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MedKoo Cat#: 527842 | Name: Spiperone HCl
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Description:

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

Spiperone HCl is a 5-HT2A serotonin and selective D2-like dopamine receptor antagonist.

Chemical Structure

Spiperone HCl
Spiperone HCl
CAS#2022-29-9 (HCl)

Theoretical Analysis

MedKoo Cat#: 527842

Name: Spiperone HCl

CAS#: 2022-29-9 (HCl)

Chemical Formula: C23H27ClFN3O2

Exact Mass: 0.0000

Molecular Weight: 431.94

Elemental Analysis: C, 63.96; H, 6.30; Cl, 8.21; F, 4.40; N, 9.73; O, 7.41

Price and Availability

Size Price Availability Quantity
50mg USD 200.00
250mg USD 350.00
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Related CAS #
749-02-0 (free base)
Synonym
Spiperone HCl; NSC 170983; R 5147; Spiperone; Spiroperidol; Spiroperidone; Spiropitan;
IUPAC/Chemical Name
8-[4-(4-Fluorophenyl)-4-oxobutyl]-1-phenyl-1,3,8-triazaspiro[4,5]decan-4-one hydrochloride
InChi Key
QUIKMLCZZMOBLH-UHFFFAOYSA-N
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
SMILES Code
O=C1NCN(C2=CC=CC=C2)C13CCN(CCCC(C4=CC=C(F)C=C4)=O)CC3.[H]Cl
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
>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
Product Data
Product Data
Instruction
View handling instruction
Biological target:
Spiperone HCl is a 5-HT2A serotonin and selective D2-like dopamine receptor antagonist (Ki values are 0.06, 0.6, 0.08, ~ 350, ~ 3500 nM for D2, D3, D4, D1 and D5 receptors respectively).
In vitro activity:
The findings of this study suggest that antipsychotics decrease dopamine release by reducing vesicular dopamine content. In PC12 cells, spiperone, haloperidol, pimozide, aripiprazole, and risperidone inhibited high potassium-evoked dopamine release. Spiperone, haloperidol, pimozide, aripiprazole, and reserpine transiently increased extracellular levels of dopamine metabolites. Additionally, spiperone, haloperidol, pimozide, aripiprazole, and risperidone reduced intracellular dopamine levels. Reference: BMC Pharmacol. 2009 Nov 30;9:13. https://pubmed.ncbi.nlm.nih.gov/20460122/
In vivo activity:
In a murine model of chronic obstructive pulmonary disease (COPD), results suggest that spiperone mediated endothelial regeneration and could be a novel therapeutic approach for treatment of emphysema associated with COPD. Spiperone increased the number of capillaries and the expression of the CD31 in the alveolar tissue. Spiperone prevented alveolar wall destruction and reduced the area of emphysema. Reference: Int J Chron Obstruct Pulmon Dis. 2021 Dec 30;16:3575-3591. https://pubmed.ncbi.nlm.nih.gov/35002229/
Solvent mg/mL mM comments
Solubility
DMSO 125.0 289.40
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 431.94 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.

Recalculate based on batch purity %
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:
1. Matsuo T, Izumi Y, Wakita S, Kume T, Takada-Takatori Y, Sawada H, Akaike A. Haloperidol, spiperone, pimozide and aripiprazole reduce intracellular dopamine content in PC12 cells and rat mesencephalic cultures: Implication of inhibition of vesicular transport. Eur J Pharmacol. 2010 Aug 25;640(1-3):68-74. doi: 10.1016/j.ejphar.2010.04.043. Epub 2010 May 9. PMID: 20460122. 2. Lu D, Carson DA. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. BMC Pharmacol. 2009 Nov 30;9:13. doi: 10.1186/1471-2210-9-13. PMID: 19948059; PMCID: PMC2789054. 3. Skurikhin E, Pershina O, Zhukova M, Widera D, Pan E, Pakhomova A, Krupin V, Ermakova N, Skurikhina V, Sandrikina L, Morozov S, Kubatiev A, Dygai A. Spiperone Stimulates Regeneration in Pulmonary Endothelium Damaged by Cigarette Smoke and Lipopolysaccharide. Int J Chron Obstruct Pulmon Dis. 2021 Dec 30;16:3575-3591. doi: 10.2147/COPD.S336410. PMID: 35002229; PMCID: PMC8722540. 4. Skurikhin EG, Khmelevskaya ES, Ermakova NN, Pershina OV, Reztsova AM, Krupin VA, Stepanova IE, Reztsova VM, Reikhart DV, Dygai AM. Effect of spiperone on mesenchymal multipotent stromal and hemopoietic stem cells under conditions of pulmonary fibrosis. Bull Exp Biol Med. 2014 May;157(1):132-7. doi: 10.1007/s10517-014-2508-y. Epub 2014 Jun 11. PMID: 24913578.
In vitro protocol:
1. Matsuo T, Izumi Y, Wakita S, Kume T, Takada-Takatori Y, Sawada H, Akaike A. Haloperidol, spiperone, pimozide and aripiprazole reduce intracellular dopamine content in PC12 cells and rat mesencephalic cultures: Implication of inhibition of vesicular transport. Eur J Pharmacol. 2010 Aug 25;640(1-3):68-74. doi: 10.1016/j.ejphar.2010.04.043. Epub 2010 May 9. PMID: 20460122. 2. Lu D, Carson DA. Spiperone enhances intracellular calcium level and inhibits the Wnt signaling pathway. BMC Pharmacol. 2009 Nov 30;9:13. doi: 10.1186/1471-2210-9-13. PMID: 19948059; PMCID: PMC2789054.
In vivo protocol:
1. Skurikhin E, Pershina O, Zhukova M, Widera D, Pan E, Pakhomova A, Krupin V, Ermakova N, Skurikhina V, Sandrikina L, Morozov S, Kubatiev A, Dygai A. Spiperone Stimulates Regeneration in Pulmonary Endothelium Damaged by Cigarette Smoke and Lipopolysaccharide. Int J Chron Obstruct Pulmon Dis. 2021 Dec 30;16:3575-3591. doi: 10.2147/COPD.S336410. PMID: 35002229; PMCID: PMC8722540. 2. Skurikhin EG, Khmelevskaya ES, Ermakova NN, Pershina OV, Reztsova AM, Krupin VA, Stepanova IE, Reztsova VM, Reikhart DV, Dygai AM. Effect of spiperone on mesenchymal multipotent stromal and hemopoietic stem cells under conditions of pulmonary fibrosis. Bull Exp Biol Med. 2014 May;157(1):132-7. doi: 10.1007/s10517-014-2508-y. Epub 2014 Jun 11. PMID: 24913578.
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