Fananserin

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Fananserin
Fananserin.svg
Systematic (IUPAC) name
2-(3-(4-(p-Fluorophenyl)-1-piperazinyl)propyl)-2H-naphth(1,8-cd)isothiazole 1,1-dioxide
Identifiers
CAS Number 127625-29-0 YesY
ATC code none
PubChem CID: 60785
IUPHAR/BPS 5434
ChemSpider 54781 N
UNII 38QJ762ET6 YesY
KEGG D02656 YesY
Synonyms Fananserin
Chemical data
Formula C23H24FN3O2S
Molecular mass 425.519 g/mol
  • C1CN(CCN1CCCN2C3=CC=CC4=C3C(=CC=C4)S2(=O)=O)C5=CC=C(C=C5)F
  • InChI=1S/C23H24FN3O2S/c24-19-8-10-20(11-9-19)26-16-14-25(15-17-26)12-3-13-27-21-6-1-4-18-5-2-7-22(23(18)21)30(27,28)29/h1-2,4-11H,3,12-17H2 N
  • Key:VGIGHGMPMUCLIQ-UHFFFAOYSA-N N
 NYesY (what is this?)  (verify)

Fananserin (RP-62203) is a drug which acts as a potent antagonist at both the 5HT2A receptor,[1] and the Dopamine D4 receptor,[2] but without blocking other dopamine receptors such as D2.[3] It has sedative[4] and antipsychotic effects, and has been researched for the treatment of schizophrenia,[5] although efficacy was less than expected and results were disappointing.[6]

References

  1. ↑ 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
  2. ↑ 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
  3. ↑ 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
  4. ↑ 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
  5. ↑ 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
  6. ↑ 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
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