A voltage-dependent calcium channel blocker
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Lomerizine (hydrochloride)

Item No. 28374

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
1-[bis(4-fluorophenyl)methyl]-4-[(2,3,4-trimethoxyphenyl)methyl]-piperazine, dihydrochloride
CAS Number
101477-54-7
Synonyms
  • KB-2796
Molecular Formula
C27H30F2N2O3 • 2HCl
Formula Weight
541.5
Purity
≥98%
Formulation
A crystalline solid
Solubility(Learn about Variance in Solubility)
DMF: 20 mg/mlDMSO: 20 mg/mlEthanol: 1 mg/ml
SMILES
COC1=CC=C(CN2CCN(C(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC2)C(OC)=C1OC.Cl.Cl
InChi Code
InChI=1S/C27H30F2N2O3.2ClH/c1-32-24-13-8-21(26(33-2)27(24)34-3)18-30-14-16-31(17-15-30)25(19-4-9-22(28)10-5-19)20-6-11-23(29)12-7-20;;/h4-13,25H,14-18H2,1-3H3;2*1H
InChi Key
LOGVKVSFYBBUAJ-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Wet ice in continental US; may vary elsewhere
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    100 mg

    $37

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    250 mg

    $75

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    500 mg

    $117

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    1 g

    $209

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    Product Description

    Lomerizine is a voltage-dependent calcium channel blocker that inhibits low- and high-voltage activated calcium currents in rat hippocampal CA1 pyramidal neurons with IC50 values of 1.9 and 4 μM, respectively.1,2 It inhibits vasoconstriction induced by potassium chloride, serotonin (5-HT; Item No. 14332), or vasopressin in isolated rat basilar arteries when used at a concentration of 1 μM.1 Lomerizine (1 μM) reduces neurotoxicity induced by glutamate, NMDA, or kainate in rat retinal primary cell cultures.3 It reduces retinal damage in a rat model of retinal ischemia-reperfusion injury when administered at a dose of 1 mg/kg.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Ishii, M., Kobayashi, S., Ohkura, M., et al. Inhibitory effect of lomerizine, a prophylactic drug for migraines, on serotonin-induced contraction of the basilar artery. J. Pharmacol. Sci. 111(2), 221-225 (2009).

    2. Akaike, N., Ishibashi, H., Hara, H., et al. Effect of KB-2796, a new diphenylpiperazine Ca2+ antagonist, on voltage-dependent Ca2+ currents and oxidative metabolism in dissociated mammalian CNS neurons. Brain Res. 619(1-2), 263-270 (1993).

    3. Toriu, N., Akaike, A., Yasuyoshi, H., et al. Lomerizine, a Ca2+ channel blocker, reduces glutamate-induced neurotoxicity and ischemia/reperfusion damage in rat retina. Exp. Eye Res. 70(4), 475-484 (2000).