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Spiperone HCl (NSC-170983; E-525; R-5147; Spiroperidol) is a novel and potent antipsychotic agent acting as a dopamine D2, serotonin 5-HT1A, and serotonin 5-HT2A antagonist with the potential for neurology diseases.
| Targets |
D2 Receptor ( Ki = 0.06 nM ); D1 Receptor ( Ki ~350 nM ); D3 Receptor ( Ki = 0.6 nM ); D4 Receptor ( Ki = 0.08 nM ); D5 Receptor ( Ki ~ 3500 nM ); 5-HT2A Receptor ( Ki = 1 nM ); 5-HT1A Receptor ( Ki = 49 nM ); α1B-adrenoceptor; Calcium-activated chloride channel
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| ln Vitro |
Spiperone is a strong enhancer of intracellular Ca2+ (EC50=9.3 μM) that acts on intracellular Ca2+ via a pathway dependent on phospholipase C and coupled to protein tyrosine kinase. This causes increased Cl-secretion in Calu-3 and CFBE41o-cell monolayers[2].
Spiperone reduces nitric oxide production in primary astrocyte, primary microglia, and lipopolysaccharide-stimulated BV-2 microglia cells significantly. Additionally, nitric oxide production in primary microglia cultures stimulated with ATP is markedly inhibited by diperone. Spiperone significantly reduces the BV-2 microglia cells' ability to produce TNF-α. In BV-2 microglia cells, siperone reduces the mRNA expression of proinflammatory cytokines like TNF-α and IL-1β as well as inducible nitric oxide synthase[3]. |
| ln Vivo |
Spiperone (1.5 mg/kg; intraperitoneal injection; on days 1, 3, 6, 7, and 13-21; C57Bl/6 mice) treatment inhibits the growth of connective tissue in the parenchyma of Bleomycin lungs and decreases the infiltration of inflammatory cells into the alveolar ducts and alveolar interstitium[6].
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| Animal Protocol |
C57Bl/6 mice (7-8-week-old) induced pulmonary fibrosis by Bleomycin
1.5 mg/kg Intraperitoneal injection; on days 1, 3, 6, 7, and 13-21 |
| References |
| Molecular Formula |
C23H27CLFN3O2
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|---|---|
| Molecular Weight |
431.9364
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| Exact Mass |
431.18
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| Elemental Analysis |
C, 63.96; H, 6.30; Cl, 8.21; F, 4.40; N, 9.73; O, 7.41
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| CAS # |
2022-29-9
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| Related CAS # |
Spiperone; 749-02-0
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| Appearance |
Solid powder
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| SMILES |
C1CN(CCC12C(=O)NCN2C3=CC=CC=C3)CCCC(=O)C4=CC=C(C=C4)F.Cl
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| InChi Key |
QUIKMLCZZMOBLH-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C23H26FN3O2.ClH/c24-19-10-8-18(9-11-19)21(28)7-4-14-26-15-12-23(13-16-26)22(29)25-17-27(23)20-5-2-1-3-6-20;/h1-3,5-6,8-11H,4,7,12-17H2,(H,25,29);1H
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| Chemical Name |
8-[4-(4-fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4.5]decan-4-one;hydrochloride
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| Synonyms |
Spiperone HCl; Spiropitan; Spiperone; Spiroperidol; Spiroperidone; R-5147; NSC-170983
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: ~125 mg/mL (~289.4 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (4.82 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.82 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.08 mg/mL (4.82 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.3151 mL | 11.5757 mL | 23.1514 mL | |
| 5 mM | 0.4630 mL | 2.3151 mL | 4.6303 mL | |
| 10 mM | 0.2315 mL | 1.1576 mL | 2.3151 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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