3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine
Lamotrigine
CAS: 84057-84-1
Molecular Formula: C9H7Cl2N5
3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine - Names and Identifiers
| Name | Lamotrigine |
| Synonyms | BW-430C LAMICTAL GI 267119X LAMOTRIGIN Lemotrigine LAMOTRIGINE Lamotrigine LAMOTRIGINE-13C1 4-triazine-3,5-diamine,6-(2,3-dichlorophenyl)-2 3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine |
| CAS | 84057-84-1 |
| EINECS | 281-901-8 |
| InChI | InChI=1/C9H7Cl2N5/c10-5-3-1-2-4(6(5)11)7-8(12)14-9(13)16-15-7/h1-3H,(H4,12,13,14,16) |
| InChIKey | PYZRQGJRPPTADH-UHFFFAOYSA-N |
3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine - Physico-chemical Properties
| Molecular Formula | C9H7Cl2N5 |
| Molar Mass | 256.09 |
| Density | 1.572±0.06 g/cm3(Predicted) |
| Melting Point | 177-181°C |
| Boling Point | 503.1±60.0 °C(Predicted) |
| Flash Point | 9℃ |
| Solubility | Slightly soluble in water, easily soluble in benzene, toluene, hot ethanol and other organic solvents. |
| Appearance | White crystal |
| Color | white |
| Merck | 14,5353 |
| pKa | 5.7(at 25℃) |
| Storage Condition | 2-8°C |
| Sensitive | Sensitive to heat and air |
| MDL | MFCD00865333 |
| Physical and Chemical Properties | Melting point 177-181°C |
| Use | For the treatment of intractable epilepsy |
3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine - Risk and Safety
| Risk Codes | R25 - Toxic if swallowed R36/37/38 - Irritating to eyes, respiratory system and skin. R39/23/24/25 - R23/24/25 - Toxic by inhalation, in contact with skin and if swallowed. R11 - Highly Flammable |
| Safety Description | S45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) S36 - Wear suitable protective clothing. S26 - In case of contact with eyes, rinse immediately with plenty of water and seek medical advice. S36/37 - Wear suitable protective clothing and gloves. S16 - Keep away from sources of ignition. |
| UN IDs | UN 2811 6.1/PG 3 |
| WGK Germany | 3 |
| RTECS | XY5850700 |
| HS Code | 29336990 |
| Hazard Class | 6.1(b) |
| Packing Group | III |
| Toxicity | LD50 in mice, rats (mg/kg): 250, >640 orally (Sawyer) |
3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine - Reference
| Reference Show more | 1. Wu Yan, Li Huiting, Wang Liwen, etc. Internal quality control evaluation of lamotrigine therapeutic drug monitoring based on Westgard multi-rule theory [J]. China Modern Applied Pharmacy, 2019, v.36(19):53-57. 2. Lu Haimei, Xie Meijuan, Li Shan, et al. Improvement of 6Hz corneal kindling drug-resistant epilepsy mouse model and effects of three traditional Chinese medicines [J]. Chinese Journal of Pharmacy, 2018, 053(007):1048-1053. 3. Wang, Fangyuan, et al. "Facile nose-to-brain delivery of rotigotine-loaded polymer micells thermo sensitive hydrogels: In vitro characterization and in vivo behavior study." International journal of pharmaceutics 577 (2020): 119046.https://doi.org/10.1016/ 4. [IF = 5.875] Fangyuan Wang et al."Facile nose-to-brain delivery of rotigotine-loaded polymer micelles thermosensitive hydrogels: In vitro characterization and in vivo behavior study."Int J Pharmaceut. 2020 Mar;577:119046 |
3,5-Diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine - Reference Information
| Introduction | lamotrigine is a new type of benzotriazine antiepileptic drug, which was marketed in China in 2005. Its mechanism of action is to block the presynaptic membrane voltage-gated sodium pathway and inhibit the release of pathological glutamate, thereby inhibiting the burst of glutamate-induced action potential, thereby stabilizing the neuronal cell membrane. As a broad-spectrum antiepileptic drug, lamotrigine is mainly used in clinical partial and systemic seizures monotherapy or adjuvant therapy, and can also be used as an emotional stabilizer in the treatment of type I bipolar disorder. |
| mechanism of action | lamotrigine is a voltage-dependent sodium channel blocker: ① inhibit voltage-dependent ⅱa Na channel, stabilize cell membrane and inhibit abnormal discharge of neuronal cells; ② stabilize presynaptic membrane, inhibits the release of excitatory neurotransmitters, especially glutamate; ③inhibits voltage-gated calcium channels. |
| pharmacokinetics | lamotrigine is well absorbed after oral administration and is not affected by food intake, high bioavailability, long half-life, and no obvious first-pass metabolism, pharmacokinetics is linear, the induction of liver drug enzyme and its induction effect is small, it has no adverse effect on the cognitive function of patients, and has the effect of improving cognitive function. There are few interactions between LTG and other drugs, good pharmacokinetic characteristics and low protein binding rate, which rarely affect the metabolism and elimination of other drugs. |
| properties | lamotrigine is white or almost white and slightly yellow. Crystallization in isopropanol, slightly soluble in water, melting point, 216~218 ℃, soluble in benzene, toluene, hot ethanol and other organic solvents. |
| Use | lamotrigine is a phenyltriazine compound, which is a new type of antiepileptic drug. The new antiepileptic drug, which acts like phenytoin sodium and carbamazepine, has a significant inhibitory effect on hind limb rigidity in mice induced by strong electrical stimulation or pentylenetetrazol. For anti-epilepsy. lamotrigine is an anticonvulsant for the treatment of intractable epilepsy. Inhibition of glutamate release, possibly by inhibition of sodium, potassium and calcium currents. For the treatment of bipolar depression. |
| Application | is mainly used for partial epilepsy, especially for refractory partial epilepsy that cannot be controlled by other single or combined drugs, its role is safe and effective. For absence seizures, or atypical absence seizures, myoclonic seizures are controlled in about 50% of patients. It is also suitable as an adjunct to the treatment of Lennox-Gastant syndrome in intractable epilepsy, as well as secondary and idiopathic generalized tonic-clonic seizures. |
| production method | 2, 3-dichlorobenzoic acid is chlorinated to 2, 3-dichlorobenzoyl chloride and reacted with cuprous cyanide, and aminoguanidine condensation, and finally under the action of potassium hydroxide lamotrigine ring. |
| toxic substance data | information provided by: pubchem.ncbi.nlm.nih.gov (external link) |
Last Update：2024-04-09 15:16:53
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Mobile: 86+15671228036
QQ: 2853786052
Wechat: 15671228036
Multiple SpecificationsSpot supply
Product Name: Lamotrigine Visit Supplier Webpage Request for quotationCAS: 84057-84-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
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