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ChemicalBook Optimization Suppliers |
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| 融点 | 141-143?C | | 比旋光度 | D23 +16.0° (c = 1 in CH3OH) | | 沸点 | 536.4±50.0 °C(Predicted) | | 比重(密度) | 1.120±0.06 g/cm3(Predicted) | | 闪点 | 2℃ | | 貯蔵温度 | Refrigerator | | 溶解性 | DMF: 20 mg/ml; DMSO: 20 mg/ml; Ethanol: 20 mg/ml; PBS (pH 7.2): 2 mg/ml | | 外見 | A crystalline solid | | 酸解離定数(Pka) | 14.19±0.46(Predicted) | | InChIKey | VPPJLAIAVCUEMN-GFCCVEGCSA-N | | CAS データベース | 175481-36-4 |
| | ラコサミド Usage And Synthesis |
| 効能 | 抗てんかん薬, 疼痛治療 (神経因性) | | 商品名 | ビムパット (ユーシービージャパン); ビムパット (ユーシービージャパン); ビムパット (ユーシービージャパン) | | 説明 | Although epilepsy is a neurological disorder with varying etiology and
severity, the common feature is unprovoked, recurring seizures. Whether
classified as generalized, involving both cerebral hemispheres, or partial
with only localized portions of brain participation at onset, effective
treatment relies on accurate assessment of syndrome type to optimally
decrease the frequency, duration, and severity of seizures. The
latest weapon against partial onset epilepsy is lacosamide, formerly
known as harkoseride and erlosamide. The data also indicate that lacosamide
binds to collapsing response mediator protein 2 (CRMP2); CRMP2 is
involved in neuronal differentiation, control of axonal outgrowth, and
possibly epileptogenesis. Furthermore, lacosamide is heralded as having
a dual mode of action as it has also displayed efficacy against diabetic
neuropathy, possibly as a result of stabilization of neuronal hyperexcitability. Currently,lacosamide is approved as adjunctive treatment of partial onset seizures in patients 17 years or older and is in development as a monotherapy
for epilepsy and for neuropathic pain. | | 説明 | Lacosamide selectively enhances sodium channel slow inactivation without affecting fast inactivation. It is effective in multiple rodent models of seizure activity. The neuroprotective effects of lacosamide are also attributed to its ability to modulate collapsin response mediator protein 2 (CRMP-2), a member of the semaphorin signal transduction pathway. Formulations containing lacosamide have been used as an adjunctive or monotherapy for focal-onset seizures but, at higher doses, have a low potential for abuse. Lacosamide is regulated as a Schedule V compound in the United States. | | 化学的特性 | White to Off-White Solid | | Originator | Harris FRC (United States) | | 使用 | A potent anticonvulsant. | | 定義 | ChEBI: Lacosamide is a N-acyl-amino acid. | | brand name | Vimpat | | 合成 | The most common adverse events were diplopia, headache, dizziness, and nausea. As typical with AEDs, lacosamide may increase the risk of suicidal thoughts or behavior. Patients should, therefore, be monitored for the emergence or worsening of depression. Caution should also be exercised in patients with known conduction problems or severe cardiac disease (myocardial ischemia or heart failure) since dose-dependent prolongations in PR interval have been observed in clinical studies. |
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