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. Journal of Medicinal Chemistry. 1991 Aug;34(8):2477-83. PMID 1908521
- ^ 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. 1996 Oct 24;314(1-2):229-33. PMID 8957240
- ^ Doble A, Girdlestone D, Piot O, Allam D, Betschart J, Boireau A, Dupuy A, Guérémy C, Ménager J, Zundel JL, et al. Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist. British Journal of Pharmacology. 1992 Jan;105(1):27-36. PMID 1596688
- ^ Stutzmann JM, Eon B, Lucas M, Blanchard JC, Laduron PM. RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats. Sleep. 1992 Apr;15(2):119-24. PMID 1579785
- ^ Sramek JJ, Kirkesseli S, Paccaly-Moulin A, Davidson J, Jhee SS, Hourani J, Sémiond D, Cutler NR. A bridging study of fananserin in schizophrenic patients. Psychopharmacology Bulletin. 1998;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. American Journal of Psychiatry. 1999 Mar;156(3):419-25. PMID 10080558
