SB-258,719

Izvor: Wikipedia
SB-258,719
(IUPAC) ime
(1R)-3,N-dimetil-N-[1-metil-3-(4-metilpiperidin-1-il)propil]benzenesulfonamid
Klinički podaci
Identifikatori
CAS broj 195199-95-2
ATC kod nije dodeljen
PubChem[1][2] 5312148
ChemSpider[3] 4471578
ChEMBL[4] CHEMBL12264 YesY
Hemijski podaci
Formula C18H32N2O2S 
Mol. masa 340,523 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća  ?
Pravni status

SB-258,719 je lek koji deluje kao selektivni parcijalni inverzni agonist 5-HT7 receptora.[5] On je bio prvi identifikovani antagonist 5-HT7 receptora.[6] On se uglavnom upotrebljan u istraživanjima za demonstriranje potencijalne uloge 5-HT7 agonista kao potencijalnih analgetika, usled njegove sposobnosti da blokira analgetičke efekte raznih 5-HT7 agonista u miše modela.[7][8][9][10]

Reference[uredi - уреди]

  1. Li Q, Cheng T, Wang Y, Bryant SH (2010). "PubChem as a public resource for drug discovery.". Drug Discov Today 15 (23-24): 1052–7. doi:10.1016/j.drudis.2010.10.003. PMID 20970519.  edit
  2. Evan E. Bolton, Yanli Wang, Paul A. Thiessen, Stephen H. Bryant (2008). "Chapter 12 PubChem: Integrated Platform of Small Molecules and Biological Activities". Annual Reports in Computational Chemistry 4: 217–241. doi:10.1016/S1574-1400(08)00012-1. 
  3. Hettne KM, Williams AJ, van Mulligen EM, Kleinjans J, Tkachenko V, Kors JA. (2010). "Automatic vs. manual curation of a multi-source chemical dictionary: the impact on text mining". J Cheminform 2 (1): 3. doi:10.1186/1758-2946-2-3. PMID 20331846.  edit
  4. Gaulton A, Bellis LJ, Bento AP, Chambers J, Davies M, Hersey A, Light Y, McGlinchey S, Michalovich D, Al-Lazikani B, Overington JP. (2012). "ChEMBL: a large-scale bioactivity database for drug discovery". Nucleic Acids Res 40 (Database issue): D1100–7. doi:10.1093/nar/gkr777. PMID 21948594.  edit
  5. Mahé C, Loetscher E, Feuerbach D, Müller W, Seiler MP, Schoeffter P (July 2004). "Differential inverse agonist efficacies of SB-258719, SB-258741 and SB-269970 at human recombinant serotonin 5-HT7 receptors". European Journal of Pharmacology 495 (2-3): 97–102. doi:10.1016/j.ejphar.2004.05.033. PMID 15249157. 
  6. Forbes IT, Dabbs S, Duckworth DM, Jennings AJ, King FD, Lovell PJ, Brown AM, Collin L, Hagan JJ, Middlemiss DN, Riley GJ, Thomas DR, Upton N (February 1998). "(R)-3,N-dimethyl-N-[1-methyl-3-(4-methyl-piperidin-1-yl) propyl]benzenesulfonamide: the first selective 5-HT7 receptor antagonist". Journal of Medicinal Chemistry 41 (5): 655–7. doi:10.1021/jm970519e. PMID 9513592. 
  7. Brenchat A, Romero L, García M, Pujol M, Burgueño J, Torrens A, Hamon M, Baeyens JM, Buschmann H, Zamanillo D, Vela JM (February 2009). "5-HT7 receptor activation inhibits mechanical hypersensitivity secondary to capsaicin sensitization in mice". Pain 141 (3): 239–47. doi:10.1016/j.pain.2008.11.009. PMID 19118950. 
  8. Yanarates O, Dogrul A, Yildirim V, Sahin A, Sizlan A, Seyrek M, Akgül O, Kozak O, Kurt E, Aypar U (March 2010). "Spinal 5-HT7 receptors play an important role in the antinociceptive and antihyperalgesic effects of tramadol and its metabolite, O-Desmethyltramadol, via activation of descending serotonergic pathways". Anesthesiology 112 (3): 696–710. doi:10.1097/ALN.0b013e3181cd7920. PMID 20179508. 
  9. Brenchat A, Nadal X, Romero L, Ovalle S, Muro A, Sánchez-Arroyos R, Portillo-Salido E, Pujol M, Montero A, Codony X, Burgueño J, Zamanillo D, Hamon M, Maldonado R, Vela JM (June 2010). "Pharmacological activation of 5-HT7 receptors reduces nerve injury-induced mechanical and thermal hypersensitivity". Pain 149 (3): 483–94. doi:10.1016/j.pain.2010.03.007. PMID 20399562. 
  10. Brenchat A, Ejarque M, Zamanillo D, Vela JM, Romero L (August 2011). "Potentiation of Morphine Analgesia by Adjuvant Activation of 5-HT(7) Receptors". Journal of Pharmacological Sciences 116 (4): 388–91. PMID 21778664. 

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