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]
(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 | ||
Hemijski podaci | |||
Formula | C21H24N2O2 | ||
Mol. masa | 336,427 g/mol | ||
SMILES | eMolekuli & PubHem | ||
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Farmakoinformacioni podaci | |||
Trudnoća | ? | ||
Pravni status |
Reference
uredi- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 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.
- ↑ 7,0 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.
- ↑ 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.