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1841-19-6

1841-19-6 structure
1841-19-6 structure
  • Name: fluspirilene
  • Chemical Name: Fluspirilene
  • CAS Number: 1841-19-6
  • Molecular Formula: C29H31F2N3O
  • Molecular Weight: 475.573
  • Catalog: API Nervous system medication Antipsychotic
  • Create Date: 2018-07-18 14:26:11
  • Modify Date: 2024-01-02 15:12:06
  • Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.

Name Fluspirilene
Synonyms 8-[4,4-Bis(4-fluorophenyl)butyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one
fluspirilene
8-[4,4-bis(p-Fluorophenyl)butyl]-1-phenyl-1,3,8-triazino[4.5]decan-4-one,R 6218
8-[4,4-bis(p-Fluorophenyl)butyl]-1-phenyl-1,3,8-triazino[4.5]decan-4-one R 6218
1,3,8-Triazaspiro[4.5]decan-4-one, 8-[4,4-bis(4-fluorophenyl)butyl]-1-phenyl-
1,3,8-Triazaspiro(4.5)decan-4-one, 8-(4,4-bis(4-fluorophenyl)butyl)-1-phenyl-
Description Fluspirilene is a non-competitive antagonist of L-type calcium channels with an IC50 of 0.03 μM. Fluspirileneis a long-acting injectable depot antipsychotic drug used for schizophrenia.
Related Catalog
Target

IC50: 0.03 μM (L-type calcium channel)[1]

In Vitro Fluspirilene, at concentrations which non-competitively modify dihydropyridine binding, selectively antagonizes the effects of calcium-channel activators[1]. Fluspirilene decreases the viability and suppresses sphere-forming of glioma stem cell lines in a dose-dependent manner. Fluspirilene demonstrates the inhibition of proliferation of T98, U87 and all GSC lines at 1.25, 2.5, and 5 μM, while it inhibits the proliferation of U251 and SNB19 at 2.5 and 5 μM[2].
In Vivo Mice treated with fluspirilene shows a remarkable reduction of the tumor size. Fluspirilene significantly prolongs survival of the TGS04 mouse model[2].
Cell Assay To investigate the effect of fluspirilene on cell proliferation, cells are treated with 1.25, 2.5, and 5 μM of fluspirilene. GSC viability is assessed using a Cell Counting Kit-8[2].
Animal Admin Mice[2] The mice are randomly assigned to two groups and treated with either fluspirilene (n=5) or with DMSO as a control group (n=5). All mice are given intramuscular injections of 200 μL of DMSO or fluspirilene dissolved in DMSO at 1 mg/kg body weight four times[2].
References

[1]. Kenny BA, et al. Selective antagonism of calcium channel activators by fluspirilene. Br J Pharmacol. 1990 Jun;100(2):211-6.

[2]. Dong Y, et al. Identification of antipsychotic drug fluspirilene as a potential anti-glioma stem cell drug. Oncotarget. 2017 Dec 4;8(67):111728-111741.

Density 1.3±0.1 g/cm3
Boiling Point 668.9±55.0 °C at 760 mmHg
Melting Point 187.5-190°
Molecular Formula C29H31F2N3O
Molecular Weight 475.573
Flash Point 358.3±31.5 °C
Exact Mass 475.243530
PSA 35.58000
LogP 3.89
Appearance amorphous solid | white to yellow
Vapour Pressure 0.0±2.0 mmHg at 25°C
Index of Refraction 1.632
Storage condition room temp
Water Solubility DMSO: soluble

CHEMICAL IDENTIFICATION

RTECS NUMBER :
XX8750000
CHEMICAL NAME :
1,3,8-Triazaspiro(4.5)decan-4-one, 8-(4,4-bis(p-fluorophenyl)butyl)-1-phenyl-
CAS REGISTRY NUMBER :
1841-19-6
BEILSTEIN REFERENCE NO. :
0633853
LAST UPDATED :
199612
DATA ITEMS CITED :
5
MOLECULAR FORMULA :
C29-H31-F2-N3-O
MOLECULAR WEIGHT :
475.63
WISWESSER LINE NOTATION :
T6N DXTJ A3YR DF&R DF& D-& CT5MVXN EHJ DR

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :
TDLo - Lowest published toxic dose
ROUTE OF EXPOSURE :
Intravenous
SPECIES OBSERVED :
Human - man
DOSE/DURATION :
183 ug/kg
TOXIC EFFECTS :
Skin and Appendages - corrosive (after topical exposure)
REFERENCE :
BMJOAE British Medical Journal. (British Medical Assoc., BMA House, Tavistock Sq., London WC1H 9JR, UK) V.1- 1857- Volume(issue)/page/year: 1,523,1979
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - rat
DOSE/DURATION :
>146 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1689,1970
TYPE OF TEST :
LD50 - Lethal dose, 50 percent kill
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - mouse
DOSE/DURATION :
106 mg/kg
TOXIC EFFECTS :
Sense Organs and Special Senses (Eye) - ptosis Behavioral - somnolence (general depressed activity)
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1689,1970
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Mammal - dog
DOSE/DURATION :
>37 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1689,1970
TYPE OF TEST :
LDLo - Lowest published lethal dose
ROUTE OF EXPOSURE :
Intramuscular
SPECIES OBSERVED :
Rodent - guinea pig
DOSE/DURATION :
>80 mg/kg
TOXIC EFFECTS :
Details of toxic effects not reported other than lethal dose value
REFERENCE :
ARZNAD Arzneimittel-Forschung. Drug Research. (Editio Cantor Verlag, Postfach 1255, W-7960 Aulendorf, Fed. Rep. Ger.) V.1- 1951- Volume(issue)/page/year: 20,1689,1970
Personal Protective Equipment Eyeshields;Gloves;type N95 (US);type P1 (EN143) respirator filter
RIDADR UN 3249
WGK Germany 3
RTECS XX8750000
Packaging Group III
Hazard Class 6.1(b)
HS Code 2933990090
HS Code 2933990090
Summary 2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%