Spiperone (hydrochloride)

Spiperone hydrochloride (Spiroperidol hydrochloride) is a selective dopamine D2 receptor (Ki values of 0.06 nM, 0.6 nM, 0.08 nM, ~350 nM, ~3500 nM for D2, D3, D4, D1 and D5 receptors, respectively) and 5-HT2A/5-HT1A receptor (Kis of 1 nM/49 nM) antagonist. Spiperone hydrochloride is also a selective α1B-adrenoceptor antagonist. Spiperone hydrochloride activates calcium-activated chloride channel (CaCC) . Antipsychotic and anti-inflammatory activities[1][2][3][4][5].

Product Specifications

CAS Number

[2022-29-9]

Product Name Alternative

Spiroperidol (hydrochloride)

UNSPSC

12352005

Target

5-HT Receptor; Adrenergic Receptor; Chloride Channel; Dopamine Receptor

Type

Reference compound

Related Pathways

GPCR/G Protein; Membrane Transporter/Ion Channel; Neuronal Signaling

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Neurological Disease

Assay Protocol

https://www.medchemexpress.com/spiperone-hydrochloride.html

Purity

99.10

Solubility

DMSO : 100 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

O=C1NCN(C2=CC=CC=C2)C13CCN(CCCC(C4=CC=C(F)C=C4)=O)CC3.[H]Cl

Molecular Formula

C23H27ClFN3O2

Molecular Weight

431.93

References & Citations

[1]P Seeman, et al. Dopamine receptor pharmacology. Trends Pharmacol Sci. 1994 Jul;15 (7) :264-70.|[2]Lihua Liang, et al. Spiperone, identified through compound screening, activates calcium-dependent chloride secretion in the airway. Am J Physiol Cell Physiol. 2009 Jan;296 (1) :C131-41.|[3]Long Tai Zheng, et al. The antipsychotic spiperone attenuates inflammatory response in cultured microglia via the reduction of proinflammatory cytokine expression and nitric oxide production. J Neurochem. 2008 Dec;107 (5) :1225-35.|[4]Richard A Glennon, et al. Ketanserin and spiperone as templates for novel serotonin 5-HT (2A) antagonists. Curr Top Med Chem. 2002 Jun;2 (6) :539-58.|[5]Andrea E Errasti, et al. Human umbilical vein vasoconstriction induced by epinephrine acting on alpha1B-adrenoceptor subtype. Am J Obstet Gynecol. 2003 Nov;189 (5) :1472-80.|[6]E G Skurikhin, et al. 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.