WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H317897
CAS#: 1841-19-6
Description: Fluspirilene is a diphenylbutylpiperidine typical antipsychotic drug, used for the treatment of schizophrenia. It is administered intramuscularly.
Hodoodo Cat#: H317897
Name: Fluspirilene
CAS#: 1841-19-6
Chemical Formula: C29H31F2N3O
Exact Mass: 475.24
Molecular Weight: 475.573
Elemental Analysis: C, 73.24; H, 6.57; F, 7.99; N, 8.84; O, 3.36
Synonym: Fluspirilene, Redeptin, Imap, R6218, Spirodiflamine
IUPAC/Chemical Name: 8-[4,4-bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
InChi Key: QOYHHIBFXOOADH-UHFFFAOYSA-N
InChi Code: InChI=1S/C29H31F2N3O/c30-24-12-8-22(9-13-24)27(23-10-14-25(31)15-11-23)7-4-18-33-19-16-29(17-20-33)28(35)32-21-34(29)26-5-2-1-3-6-26/h1-3,5-6,8-15,27H,4,7,16-21H2,(H,32,35)
SMILES Code: O=C1NCN(C2=CC=CC=C2)C13CCN(CCCC(C4=CC=C(F)C=C4)C5=CC=C(F)C=C5)CC3
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, not in water
Shelf Life: >2 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: 2934.99.9001
More Info:
Biological target: | |
In vitro activity: | |
In vivo activity: |
The following data is based on the product molecular weight 475.57 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: |
1: Patil SP, Pacitti MF, Gilroy KS, Ruggiero JC, Griffin JD, Butera JJ, Notarfrancesco JM, Tran S, Stoddart JW. Identification of antipsychotic drug fluspirilene as a potential p53-MDM2 inhibitor: a combined computational and experimental study. J Comput Aided Mol Des. 2015 Feb;29(2):155-63. doi: 10.1007/s10822-014-9811-6. Epub 2014 Nov 7. PubMed PMID: 25377899.
2: Shi XN, Li H, Yao H, Liu X, Li L, Leung KS, Kung HF, Lu D, Wong MH, Lin MC. In Silico Identification and In Vitro and In Vivo Validation of Anti-Psychotic Drug Fluspirilene as a Potential CDK2 Inhibitor and a Candidate Anti-Cancer Drug. PLoS One. 2015 Jul 6;10(7):e0132072. doi: 10.1371/journal.pone.0132072. eCollection 2015. PubMed PMID: 26147897; PubMed Central PMCID: PMC4493148.
3: Wang SJ. Inhibition of glutamate release by fluspirilene in cerebrocortical nerve terminals (synaptosomes). Synapse. 2002 Apr;44(1):36-41. PubMed PMID: 11842444.
4: Kuhn W, Wöhrle M, Müller T, Welter F. [Fluspirilene--safe weekly tranquilizer?]. Nervenarzt. 1997 Jun;68(6):528. German. PubMed PMID: 9312689.
5: Wang SJ, Lu KT, Gean PW. Inhibition of synaptic transmission and epileptiform activity in central neurones by fluspirilene. Br J Pharmacol. 1997 Mar;120(6):1114-8. PubMed PMID: 9134224; PubMed Central PMCID: PMC1564570.
6: Grantham CJ, Main MJ, Cannell MB. Fluspirilene block of N-type calcium current in NGF-differentiated PC12 cells. Br J Pharmacol. 1994 Feb;111(2):483-8. PubMed PMID: 8004393; PubMed Central PMCID: PMC1909950.
7: Kappler J, Menges C, Ferbert A, Ebel H. [Severe "late" dystonia after neuroleptic anxiolysis with fluspirilene]. Nervenarzt. 1994 Jan;65(1):66-8. German. PubMed PMID: 8145878.
8: Tegeler J, Lehmann E, Weiher A, Heinrich K. Safety of long-term neuroleptanxiolysis with fluspirilene 1.5 mg per week. Pharmacopsychiatry. 1990 Nov;23(6):259-64. PubMed PMID: 2284327.
9: Kenny BA, Fraser S, Kilpatrick AT, Spedding M. Selective antagonism of calcium channel activators by fluspirilene. Br J Pharmacol. 1990 Jun;100(2):211-6. PubMed PMID: 1696149; PubMed Central PMCID: PMC1917424.
10: Contreras PC, Bremer ME, Rao TS. GBR-12909 and fluspirilene potently inhibited binding of [3H] (+)3-PPP to sigma receptors in rat brain. Life Sci. 1990;47(22):PL133-7. PubMed PMID: 1980329.
11: Skopová J, Faltus F, Filip V, Jirák R, Karen P, Posmurová M, Dobiásová A. [Fluspirilene in schizophrenia maintenance therapy and its interaction with dexetimide]. Cesk Psychiatr. 1985 Dec;81(6):414-9. Czech. PubMed PMID: 3912068.
12: Lehmann E, Hassel P, Thörner GW, Karrass W. [Alternative therapy concept for the treatment of psychosomatic disorders. Controlled double-blind evaluation of fluspirilene versus bromazepam]. Fortschr Med. 1984 Oct 25;102(40):1033-6. German. PubMed PMID: 6149989.
13: Brumback RA, Staton RD. Fluspirilene neuroleptic depot injections and indurations. Can J Psychiatry. 1984 Mar;29(2):184-5. PubMed PMID: 6722713.
14: Thilmann J. [Leading symptom of anxiety and tension and its concomitant somatic manifestations. A multicenter trial of fluspirilene versus bromazepam]. Fortschr Med. 1983 Oct 6;101(37):1676-8. German. PubMed PMID: 6139327.
15: McGee HM, Seeman MV, Deck JH. Fluspirilene neuroleptic depot injections and indurations. Can J Psychiatry. 1983 Aug;28(5):379-81. PubMed PMID: 6627197.
16: Giannelli A, Zarattini F. [New long-acting treatment of anxiety and its different forms of somatization: low-dose fluspirilene]. Minerva Med. 1983 Mar 31;74(13):727-33. Italian. PubMed PMID: 6835561.
17: Russell N, Landmark J, Merskey H, Turpin T. A double-blind comparison of fluspirilene and fluphenazine decanoate in schizophrenia. Can J Psychiatry. 1982 Nov;27(7):593-6. PubMed PMID: 7172160.
18: Kalis D, Ten Oever GH, Erdmann JF. Fluspirilene (Imap) in the treatment of psychosomatic complaints in hypochondriacal patients. Acta Psychiatr Belg. 1980 May-Jun;80(3):321-8. PubMed PMID: 7211423.
19: McCreadie RG, Kiernan WE, Venner RM, Denholm RB. Probable toxic necrosis after prolonged fluspirilene administration. Br Med J. 1979 Feb 24;1(6162):523-4. PubMed PMID: 444867; PubMed Central PMCID: PMC1598079.
20: Börger J, Van Epen JH, Dekkers A. A double-blind clinical evaluation of different dose intervals with fluspirilene (IMAP). Acta Psychiatr Belg. 1978 Mar-Apr;78(2):383-91. PubMed PMID: 354325.