Fananserin
Fananserin (RP-62204) je leki koji deluje kao potentan antagonist na 5HT2A receptoru,[1] i Dopaminskom D4 receptoru,[2] a ne blokira druge dopaminske receptore kao što je D2.[3] On ima sedativno[4] i antipsihotično dejstvo, te je istraživan za moguću primenu u lečenju šizofrenije.[5] Nije se pokazao dovoljno efektivnim, i rezultati su bili nezadovoljavajući.[6]
 | |
| IUPAC ime | |
|---|---|
2-(3-(4-(p-Fluorofenil)-1-piperazinil)propil)-2H-naft(1,8-cd)izotiazol 1,1-dioksid | |
| Identifikatori | |
| CAS broj | 127625-29-0  |
| ATC kod | none |
| PubChem | CID 60785 |
| UNII | 38QJ762ET6 |
| KEGG | D02656 |
| Sinonimi | Fananserin |
| Hemijski podaci | |
| Formula | C23H24FN3O2S |
| Molarna masa | 425,519 g/mol |
| |
Reference
уреди- ^ Malleron JL, Comte MT, Gueremy C, Peyronel JF, Truchon A, Blanchard JC, Doble A, Piot O, Zundel JL, Huon C, et al. Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists. Malleron, J. L.; Comte, M. T.; Gueremy, C.; Peyronel, J. F.; Truchon, A.; Blanchard, J. C.; Doble, A.; Piot, O.; Zundel, J. L.; Huon, C. (август 1991). „Naphthosultam derivatives: A new class of potent and selective 5-HT2 antagonists”. Journal of Medicinal Chemistry. 34 (8): 2477—83. PMID 1908521. doi:10.1021/jm00112a025.
- ^ Heuillet E, Petitet F, Mignani S, Malleron JL, Lavayre J, Néliat G, Doble A, Blanchard JC. The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor. European Journal of Pharmacology. 24;314(1-2):229-33. Heuillet, E.; Petitet, F.; Mignani, S.; Malleron, J. L.; Lavayre, J.; Néliat, G.; Doble, A.; Blanchard, J. C. (1996 Oct). „The naphtosultam derivative RP 62203 (Fananserin) has high affinity for the dopamine D4 receptor”. European Journal of Pharmacology. 314 (1–2): 229—233. PMID 8957240. doi:10.1016/s0014-2999(96)00554-7. Проверите вредност парамет(а)ра за датум:
|date=(помоћ) - ^ Doble A, Girdlestone D, Piot O, Allam D, Betschart J, Boireau A, Dupuy A, Guérémy C, Ménager J, Zundel JL, et al. Doble, A.; Girdlestone, D.; Piot, O.; Allam, D.; Betschart, J.; Boireau, A.; Dupuy, A.; Guérémy, C.; Ménager, J.; Zundel, J. L. (јануар 1992). „Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist”. British Journal of Pharmacology. 105 (1): 27—36. PMC 1908636
. PMID 1596688. doi:10.1111/j.1476-5381.1992.tb14206.x.
- ^ Stutzmann JM, Eon B, Lucas M, Blanchard JC, Laduron PM. Stutzmann, J. M.; Eon, B.; Lucas, M.; Blanchard, J. C.; Laduron, P. M. (април 1992). „RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats”. Sleep. 15 (2): 119—24. PMID 1579785. doi:10.1093/sleep/15.2.119.
- ^ Sramek JJ, Kirkesseli S, Paccaly-Moulin A, Davidson J, Jhee SS, Hourani J, Sémiond D, Cutler NR. Sramek, J. J.; Kirkesseli, S.; Paccaly-Moulin, A.; Davidson, J.; Jhee, S. S.; Hourani, J.; Sémiond, D.; Cutler, N. R. (1998). „A bridging study of fananserin in schizophrenic patients”. Psychopharmacology Bulletin. 34 (4): 811—8. PMID 10513457.
- ^ Truffinet P, Tamminga CA, Fabre LF, Meltzer HY, Rivière ME, Papillon-Downey C. Placebo-controlled study of the D4/5-HT2A antagonist fananserin in the treatment of schizophrenia. Truffinet, P.; Tamminga, C. A.; Fabre, L. F.; Meltzer, H. Y.; Rivière, M. E.; Papillon-Downey, C. (март 1999). „Placebo-controlled study of the D4/5-HT2A antagonist fananserin in the treatment of schizophrenia”. American Journal of Psychiatry. 156 (3): 419—25. PMID 10080558. doi:10.1176/ajp.156.3.419.
