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Lidoflazine

From Wikipedia, the free encyclopedia
Chemical compound
Pharmaceutical compound
Lidoflazine
Clinical data
AHFS/Drugs.comInternational Drug Names
ATC code
Identifiers
  • 2-[4-[4,4-bis(4-fluorophenyl)butyl]piperazin-1-yl]-N-(2,6-dimethylphenyl)acetamide
CAS Number
PubChemCID
ChemSpider
UNII
KEGG
CompTox Dashboard(EPA)
ECHA InfoCard100.020.285Edit this at Wikidata
Chemical and physical data
FormulaC30H35F2N3O
Molar mass491.627 g·mol−1
3D model (JSmol)
Melting point159 to 161 °C (318 to 322 °F)
Solubility in waterAlmost insoluble in water(<0.01%); Very soluble in chloroform(>50%); mg/mL (20 °C)
  • CC1=C(C(=CC=C1)C)NC(=O)CN2CCN(CC2)CCCC(C3=CC=C(C=C3)F)C4=CC=C(C=C4)F
  • InChI=1S/C30H35F2N3O/c1-22-5-3-6-23(2)30(22)33-29(36)21-35-19-17-34(18-20-35)16-4-7-28(24-8-12-26(31)13-9-24)25-10-14-27(32)15-11-25/h3,5-6,8-15,28H,4,7,16-21H2,1-2H3,(H,33,36) ☒N
  • Key:ZBIAKUMOEKILTF-UHFFFAOYSA-N ☒N
 ☒NcheckY (what is this?)  (verify)

Lidoflazine is apiperazinecalcium channel blocker. It is a coronary vasodilator with some antiarrhythmic action.[1] Lidoflazine was discovered atJanssen Pharmaceutica in 1964. In 2025 Lidoflazine has also been reported to interact withtubulin and inhibit its polymerization.[2]


Physical properties

[edit]

Solubility at room temperature

[edit]

Extracted from[1]

Solvent0.01

N

0.1

N

%pH%pH
Hydrochloric Acid0.43.00.71.9
Tartaric Acid0.33.11.02.5
Citric Acid0.33.10.52.5
Lactic Acid0.23.40.72.9
Acetic Acid0.13.50.43.8

References

[edit]
  1. ^abSchaper WK, Xhoneux R, Jageneau AH, Janssen PA (May 1966)."The cardiovascular pharmacology of lidoflazine, a long-acting coronary vasodilator".The Journal of Pharmacology and Experimental Therapeutics.152 (2):265–274.doi:10.1016/S0022-3565(25)27319-0.PMID 5944369.
  2. ^Baksheeva VE, La Rocca R, Allegro D, Derviaux C, Pasquier E, Roche P, Morelli X, Devred F, Golovin AV, Tsvetkov PO (2025). "NanoDSF Screening for Anti-tubulin Agents Uncovers New Structure–Activity Insights".Journal of Medicinal Chemistry.doi:10.1021/acs.jmedchem.5c01008.

Further reading

[edit]
  • Schaper WK, Xhonneux R, Jageneau AH (November 1965). "Stimulation of the coronary collateral circulation by lidoflazine (R 7904)".Naunyn-Schmiedebergs Archiv für Experimentelle Pathologie und Pharmakologie.252 (1):1–8.doi:10.1007/bf00246424.PMID 4222721.S2CID 31959581.
Calcium
VDCCsTooltip Voltage-dependent calcium channels
Blockers
Activators
Potassium
VGKCsTooltip Voltage-gated potassium channels
Blockers
Activators
IRKsTooltip Inwardly rectifying potassium channel
Blockers
Activators
KCaTooltip Calcium-activated potassium channel
Blockers
Activators
K2PsTooltip Tandem pore domain potassium channel
Blockers
Activators
Sodium
VGSCsTooltip Voltage-gated sodium channels
Blockers
Activators
ENaCTooltip Epithelial sodium channel
Blockers
Activators
ASICsTooltip Acid-sensing ion channel
Blockers
Chloride
CaCCsTooltip Calcium-activated chloride channel
Blockers
Activators
CFTRTooltip Cystic fibrosis transmembrane conductance regulator
Blockers
Activators
Unsorted
Blockers
Others
TRPsTooltip Transient receptor potential channels
LGICsTooltip Ligand gated ion channels
Phenylpiperazines
Benzylpiperazines
Naphthylpiperazines
Quinolinylpiperazines
Diphenylalkylpiperazines
Pyrimidinylpiperazines
Pyridinylpiperazines
Benzo(iso)thiazolylpiperazines
Tricyclic-linked piperazines
Others/uncategorized

[1]


Stub icon

Thisdrug article relating to thecardiovascular system is astub. You can help Wikipedia byexpanding it.

  1. ^Zhou PZ, Babcock J, Liu LQ, Li M, Gao ZB (June 2011)."Activation of human ether-a-go-go related gene (hERG) potassium channels by small molecules".Acta Pharmacologica Sinica.32 (6):781–788.doi:10.1038/aps.2011.70.PMC 4085723.PMID 21623390.
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