谢物的名称，可以跳转到相关代谢物的信息页面。
文献列表
- Joanne L Griggs, Michael L Mathai, Puspha Sinnayah. Caralluma fimbriata extract activity involves the 5-HT2c receptor in PWS Snord116 deletion mouse model.
Brain and behavior.
2018 12; 8(12):e01102. doi:
10.1002/brb3.1102. [PMID: 30353709] - Chinami Matsumoto, Chihiro Yamada, Chiharu Sadakane, Miwa Nahata, Tomohisa Hattori, Hiroshi Takeda. Psychological stress in aged female mice causes acute hypophagia independent of central serotonin 2C receptor activation.
PloS one.
2017; 12(11):e0187937. doi:
10.1371/journal.pone.0187937. [PMID: 29125864] - Caleb J Browne, Paul J Fletcher. Decreased Incentive Motivation Following Knockout or Acute Blockade of the Serotonin Transporter: Role of the 5-HT2C Receptor.
Neuropsychopharmacology : official publication of the American College of Neuropsychopharmacology.
2016 09; 41(10):2566-76. doi:
10.1038/npp.2016.63. [PMID: 27125304] - Jennifer L Harmon, Lauren P Wills, Caitlin E McOmish, Elena Y Demireva, Jay A Gingrich, Craig C Beeson, Rick G Schnellmann. 5-HT2 Receptor Regulation of Mitochondrial Genes: Unexpected Pharmacological Effects of Agonists and Antagonists.
The Journal of pharmacology and experimental therapeutics.
2016 Apr; 357(1):1-9. doi:
10.1124/jpet.115.228395. [PMID: 26787771] - Olivér Éliás, Katalin Nógrádi, György Domány, Zoltán Szakács, János Kóti, Csaba Szántay, Ákos Tarcsay, György M Keserű, Anikó Gere, Béla Kiss, Dalma Kurkó, Sándor Kolok, Zsolt Némethy, Zoltán Kapui, Éva Hellinger, Mónika Vastag, Katalin Sághy, Rita Kedves, István Gyertyán. The influence of 5-HT(2A) activity on a 5-HT(2C) specific in vivo assay used for early identification of multiple acting SERT and 5-HT(2C) receptor ligands.
Bioorganic & medicinal chemistry letters.
2016 Feb; 26(3):914-920. doi:
10.1016/j.bmcl.2015.12.071. [PMID: 26748694] - Chihiro Yamada, Chiharu Sadakane, Miwa Nahata, Yayoi Saegusa, Koji Nakagawa, Naoto Okubo, Shunsuke Ohnishi, Tomohisa Hattori, Hiroshi Takeda. Serotonin 2C receptor contributes to gender differences in stress-induced hypophagia in aged mice.
Psychoneuroendocrinology.
2015 May; 55(?):81-93. doi:
10.1016/j.psyneuen.2015.02.006. [PMID: 25732068] - Qiang Zhang, Yunxia Zhu, Wenbo Zhou, Lu Gao, Li Yuan, Xiao Han. Serotonin receptor 2C and insulin secretion.
PloS one.
2013; 8(1):e54250. doi:
10.1371/journal.pone.0054250. [PMID: 23349838] - Mark J Millan, Clotilde Mannoury la Cour, Benjamin Chanrion, Delphine S Dupuis, Benjamin Di Cara, Valérie Audinot, Didier Cussac, Adrian Newman-Tancredi, Maud Kamal, Jean A Boutin, Ralf Jockers, Philippe Marin, Joël Bockaert, Olivier Muller, Anne Dekeyne, Gilbert Lavielle. S32212, a novel serotonin type 2C receptor inverse agonist/α2-adrenoceptor antagonist and potential antidepressant: I. A mechanistic characterization.
The Journal of pharmacology and experimental therapeutics.
2012 Mar; 340(3):750-64. doi:
10.1124/jpet.111.187468. [PMID: 22178752] - Marilyne Labasque, Julie Meffre, Gaelle Carrat, Carine Becamel, Joël Bockaert, Philippe Marin. Constitutive activity of serotonin 2C receptors at G protein-independent signaling: modulation by RNA editing and antidepressants.
Molecular pharmacology.
2010 Nov; 78(5):818-26. doi:
10.1124/mol.110.066035. [PMID: 20699324] - Koji Yakabi, Chiharu Sadakane, Masamichi Noguchi, Shino Ohno, Shoki Ro, Katsuya Chinen, Toru Aoyama, Tomoya Sakurada, Hideaki Takabayashi, Tomohisa Hattori. Reduced ghrelin secretion in the hypothalamus of rats due to cisplatin-induced anorexia.
Endocrinology.
2010 Aug; 151(8):3773-82. doi:
10.1210/en.2010-0061. [PMID: 20534732] - Hiroshi Takeda, Chiharu Sadakane, Tomohisa Hattori, Takehiko Katsurada, Tatsuya Ohkawara, Koichi Nagai, Masahiro Asaka. Rikkunshito, an herbal medicine, suppresses cisplatin-induced anorexia in rats via 5-HT2 receptor antagonism.
Gastroenterology.
2008 Jun; 134(7):2004-13. doi:
10.1053/j.gastro.2008.02.078. [PMID: 18439428] - Benjamin Chanrion, Clotilde Mannoury la Cour, Sophie Gavarini, Mathieu Seimandi, Laurent Vincent, Jean-François Pujol, Joël Bockaert, Philippe Marin, Mark J Millan. Inverse agonist and neutral antagonist actions of antidepressants at recombinant and native 5-hydroxytryptamine2C receptors: differential modulation of cell surface expression and signal transduction.
Molecular pharmacology.
2008 Mar; 73(3):748-57. doi:
10.1124/mol.107.041574. [PMID: 18083778] - K J Damjanoska, N A Muma, Y Zhang, D N D'Souza, F Garcia, G A Carrasco, G H Kindel, K A Haskins, M Shankaran, B R Petersen, L D Van De Kar. Neuroendocrine evidence that (S)-2-(chloro-5-fluoro-indol- l-yl)-1-methylethylamine fumarate (Ro 60-0175) is not a selective 5-hydroxytryptamine(2C) receptor agonist.
The Journal of pharmacology and experimental therapeutics.
2003 Mar; 304(3):1209-16. doi:
10.1124/jpet.102.043489. [PMID: 12604698] - Susan K Hemrick-Luecke, David C Evans. Comparison of the potency of MDL 100,907 and SB 242084 in blocking the serotonin (5-HT)(2) receptor agonist-induced increases in rat serum corticosterone concentrations: evidence for 5-HT(2A) receptor mediation of the HPA axis.
Neuropharmacology.
2002 Feb; 42(2):162-9. doi:
10.1016/s0028-3908(01)00166-6. [PMID: 11804612]