Fananserin

Fananserin

Clinical data
Other names	RP-62203; RP62203
Drug class	Serotonin 5-HT2A receptor antagonist; Dopamine D4 receptor antagonist
ATC code	None
Identifiers
IUPAC name 2-(3-(4-(p-Fluorophenyl)-1-piperazinyl)propyl)-2H-naphth(1,8-cd)isothiazole 1,1-dioxide
CAS Number	127625-29-0  Y
PubChem CID	60785
IUPHAR/BPS	5434
ChemSpider	54781  N
UNII	38QJ762ET6
KEGG	D02656  Y
CompTox Dashboard (EPA)	DTXSID8046743
Chemical and physical data
Formula	C23H24FN3O2S
Molar mass	425.52 g·mol−1
3D model (JSmol)	Interactive image
SMILES C1CN(CCN1CCCN2C3=CC=CC4=C3C(=CC=C4)S2(=O)=O)C5=CC=C(C=C5)F
InChI 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
NY  (what is this?)    (verify)

Fananserin (RP-62203) is a drug which acts as a potent antagonist at both the serotonin 5-HT_2A receptor, ^[1] and the dopamine D₄ receptor, ^[2] but without blocking other dopamine receptors such as the dopamine D₂ receptor. ^[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]

See also

• Serotonin 5-HT_2A receptor antagonist

References

1. Malleron JL, Comte MT, Gueremy C, Peyronel JF, Truchon A, Blanchard JC, et al. (August 1991). "Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists". Journal of Medicinal Chemistry. 34 (8): 2477–83. doi:10.1021/jm00112a025. PMID   1908521.
2. Heuillet E, Petitet F, Mignani S, Malleron JL, Lavayre J, Néliat G, et al. (October 1996). "The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor". European Journal of Pharmacology. 314 (1–2): 229–33. doi:10.1016/s0014-2999(96)00554-7. PMID   8957240.
3. Doble A, Girdlestone D, Piot O, Allam D, Betschart J, Boireau A, et al. (January 1992). "Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist". British Journal of Pharmacology. 105 (1): 27–36. doi:10.1111/j.1476-5381.1992.tb14206.x. PMC   1908636 . PMID   1596688.
4. Stutzmann JM, Eon B, Lucas M, Blanchard JC, Laduron PM (April 1992). "RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats". Sleep. 15 (2): 119–24. doi: 10.1093/sleep/15.2.119 . PMID   1579785.
5. Sramek JJ, Kirkesseli S, Paccaly-Moulin A, Davidson J, Jhee SS, Hourani J, et al. (1998). "A bridging study of fananserin in schizophrenic patients". Psychopharmacology Bulletin. 34 (4): 811–8. PMID   10513457.
6. Truffinet P, Tamminga CA, Fabre LF, Meltzer HY, Rivière ME, Papillon-Downey C (March 1999). "Placebo-controlled study of the D₄/5-HT_2A antagonist fananserin in the treatment of schizophrenia" . The American Journal of Psychiatry. 156 (3): 419–25. doi:10.1176/ajp.156.3.419. PMID   10080558. S2CID   41422352.