Chemistry: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 ;
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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Short description: Chemical compound

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

↑ "Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists". Journal of Medicinal Chemistry 34 (8): 2477–83. August 1991. doi:10.1021/jm00112a025. PMID 1908521.
↑ "The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor". European Journal of Pharmacology 314 (1–2): 229–33. October 1996. doi:10.1016/s0014-2999(96)00554-7. PMID 8957240.
↑ "Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist". British Journal of Pharmacology 105 (1): 27–36. January 1992. doi:10.1111/j.1476-5381.1992.tb14206.x. PMID 1596688.
↑ "RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats". Sleep 15 (2): 119–24. April 1992. doi:10.1093/sleep/15.2.119. PMID 1579785.
↑ "A bridging study of fananserin in schizophrenic patients". Psychopharmacology Bulletin 34 (4): 811–8. 1998. PMID 10513457.
↑ "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. March 1999. doi:10.1176/ajp.156.3.419. PMID 10080558. https://ajp.psychiatryonline.org/doi/10.1176/ajp.156.3.419.

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Original source: https://en.wikipedia.org/wiki/Fananserin. Read more

[1] "Naphthosultam derivatives: a new class of potent and selective 5-HT2 antagonists". Journal of Medicinal Chemistry 34 (8): 2477–83. August 1991. doi:10.1021/jm00112a025. PMID 1908521.

[2] "The naphtosultam derivative RP 62203 (fananserin) has high affinity for the dopamine D4 receptor". European Journal of Pharmacology 314 (1–2): 229–33. October 1996. doi:10.1016/s0014-2999(96)00554-7. PMID 8957240.

[3] "Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist". British Journal of Pharmacology 105 (1): 27–36. January 1992. doi:10.1111/j.1476-5381.1992.tb14206.x. PMID 1596688.

[4] "RP 62203, a 5-hydroxytryptamine2 antagonist, enhances deep NREM sleep in rats". Sleep 15 (2): 119–24. April 1992. doi:10.1093/sleep/15.2.119. PMID 1579785.

[5] "A bridging study of fananserin in schizophrenic patients". Psychopharmacology Bulletin 34 (4): 811–8. 1998. PMID 10513457.

[6] "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. March 1999. doi:10.1176/ajp.156.3.419. PMID 10080558. https://ajp.psychiatryonline.org/doi/10.1176/ajp.156.3.419.

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