Fananserin

Fananserin
Clinical data
Other names	Fananserin
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 ;
PubChem CID	60785;
IUPHAR/BPS	5434;
ChemSpider	54781 ;
UNII	38QJ762ET6;
KEGG	D02656 ;
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 ; Key:VGIGHGMPMUCLIQ-UHFFFAOYSA-N ;
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Fananserin (RP-62203) is a drug which acts as a potent antagonist at both the 5HT_2A 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

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.
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.
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.
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.
Sramek JJ, Kirkesseli S, Paccaly-Moulin A, Davidson J, Jhee SS, Hourani J, et al. "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 (March 1999). "Placebo-controlled study of the D4/5-HT2A 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.

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[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. "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-HT2A 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.