Fananserin

drugbox
IUPAC_name = 2-(3-(4-(p-Fluorophenyl)-1-piperazinyl)propyl)-2H-naphth(1,8-cd)isothiazole 1,1-dioxide



width = 240
CAS_number = 127625-29-0
synonyms = Fananserin
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PubChem = 60785
DrugBank =
C = 23 | H = 24 | F = 1 | N = 3 | O = 2 | S = 1
molecular_weight = 425.519 g/mol
smiles = C1CN(CCN1CCCN2C3=CC=CC4=C3C(=CC=C4)S2(=O)=O)C5=CC=C(C=C5)F
bioavailability =
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Fananserin (RP-62204) is a drug which acts as a potent antagonist at both the 5HT2A receptor, [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] and the Dopamine D4 receptor, [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] but without blocking other dopamine receptors such as D2. [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] It has sedative [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] and antipsychotic effects, and has been researched for the treatment of schizophrenia, [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] although efficacy was less than expected and results were disappointing. [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]

References


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