product name Lomerizine HCl
Description: Lomerizine (also known as KB-2796) dihydrochloride is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine. Lomerizine (0.1 μM and 1 μM) significantly reduces glutamate-induced neurotoxicity in rat cultured retinal neurons. Lomerizine (1 μM) also exhibits protective effects against both the N-methyl-D-aspartate and kainate induced types of neurotoxicity in rat cultured retinal neurons.
References: Exp Eye Res. 2000 Apr;70(4):475-84; Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5456-62; Exp Neurol. 2009 Mar;216(1):219-30.
541.46
Formula
C27H30F2N2O3.2HCl
CAS No.
101477-54-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (184.7 mM)
Water: <1 mg/mL
Ethanol: 52 mg/mL warmed (96.0 mM)
Solubility (In vivo)
2% DMSO+ddH2O: 5mg/mL
Synonyms
KB-2796
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403903
| In Vitro |
In vitro activity: Lomerizine (0.1 μM and 1 μM) significantly reduces glutamate-induced neurotoxicity in rat cultured retinal neurons. Lomerizine (1 μM) also exhibits protective effects against both the N-methyl-D-aspartate and kainate induced types of neurotoxicity in rat cultured retinal neurons. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Lomerizine (0.1 mg/kg and 1 mg/kg, i.v.) prior to ischemia and again immediately after reperfusion dose-dependently reduces the retinal damage in rat retina. Lomerizine (30 mg/kg, oral) reduces secondary necrosis at 2 weeks and secondary caspase-3 expression at 3 weeks in adult Piebald-Virol-Glaxo (PVG) rats. Lomerizine (30 mg/kg, oral) reduces morphological disruption, oxidative stress and phosphacan expression, and limits early increases in macrophage numbers in female PVG Hooded rats. Lomerizine (30 mg/kg, oral) protects RGCs from secondary death at 4 weeks but does not fully restore behavioural function (optokinetic nystagmus) in female PVG Hooded rats. Lomerizine (0.1 mg/kg or 0.3 mg/kg) significantly increases blood flow in the rabbit retina and optic nerve head (ONH), but blood flow changed little in the choroid or iris-ciliary body. Lomerizine (0.1 and 0.3 mg/kg, i.v.) significantly increases tissue blood flow in the optic nerve head and the putative blood flow in the long posterior ciliary artery with smaller reduction of blood pressure (0.3 mg/kg, i.v.) and without change in heart rate in rabbit. Lomerizine (0.1 and 0.3 mg/kg, i.v.) inhibits the hypoperfusion in the optic nerve head of rabbit. |
| Animal model | |
| Formulation & Dosage | |
| References | Exp Eye Res. 2000 Apr;70(4):475-84; Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5456-62; Exp Neurol. 2009 Mar;216(1):219-30. |
Related Posts
product name Lomerizine HCl
Description: Lomerizine (also known as KB-2796) dihydrochloride is a relatively new L- and T-type calcium channel blocker used in the treatment of migraine. Lomerizine (0.1 μM and 1 μM) significantly reduces glutamate-induced neurotoxicity in rat cultured retinal neurons. Lomerizine (1 μM) also exhibits protective effects against both the N-methyl-D-aspartate and kainate induced types of neurotoxicity in rat cultured retinal neurons.
References: Exp Eye Res. 2000 Apr;70(4):475-84; Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5456-62; Exp Neurol. 2009 Mar;216(1):219-30.
541.46
Formula
C27H30F2N2O3.2HCl
CAS No.
101477-54-7
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (184.7 mM)
Water: <1 mg/mL
Ethanol: 52 mg/mL warmed (96.0 mM)
Solubility (In vivo)
2% DMSO+ddH2O: 5mg/mL
Synonyms
KB-2796
other peoduct :References PubMed ID：:http://www.ncbi.nlm.nih.gov/pubmed/19403903
| In Vitro |
In vitro activity: Lomerizine (0.1 μM and 1 μM) significantly reduces glutamate-induced neurotoxicity in rat cultured retinal neurons. Lomerizine (1 μM) also exhibits protective effects against both the N-methyl-D-aspartate and kainate induced types of neurotoxicity in rat cultured retinal neurons. Kinase Assay: Cell Assay: |
|---|---|
| In Vivo | Lomerizine (0.1 mg/kg and 1 mg/kg, i.v.) prior to ischemia and again immediately after reperfusion dose-dependently reduces the retinal damage in rat retina. Lomerizine (30 mg/kg, oral) reduces secondary necrosis at 2 weeks and secondary caspase-3 expression at 3 weeks in adult Piebald-Virol-Glaxo (PVG) rats. Lomerizine (30 mg/kg, oral) reduces morphological disruption, oxidative stress and phosphacan expression, and limits early increases in macrophage numbers in female PVG Hooded rats. Lomerizine (30 mg/kg, oral) protects RGCs from secondary death at 4 weeks but does not fully restore behavioural function (optokinetic nystagmus) in female PVG Hooded rats. Lomerizine (0.1 mg/kg or 0.3 mg/kg) significantly increases blood flow in the rabbit retina and optic nerve head (ONH), but blood flow changed little in the choroid or iris-ciliary body. Lomerizine (0.1 and 0.3 mg/kg, i.v.) significantly increases tissue blood flow in the optic nerve head and the putative blood flow in the long posterior ciliary artery with smaller reduction of blood pressure (0.3 mg/kg, i.v.) and without change in heart rate in rabbit. Lomerizine (0.1 and 0.3 mg/kg, i.v.) inhibits the hypoperfusion in the optic nerve head of rabbit. |
| Animal model | |
| Formulation & Dosage | |
| References | Exp Eye Res. 2000 Apr;70(4):475-84; Invest Ophthalmol Vis Sci. 2009 Nov;50(11):5456-62; Exp Neurol. 2009 Mar;216(1):219-30. |