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GR-125743

  Cat. No.:  DC39822   Featured
Chemical Structure
148547-33-5
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More than 5000 active chemicals with high quality for research!
Field of application
GR 125,743 is a novel 5-HT1B/1D receptor antagonist.
Chemicals PropertiesBiological activity COA & MSDSRelated productsDatasheet
Cas No.: 148547-33-5
Chemical Name: GR 125743
SMILES: O=C(C1=CC=C(C(C)=C1)C2=CC=NC=C2)NC3=CC=C(C(N4CCN(CC4)C)=C3)OC
Formula: C25H28N4O2
M.Wt: 416.52
Purity: >98%
Sotrage: 2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO
Publication: 1: Riahi G, Morissette M, Samadi P, Parent M, Di Paolo T. Basal ganglia serotonin 1B receptors in parkinsonian monkeys with L-DOPA-induced dyskinesia. Biochem Pharmacol. 2013 Oct 1;86(7):970-8. doi: 10.1016/j.bcp.2013.08.005. Epub 2013 Aug 14. PMID: 23954709. 2: du Jardin KG, Jensen JB, Sanchez C, Pehrson AL. Vortioxetine dose-dependently reverses 5-HT depletion-induced deficits in spatial working and object recognition memory: a potential role for 5-HT1A receptor agonism and 5-HT3 receptor antagonism. Eur Neuropsychopharmacol. 2014 Jan;24(1):160-71. doi: 10.1016/j.euroneuro.2013.07.001. Epub 2013 Aug 2. PMID: 23916504. 3: Storvik M, Häkkinen M, Tupala E, Tiihonen J. Whole-hemisphere autoradiography of 5-HT₁B receptor densities in postmortem alcoholic brains. Psychiatry Res. 2012 Jun 30;202(3):264-70. doi: 10.1016/j.pscychresns.2011.11.001. Epub 2012 Jul 16. PMID: 22804971. 4: Kaspersen H, Agmo A. Paroxetine-induced reduction of sexual incentive motivation in female rats is not modified by 5-HT1B or 5-HT2C antagonists. Psychopharmacology (Berl). 2012 Mar;220(2):269-80. doi: 10.1007/s00213-011-2475-1. Epub 2011 Sep 10. PMID: 21909633. 5: Smith GT, Combs N. Serotonergic activation of 5HT1A and 5HT2 receptors modulates sexually dimorphic communication signals in the weakly electric fish Apteronotus leptorhynchus. Horm Behav. 2008 Jun;54(1):69-82. doi: 10.1016/j.yhbeh.2008.01.009. Epub 2008 Feb 9. PMID: 18336816. 6: Hanff LM, Gupta S, MaassenVanDenBrink A, Steegers EA, Saxena PR, Vulto AG, Visser W. The effect of maternal ketanserin treatment on foetal 5-HT receptor function in umbilical cord artery of pre-eclamptic patients. Neonatology. 2007;92(4):240-7. doi: 10.1159/000103742. Epub 2007 Jun 8. PMID: 17556842. 7: Ahlgren C, Eriksson A, Tellefors P, Ross SB, Stenfors C, Malmberg A. In vitro characterization of AR-A000002, a novel 5-hydroxytryptamine(1B) autoreceptor antagonist. Eur J Pharmacol. 2004 Sep 19;499(1-2):67-75. doi: 10.1016/j.ejphar.2004.07.067. PMID: 15363952. 8: Przegaliński E, Czepiel K, Nowak E, Dlaboga D, Filip M. Withdrawal from chronic cocaine up-regulates 5-HT1B receptors in the rat brain. Neurosci Lett. 2003 Nov 20;351(3):169-72. doi: 10.1016/j.neulet.2003.08.007. PMID: 14623133. 9: Garcia-Alloza M, Hirst WD, Chen CP, Lasheras B, Francis PT, Ramírez MJ. Differential involvement of 5-HT(1B/1D) and 5-HT6 receptors in cognitive and non-cognitive symptoms in Alzheimer's disease. Neuropsychopharmacology. 2004 Feb;29(2):410-6. doi: 10.1038/sj.npp.1300330. PMID: 14571255. 10: Millan MJ, Newman-Tancredi A, Lochon S, Touzard M, Aubry S, Audinot V. Specific labelling of serotonin 5-HT(1B) receptors in rat frontal cortex with the novel, phenylpiperazine derivative, [3H]GR125,743. A pharmacological characterization. Pharmacol Biochem Behav. 2002 Apr;71(4):589-98. doi: 10.1016/s0091-3057(01)00716-x. PMID: 11888550. 11: Varnäs K, Hall H, Bonaventure P, Sedvall G. Autoradiographic mapping of 5-HT(1B) and 5-HT(1D) receptors in the post mortem human brain using [(3)H]GR 125743. Brain Res. 2001 Oct 5;915(1):47-57. doi: 10.1016/s0006-8993(01)02823-2. PMID: 11578619. 12: Bhalla P, Sharma HS, Ma X, Wurch T, Pauwels PJ, Saxena PR. Molecular cloning, pharmacological properties and tissue distribution of the porcine 5-HT(1B) receptor. Br J Pharmacol. 2001 Jul;133(6):891-901. doi: 10.1038/sj.bjp.0704150. PMID: 11454663; PMCID: PMC1572856. 13: Grånäs C, Nordquist J, Mohell N, Larhammar D. Site-directed mutagenesis of the 5-HT1B receptor increases the affinity of 5-HT for the agonist low-affinity conformation and reduces the intrinsic activity of 5-HT. Eur J Pharmacol. 2001 Jun 8;421(2):69-76. doi: 10.1016/s0014-2999(01)01027-5. PMID: 11399261. 14: Audinot V, Newman-Tancredi A, Millan MJ. Constitutive activity at serotonin 5-HT(1D) receptors: detection by homologous GTPgammaS versus [(35)S]-GTPgammaS binding isotherms. Neuropharmacology. 2001;40(1):57-64. doi: 10.1016/s0028-3908(00)00104-0. PMID: 11077071. 15: Bhalla P, Sharma HS, Wurch T, Pauwels PJ, Saxena PR. Molecular cloning, sequence analysis and pharmacological properties of the porcine 5-HT(1D) receptor. Br J Pharmacol. 2000 Nov;131(5):949-57. doi: 10.1038/sj.bjp.0703645. PMID: 11053216; PMCID: PMC1572407. 16: van den Broek RW, MaassenVanDenBrink A, de Vries R, Bogers AJ, Stegmann AP, Avezaat CJ, Saxena PR. Pharmacological analysis of contractile effects of eletriptan and sumatriptan on human isolated blood vessels. Eur J Pharmacol. 2000 Oct 27;407(1-2):165-73. doi: 10.1016/s0014-2999(00)00712-3. PMID: 11050304. 17: Wurch T, Palmier C, Pauwels PJ. Induction of a high-affinity ketanserin binding site at the 5-Hydroxytryptamine(1B) receptor by modification of its carboxy-terminal intracellular portion. Biochem Pharmacol. 2000 May 1;59(9):1117-21. doi: 10.1016/s0006-2952(99)00416-5. PMID: 10704941. 18: Grånäs C, Larhammar D. Identification of an amino acid residue important for binding of methiothepin and sumatriptan to the human 5-HT(1B) receptor. Eur J Pharmacol. 1999 Sep 10;380(2-3):171-81. doi: 10.1016/s0014-2999(99)00520-8. PMID: 10513577. 19: Xie Z, Lee SP, O'Dowd BF, George SR. Serotonin 5-HT1B and 5-HT1D receptors form homodimers when expressed alone and heterodimers when co-expressed. FEBS Lett. 1999 Jul 30;456(1):63-7. doi: 10.1016/s0014-5793(99)00918-7. PMID: 10452531. 20: Bonaventure P, Umans L, Bakker MH, Cras P, Langlois X, Luyten WH, Megens AA, Serneels L, Van Leuven F, Leysen JE. Humanization of mouse 5-hydroxytryptamine1B receptor gene by homologous recombination: in vitro and in vivo characterization. Mol Pharmacol. 1999 Jul;56(1):54-67. doi: 10.1124/mol.56.1.54. PMID: 10385684.
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2018-0101
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