DC Chemicals Limited
China
Product Name: Fluspirilene (R 6218; Redeptin)
Price: $Inquiry/100mg $Inquiry/250mg $Inquiry/1g
Purity: 98.0%
Stocking Period: 3 Day
Contact: Tony Cao

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	Signaling Pathways >> Membrane Transporter/Ion Channel >> Calcium Channel Research Areas >> Neurological Disease
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

1841-17-4 structure

1841-17-4

~97%

1841-19-6 structure

1841-19-6

Literature: Schmidt, Andreas; Marchetti, Mauro; Eilbracht, Peter Tetrahedron, 2004 , vol. 60, # 50 p. 11487 - 11492

57668-61-8 structure

57668-61-8

1021-25-6 structure

1021-25-6

~68%

1841-19-6 structure

1841-19-6

Literature: Botteghi, Carlo; Marchetti, Mauro; Paganelli, Stefano; Persi-Paoli, Francesco Tetrahedron, 2001 , vol. 57, # 8 p. 1631 - 1637

345-92-6 structure

345-92-6

~%

1841-19-6 structure

1841-19-6

Literature: Tetrahedron, , vol. 60, # 50 p. 11487 - 11492

99734-06-2 structure

99734-06-2

~%

1841-19-6 structure

1841-19-6

Literature: Tetrahedron, , vol. 60, # 50 p. 11487 - 11492

817642-33-4 structure

817642-33-4

~%

1841-19-6 structure

1841-19-6

Literature: Tetrahedron, , vol. 60, # 50 p. 11487 - 11492

357-77-7 structure

357-77-7

~%

1841-19-6 structure

1841-19-6

Literature: Tetrahedron, , vol. 57, # 8 p. 1631 - 1637

293729-65-4 structure

293729-65-4

~%

1841-19-6 structure

1841-19-6

Literature: Tetrahedron, , vol. 57, # 8 p. 1631 - 1637

337506-83-9 structure

337506-83-9

~%

1841-19-6 structure

1841-19-6

Literature: Tetrahedron, , vol. 57, # 8 p. 1631 - 1637

50337-85-4 structure

50337-85-4

~%

1841-19-6 structure

1841-19-6

Literature: Tetrahedron, , vol. 57, # 8 p. 1631 - 1637

Precursor 8
57668-61-8 1021-25-6 345-92-6 817642-33-4
357-77-7 293729-65-4 337506-83-9 50337-85-4
DownStream 0

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%