S-15,535

(Preusmjereno sa stranice S-15535)

S-15535 je fenilpiperazinski lek koji je potentan i visoko selektivan ligand 5-HT1A receptor. On je agonist i antagonist (slab parcijalni agonist) na presinaptičkim i postsinaptičkim 5-HT1A receptorima, respektivno.[4][5][6][7] On ima anksiolitička svojstva.[7][8]

S-15,535
(IUPAC) ime
1-(2,3-dihidro-1,4-benzodioksin-8-il)-4-(2,3-dihidro-1H-inden-2-il)piperazin
Klinički podaci
Identifikatori
CAS broj 146998-34-7
ATC kod nije dodeljen
PubChem[1][2] 132787
ChEMBL[3] CHEMBL49247 DaY
Hemijski podaci
Formula C21H24N2O2 
Mol. masa 336,427 g/mol
SMILES eMolekuli & PubHem
Farmakoinformacioni podaci
Trudnoća ?
Pravni status

Reference

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  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. 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
  4. Millan MJ, Rivet JM, Canton H, Lejeune F, Gobert A, Widdowson P, Bervoets K, Brocco M, Peglion JL. (1993). „S 15535: a highly selective benzodioxopiperazine 5-HT1A receptor ligand which acts as an agonist and an antagonist (weak partial agonist) at presynaptic and postsynaptic sites respectively”. Eur J Pharmacol. 230 (1): 99–102. DOI:10.1016/0014-2999(93)90416-F. PMID 8381359. 
  5. Millan MJ, Canton H, Gobert A, Lejeune F, Rivet JM, Bervoets K, Brocco M, Widdowson P, Mennini T, Audinot V, et al. (1994). „Novel benzodioxopiperazines acting as antagonists at postsynaptic 5-HT1A receptors and as agonists at 5-HT1A autoreceptors: a comparative pharmacological characterization with proposed 5-HT1A antagonists”. J Pharmacol Exp Ther. 268 (1): 337–352. PMID 8301575. 
  6. Millan MJ, Newman-Tancredi A, Rivet JM, Brocco M, Lacroix P, Audinot V, Cistarelli L, Gobert A. (1997). „S 15535, a novel benzodioxopiperazine ligand of serotonin (5-HT)1A receptors: I. Interaction with cloned human (h)5-HT1A, dopamine hD2/hD3 and h alpha2A-adrenergic receptors in relation to modulation of cortical monoamine release and activity in models of potential antidepressant activity”. J Pharmacol Exp Ther. 282 (1): 132–147. PMID 9223549. 
  7. 7,0 7,1 Lejeune F, Millan MJ. (1998). „Induction of burst firing in ventral tegmental area dopaminergic neurons by activation of serotonin (5-HT)1A receptors: WAY 100,635-reversible actions of the highly selective ligands, flesinoxan and S 15535”. Synapse. 30 (2): 172–180. DOI:10.1002/(SICI)1098-2396(199810)30:2<172::AID-SYN7>3.0.CO;2-9. PMID 9723787. 
  8. Dekeyne A, Brocco M, Adhumeau A, Gobert A, Millan MJ. (2000). „The selective serotonin (5-HT)1A receptor ligand, S15535, displays anxiolytic-like effects in the social interaction and Vogel models and suppresses dialysate levels of 5-HT in the dorsal hippocampus of freely-moving rats. A comparison with other anxiolytic agents”. Psychopharmacology (Berl). 152 (1): 55–66. DOI:10.1007/s002130000449. PMID 11041316. 

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