Fananserin | CAS#127625-29-0 | antipsychotic

Fananserin
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WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#: 461454

CAS#: 127625-29-0

Description: Fananserin is a potential antipsychotic compound with high affinity for both D4 and 5-HT2A receptors, and negligible affinity for D2 receptors.

Chemical Structure

Fananserin

CAS# 127625-29-0

Instruction

Theoretical Analysis

MedKoo Cat#: 461454
Name: Fananserin
CAS#: 127625-29-0
Chemical Formula: C23H24FN3O2S
Exact Mass: 425.16
Molecular Weight: 425.520
Elemental Analysis: C, 64.92; H, 5.69; F, 4.46; N, 9.88; O, 7.52; S, 7.53

Price and Availability

Size	Price	Availability
50mg	USD 550	2 Weeks
100mg	USD 950	2 Weeks
200mg	USD 1650	2 Weeks
500mg	USD 2850	2 Weeks
1g	USD 4250	2 Weeks
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

Synonym: Fananserin; RP 62203; RP-62203; RP62203;

IUPAC/Chemical Name: 2-(3-(4-(4-fluorophenyl)piperazin-1-yl)propyl)-2H-naphtho[1,8-cd]isothiazole 1,1-dioxide

InChi Key: VGIGHGMPMUCLIQ-UHFFFAOYSA-N

InChi Code: 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

SMILES Code: FC1=CC=C(N2CCN(CCCN(C3=CC=CC4=C3C5=CC=C4)S5(=O)=O)CC2)C=C1

Appearance: Solid powder

Purity: >98% (or refer to the Certificate of Analysis)

Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility: Soluble in DMSO

Shelf Life: >3 years if stored properly

Drug Formulation: This drug may be formulated in DMSO

Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code: 2934.99.03.00

More Info:

Instruction:

View handling instruction

Biological target:
In vitro activity:
In vivo activity:

Preparing Stock Solutions

The following data is based on the product molecular weight 425.52 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:
In vitro protocol:
In vivo protocol:

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1: 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. Am J Psychiatry. 1999 Mar;156(3):419-25. PubMed PMID: 10080558.

2: 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. Psychopharmacol Bull. 1998;34(4):811-8. PubMed PMID: 10513457.

3: 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. Eur J Pharmacol. 1996 Oct 24;314(1-2):229-33. PubMed PMID: 8957240.

4: Herth MM, Knudsen GM. Current radiosynthesis strategies for 5-HT2A receptor PET tracers. J Labelled Comp Radiopharm. 2015 Jun 15;58(7):265-73. doi: 10.1002/jlcr.3288. Epub 2015 May 22. Review. PubMed PMID: 25997728.

5: Millan MJ, Schreiber R, Monneyron S, Denorme B, Melon C, Queriaux S, Dekeyne A. S-16924, a novel, potential antipsychotic with marked serotonin1A agonist properties. IV. A drug discrimination comparison with clozapine. J Pharmacol Exp Ther. 1999 Apr;289(1):427-36. PubMed PMID: 10087034.

6: Kalkman HO, Neumann V, Nozulak J, Tricklebank MD. Cataleptogenic effect of subtype selective 5-HT receptor antagonists in the rat. Eur J Pharmacol. 1998 Feb 19;343(2-3):201-7. PubMed PMID: 9570468.

7: Stutzmann JM, Eon B, Darche F, Lucas M, Rataud J, Piot O, Blanchard JC, Laduron PM. Are 5-HT2 antagonists endowed with anxiolytic properties in rodents? Neurosci Lett. 1991 Jul 8;128(1):4-8. PubMed PMID: 1681477.

8: De Castro E Silva E, Ferreira H, Cunha M, Bulcão C, Sarmento C, De Oliveira I, Fregoneze JB. Effect of central acute administration of cadmium on drinking behavior. Pharmacol Biochem Behav. 1996 Mar;53(3):687-93. PubMed PMID: 8866973.

9: Setem J, Pinheiro AP, Motta VA, Morato S, Cruz AP. Ethopharmacological analysis of 5-HT ligands on the rat elevated plus-maze. Pharmacol Biochem Behav. 1999 Mar;62(3):515-21. PubMed PMID: 10080245.

10: López-Giménez JF, Vilaró MT, Palacios JM, Mengod G. [3H]MDL 100,907 labels 5-HT2A serotonin receptors selectively in primate brain. Neuropharmacology. 1998 Sep;37(9):1147-58. PubMed PMID: 9833645.

11: Fink G, Sumner BE. Oestrogen and mental state. Nature. 1996 Sep 26;383(6598):306. PubMed PMID: 8848040.

12: 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. PubMed PMID: 1579785.

13: López-Giménez JF, Mengod G, Palacios JM, Vilaró MT. Selective visualization of rat brain 5-HT2A receptors by autoradiography with [3H]MDL 100,907. Naunyn Schmiedebergs Arch Pharmacol. 1997 Oct;356(4):446-54. PubMed PMID: 9349630.

14: Sumner BE, Fink G. Testosterone as well as estrogen increases serotonin2A receptor mRNA and binding site densities in the male rat brain. Brain Res Mol Brain Res. 1998 Aug 31;59(2):205-14. PubMed PMID: 9729388.

15: Besret L, Dauphin F, Huard C, Lasne MC, Vivet R, Mickala P, Barbelivien A, Baron JC. Specific in vivo binding in the rat brain of [18F]RP 62203: a selective 5-HT2A receptor radioligand for positron emission tomography. Nucl Med Biol. 1996 Feb;23(2):169-71. PubMed PMID: 8868290.

16: Godbout R, Mantz J, Glowinski J, Thierry AM. The novel 5-HT2 receptor antagonist, RP 62203, selectively blocks serotoninergic but not dopaminergic-induced inhibition in the rat prefrontal cortex. Eur J Pharmacol. 1991 Oct 29;204(1):97-100. PubMed PMID: 1666564.

17: Malgouris C, Flamand F, Doble A. Autoradiographic studies of RP 62203, a potent 5-HT2 receptor antagonist. Pharmacological characterization of [3H]RP 62203 binding in the rat brain. Eur J Pharmacol. 1993 Mar 16;233(1):37-45. PubMed PMID: 8472747.

18: Newman-Tancredi A, Audinot V, Chaput C, Verrièle L, Millan MJ. [35S]Guanosine-5'-O-(3-thio)triphosphate binding as a measure of efficacy at human recombinant dopamine D4.4 receptors: actions of antiparkinsonian and antipsychotic agents. J Pharmacol Exp Ther. 1997 Jul;282(1):181-91. PubMed PMID: 9223553.

19: Hashimoto K, Narita N, Tomitaka S, Iyo M, Minabe Y. In vivo regulation of serotonin 5-HT2A receptors in rat brain by subchronic administration of sigma receptor ligand NE-100. Life Sci. 1997;60(24):2245-54. PubMed PMID: 9188767.

20: Di Matteo V, Di Giovanni G, Di Mascio M, Esposito E. Selective blockade of serotonin2C/2B receptors enhances dopamine release in the rat nucleus accumbens. Neuropharmacology. 1998;37(2):265-72. PubMed PMID: 9680252.

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