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Formula | C9H7Cl2N5 |
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Molecular Weight | 256.09 | CAS No. | 84057-84-1 | ||||
Solubility (25°C)* | In vitro | DMSO | 10 mg/mL (39.04 mM) | ||||
Ethanol | 3 mg/mL (11.71 mM) | ||||||
Water | Insoluble | ||||||
In vivo (Add solvents to the product individually and in order) |
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* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
Description | Lamotrigine (BW-430C,LTG) is a novel anticonvulsant drug for inhibition of 5-HT with IC50 of 240 μM and 474 μM in human platelets and rat brain synaptosomes, and also is a sodium channel blocker. | ||||||
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Targets |
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In vitro | Lamotrigine stabilises presynaptic neuronal membranes by blockade of voltage-dependent sodium channels, thus preventing the release of excitatory neurotransmitters, particularly glutamate and aspartate. [1] In rat cerebral cortex tissue incubated with veratrine 10 mg/L, lamotrigine is twice as potent in inhibiting the release of glutamate and aspartate (ED 50 = 5.38 mg/L for each) than the release of GABA (ED50 = 11.2 mg/L), and is much less potent in inhibiting acetylcholine release (ED50 = 25.6 mg/L) when cortical slices is exposed to veratrine 75 mg/L. Basal glutamate release is unaffected . [2]Lamotrigine inhibits high-frequency sustained repetitive firing of sodium-dependent action potentials, indicating a direct effect on voltage-activated sodium channels. [3] Lamotrigine does not induce PCP-like central nervous system (CNS) effects, does not act by direct inhibition at the NMDA receptor, and would be expected to be devoid of the undesirable effects associated with NMDA blockade. [4] |
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In vivo | In mice and rats, lamotrigine prevents MES- and pentetrazol-induced hindlimb extension, suggesting an antiepileptic profile in animals. These effects peak 1 hour after lamotrigine administration and persist for more than 24 hours. [4] Lamotrigine is active in the electrically evoked EEG after-discharge test, which is thought to indicate activity against both simple and complex partial seizures. After-discharge duration is reduced dose-dependently by lamotrigine in rats at intravenous doses >5 mg/kg. [5] |
Animal Study: |
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Neuronal hyperexcitability drives central and peripheral nervous system tumor progression in models of neurofibromatosis-1 [ Nat Commun, 2022, 13(1):2785] | PubMed: 35589737 |
Establishment and Characterization of NCC-PMP1-C1: A Novel Patient-Derived Cell Line of Metastatic Pseudomyxoma Peritonei [ J Pers Med, 2022, 12(2)258] | PubMed: 35207746 |
Establishment and characterization of NCC-UPS4-C1: a novel cell line of undifferentiated pleomorphic sarcoma from a patient with Li-Fraumeni syndrome [ Hum Cell, 2022, 10.1007/s13577-022-00671-y] | PubMed: 35118583 |
Establishment and characterization of the NCC-GCTB4-C1 cell line: a novel patient-derived cell line from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00639-4] | PubMed: 34731453 |
Establishment and characterization of NCC-MFS4-C1: a novel patient-derived cell line of myxofibrosarcoma [ Hum Cell, 2021, 34(6):1911-1918] | PubMed: 34383271 |
Establishment and characterization of novel patient-derived cell lines from giant cell tumor of bone [ Hum Cell, 2021, 10.1007/s13577-021-00579-z] | PubMed: 34304386 |
Establishment and characterization of patient-derived cancer models of malignant peripheral nerve sheath tumors. [ Cancer Cell Int, 2020, 19;20:58] | PubMed: 32099531 |
Establishment and characterization of a novel cell line, NCC-TGCT1-C1, derived from a patient with tenosynovial giant cell tumor [ Hum Cell, 2020, 10.1007/s13577-020-00425-8] | PubMed: 32886306 |
Establishment and characterization of NCC-MFS2-C1: a novel patient-derived cancer cell line of myxofibrosarcoma [ Hum Cell, 2020, 10.1007/s13577-020-00420-z] | PubMed: 32870449 |
Postictal behavioural impairments are due to a severe prolonged hypoperfusion/hypoxia event that is COX-2 dependent. [ Elife, 2016, 5] | PubMed: 27874832 |
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Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
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