1. Membrane Transporter/Ion Channel
  2. Calcium Channel

Lomerizine dihydrochloride (Synonyms: KB-2796)

Cat. No.: HY-B0768A Purity: 99.97%
Handling Instructions

Lomerizine dihydrochloride is an antagonist of L- and T-type voltagegated calcium channels.

For research use only. We do not sell to patients.

Lomerizine dihydrochloride Chemical Structure

Lomerizine dihydrochloride Chemical Structure

CAS No. : 101477-54-7

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 77 In-stock
Estimated Time of Arrival: December 31
50 mg USD 70 In-stock
Estimated Time of Arrival: December 31
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  • References

Description

Lomerizine dihydrochloride is an antagonist of L- and T-type voltagegated calcium channels.

IC50 & Target[1]

T-type calcium channel

 

L-type calcium channel

 

In Vitro

Lomerizine is an antagonist of L- and T-type voltagegated calcium channels and transient receptor potential channel 5 transient receptor potential channels. Lomerizine is a dual L/T-type channel blocker used for prophylaxis of migraine. To demonstrate the effectiveness of Lomerizine in limiting intracellular [Ca2+], its ability to inhibit glutamate-induced death of motor neurons and the associated rise in cytosolic [Ca2+] is evaluated. Lomerizine inhibits the low- and high-voltage activated Ca2+ currents in dissociated rat brain neurons at a threshold concentration of 0.01 μM and IC50 of 1.9 μM and H2O2-induced Ca2+ influx in hippocampal neurons is inhibited by 1 μM Lomerizine. Pre-treatment with 1 μM Lomerizine significantly reduces acute death of motor neurons in spinal cord-DRG cultures exposed to 50 μM glutamate, a concentration that kills approximately 40% of motor neurons in the culture by 6 h, and inhibits the rise in cytosolic [Ca2+] that occurs with glutamate treatment. 0.5 μM Lomerizine is sufficient to significantly prevent the mitochondrial fragmentation of mitochondria induced by SOD1G93A[1]. Lomerizine increases the cytotoxicity of Adriamycin (ADM) and the apoptosis induced by ADM or Vincristine (VCR) in K562/ADM cells. At the concentration of 3, 10 and 30μM, Lomerizine reduces the IC50 value of ADM from 79.03 μM to 28.14, 8.16 and 3.16 μM, respectively. Lomerizine increases the intracellular accumulation of ADM and inhibits the efflux of Rh123 in K562/ ADM cells. No change in P-gp expression is observed after the treatment of Lomerizine for 72 h. Lomerizine has strong reversal effect on MDR in K562/ADM cells by inhibiting P-gp function[2].

In Vivo

To determine whether Ca2+ signaling molecules mediate NMDA-induced neurotoxicity in p50-deficient mice, the neuroprotective effects of chemical reagents are examined, which act on the Ca2+-signaling pathway including CaN activation, on NMDA-induced RGC death. The p50-deficient mice at 2 months of age, showing normal RGC survival, undergo intraperitoneal pretreatments with a NMDA antagonist, MK801 or Memantine; calcium blocker, Lomerizine; and CaN inhibitor, Tacrolimus, daily for 1 week before the injection of 5 nM NMDA. The chronic administration of Lomerizine or Tacrolimus to KO mice for 6 months results in an increase in surviving RGC numbers (p<0.0001)[3]. Lomerizine (KB-2796; 0.3 and 1 mg/kg, i.v.) dose-dependently increases cerebral blood flow significantly at 30 min and 15 min, respectively, after its administration. Lomerizine (1 mg/kg, i.v.) significantly attenuates the expression of c-Fos-like immunoreactivity in the ipsilateral frontoparietal cortex[4].

Solvent & Solubility
In Vitro: 

DMSO : 100 mg/mL (184.69 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8469 mL 9.2343 mL 18.4686 mL
5 mM 0.3694 mL 1.8469 mL 3.6937 mL
10 mM 0.1847 mL 0.9234 mL 1.8469 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Cell Assay
[2]

MTT assay is used to determine the influence of Lomerizine on the cytotoxicity of Adriamycin (ADM). The effect of Lomerizine (3, 10 and 30 μM) on the apoptosis induced by ADM and Vincristine (VCR) in K562/ADM cells is detected using flow cytometry. Intracellular accumulation of ADM is measured by fluorescence spectrophotometry. Flow cytometry is used to investigate the efflux of Rhodamine 123 (Rh123) and the expression of P-glycoprotein (P-gp) in K562/ADM cells[2].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3][4]

Mice[3]
The p50-deficient mice and wild-type mice aged 2 months are daily pre-treated intraperitoneally with Memantine (10 mg/kg), MK-801 (0.5 mg/kg), Lomerizine (1 mg/kg), or Tacrolimus (2, 0.5 and 0.2 mg/kg) for one week before the NMDA injection. These mice are given an intravitreous injection of 5 nM NMDA, which is a relatively low concentration for causing neurotoxicity[3].
Rats[4]
Male Wistar rats weighing 250 to 350 g are housed in an air-conditioned room at 25±0°C with 55±5% humidity and given food and water ad libitum. Lomerizine is injected i.v. in a volume of 1 mL/kg body weight. Effects of Lomerizine (0.3 mg/kg, i.v., or 1 mg/kg, i.v.) are measured on cerebral cortical blood flow measured by laser Doppler flowmetry (CBFLDF) in anaesthetized rats[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

541.46

Formula

C₂₇H₃₂Cl₂F₂N₂O₃

CAS No.

101477-54-7

SMILES

COC1=CC=C(CN2CCN(C(C3=CC=C(F)C=C3)C4=CC=C(F)C=C4)CC2)C(OC)=C1OC.[H]Cl.[H]Cl

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Lomerizine dihydrochloride
Cat. No.:
HY-B0768A
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Lomerizine dihydrochloride

Cat. No.: HY-B0768A