SB-612,111

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SB-612,111
(IUPAC) ime
(5S,7S)-7[4-(2,6-dihlorofenil)piperidin-1-il]metil1-metil-6,7,8,9-tetrahidro-5H-benzo[7]anulen-5-ol
Klinički podaci
Identifikatori
ATC kod ?
PubChem[1][2] 10047612
Hemijski podaci
Formula C24H29Cl2NO 
Mol. masa 418,398 g/mol
SMILES eMolekuli & PubHem
Sinonimi SB-612,111
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

SB-612,111 je ligand opioidnog receptora. On je potentan i selektivan antagonist za nociceptinskog receptora (ORL-1). Ovaj ligand je nekoliko puta potentniji od starijeg leka J-113,397.[3] On ne proizvodi analgetičke efekte, nego sprečava razvoj hiperalgezije.[4] Pokazano je da ima antidepresivno dejstvo u studijama na životinjama.[5]

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Reference[uredi - уреди | uredi izvor]

  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. PMID 20970519. doi:10.1016/j.drudis.2010.10.003.  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. Spagnolo, B; Carrà, G; Fantin, M; Fischetti, C; Hebbes, C; McDonald, J; Barnes, TA; Rizzi, A; Trapella, C (2007). "Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 (-)-cis-1-methyl-7-4-(2,6-dichlorophenyl)piperidin-1-ylmethyl-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol: in vitro studies". The Journal of pharmacology and experimental therapeutics 321 (3): 961–7. PMID 17329552. doi:10.1124/jpet.106.116764. 
  4. Zaratin, PF; Petrone, G; Sbacchi, M; Garnier, M; Fossati, C; Petrillo, P; Ronzoni, S; Giardina, GA; Scheideler, MA (2004). "Modification of nociception and morphine tolerance by the selective opiate receptor-like orphan receptor antagonist (-)-cis-1-methyl-7-4-(2,6-dichlorophenyl)piperidin-1-ylmethyl-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol (SB-612111)". The Journal of pharmacology and experimental therapeutics 308 (2): 454–61. PMID 14593080. doi:10.1124/jpet.103.055848. 
  5. Rizzi, A; Gavioli, EC; Marzola, G; Spagnolo, B; Zucchini, S; Ciccocioppo, R; Trapella, C; Regoli, D; Calò, G (2007). "Pharmacological characterization of the nociceptin/orphanin FQ receptor antagonist SB-612111 (-)-cis-1-methyl-7-4-(2,6-dichlorophenyl)piperidin-1-ylmethyl-6,7,8,9-tetrahydro-5H-benzocyclohepten-5-ol: in vivo studies". The Journal of pharmacology and experimental therapeutics 321 (3): 968–74. PMID 17329551. doi:10.1124/jpet.106.116780. 

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