LAPPACONITINE HBR
Lappaconitine hydrobromide
CAS: 97792-45-5
Molecular Formula: C32H45BrN2O8
LAPPACONITINE HBR - Names and Identifiers
| Name | Lappaconitine hydrobromide |
| Synonyms | Allapinine ALLAPININE LAPPACONITINE HBR ALLAPININE HYDROBROMIDE Lappaconite Hydrobromide Lappaconitin hydrobromide LAPPACONITINE HYDROBROMIDE Lappaconitine hydrobromide Lappaconitine Hydrobromide, CP Lappaconitine Hydrobromide 97792-45-5 (1-alpha,14-alpha,16-beta)-monohydrobromide Lappaconitine Hydrobromide And Glucose Injection (1a,14a,16b)-20-Ethyl-1,14,16-trimethoxyaconitane-4,8,9-triol 4-(2-(acetylamino)benzoate) hydrobromide |
| CAS | 97792-45-5 |
| InChI | InChI=1/C32H44N2O8.BrH/c1-6-34-16-29(42-28(36)18-9-7-8-10-21(18)33-17(2)35)12-11-25(40-4)31-23(29)14-20(26(31)34)30(37)15-22(39-3)19-13-24(31)32(30,38)27(19)41-5;/h7-10,19-20,22-27,37-38H,6,11-16H2,1-5H3,(H,33,35);1H/t19-,20?,22+,23-,24+,25+,26-,27+,29-,30+,31?,32+;/m1./s1 |
LAPPACONITINE HBR - Physico-chemical Properties
| Molecular Formula | C32H45BrN2O8 |
| Molar Mass | 665.61 |
| Melting Point | 223-226 ºC |
| Boling Point | 740.8 °C at 760 mmHg |
| Solubility | DMSO : 50 mg/mL (75.12 mM; Need ultrasonic) |
| Appearance | White powder |
| Color | White to Light yellow |
| Storage Condition | 2-8°C |
| MDL | MFCD00171334 |
LAPPACONITINE HBR - Risk and Safety
| Hazard Symbols | T+ - Very toxic |
| Risk Codes | 28 - Very Toxic if swallowed |
| Safety Description | 45 - In case of accident or if you feel unwell, seek medical advice immediately (show the label whenever possible.) |
| UN IDs | UN 1544 6.1/PG 2 |
| RTECS | AR5569600 |
| HS Code | 29399990 |
| Hazard Class | 6.1 |
| Packing Group | II |
LAPPACONITINE HBR - Reference
| Reference Show more | 1. Liu Yanhao, Liang Dahu, Sun Hua, Wu Zijing, Zhang Yuanxiang, Li Chao, Dong Jian, Li Hongjin, Han chengzheng, Xie Haitang. Simultaneous determination of six alkaloids in radix aconiti lateralis Preparata from Shenfu qiangxin pills by HPLC-MS/MS [J]. Journal of Wannan Medical College, 2021,40(01):18-21. 2. [IF = 2.629] Li Chao et al."Evaluation of the Influence of henwu Tang on the pharmacochemicals of Digoxin in Rats Using HPLC-MS/MS. Evid-Based Compl Alt. 2021;2021:2673183 3. [IF = 1.908] Yanhao Liu et al." Comparative HPLC-MS/MS-based pharmacokinetic studies of multiple diterpenoid alkaloids following the administration of Zhenwu Tang and Radix Aconiti. "Xenobiotica. 2021;51(3):345-354 |
LAPPACONITINE HBR - Reference Information
| alkaloid | Lappaconitine hydrobromide it is a kind of diterpenoid alkaloid-Laba aconitine, which is isolated from the plant aconite of Ranunculaceae, and its chemical name is (1 α,14 α,16 β)-20-ethyl -1,14,16-trimethoxyaconitine -4,8, 9-triol 4-[2-(acetylamino) benzoate hydrobromide monohydrate. It is the first non-addictive analgesic drug in China. With analgesic, antipyretic, swelling and local anesthesia, and no addiction and accumulation effect, its analgesic effect is stronger than indomethacin, weaker than morphine. |
| source plant | an alkaloid (rabazaconitine) extracted from the root of a plant of the family Ranunculaceae. Figure 1: Aconitum palmatum |
| extraction method | crush the root of Aconitum hominis-added into the extraction tank and soaked in ethanol for 1H, heated and refluxed for 3H for 3 times → concentrate, acidify with 2% hydrochloric acid, suction filter → add ammonia to make alkaline solution to PH 9-10, stir and precipitate, filter → dissolve the precipitate with chloroform → Add process water, let stand and separate into layers → add anhydrous potassium carbonate, stir and dehydrate, suction under reduced pressure to paste-dissolve with ethanol and recover ethanol until crystallization-lappaconitine was obtained. |
| pharmacological action | 1. Analgesic effect lappaconitine hydrobromide intraperitoneal injection can obviously relieve chronic constriction injury (CCL) thermal pain in rats, to achieve analgesic therapeutic effect, and no obvious toxic reaction. 2. Anti-inflammatory effect lappaconitine has obvious inhibitory effect on xylene-induced ear swelling in mice, arthritic foot swelling in rats and Agar granuloma hyperplasia in rats. The results showed that lappaconitine had anti-acute and chronic inflammatory effects, which provided a theoretical basis for the clinical treatment of pain and swelling caused by rheumatic and rheumatoid arthritis. 3. Anti-tumor effect the tumor inhibition rate of lappaconitine on liver cancer in mice was 11.20%-53.08%, and the tumor inhibition rate of S180 in mice was 29.81%-53.%. The results indicate that lappaconitine has a certain anti-liver cancer S180 effect in mice, and has no obvious effect on the body weight of mice. 4. Antiarrhythmic effect lappaconitine can increase the normal threshold of arrhythmia induced by aconitine in rats, and can significantly improve the myocardial ischemic arrhythmia in dogs, thereby reducing the incidence of arrhythmia, the mechanism may be to block the sodium channel. |
| pharmacokinetics | [pharmacokinetics] plasma elimination half-life (tl/2) of lappaconitine hydrobromide, the clearance rate of CL and apparent volume of distribution V in high, medium and low three doses had no significant difference, that is, the pharmacokinetic parameters of the drug basically does not change with the change of dose, the performance is linear dynamic behavior. The drug-time process in vivo conforms to a two-compartment open model, with faster absorption and moderate elimination. [Distribution] it is widely distributed in mouse tissues and binds to tissue proteins, resulting in lower drug concentrations in plasma. Metabolism: there are 10 metabolites of lappaconitine in rats. Metabolites include hydroxylated metabolites, O-demethylated metabolites, N-deacetylated metabolites, O-demethylated N-deacetylated metabolites, BIS O-demethyl N-deacetylated metabolite, ester hydrolysis metabolite. The main metabolic pathways of lappaconitine in rats are hydroxylation, O-demethylation, N-deacetylation and ester hydrolysis. These metabolic pathways may also cross over to produce secondary metabolites.|
| indications | for cancer pain, surgical pain, toothache, dysmenorrhea and other moderate or above pain. |
| Toxicology | This product has no teratogenic effect in animal test. Results of acute toxicity test: the oral LD50 of rats was 20mg/Kg; The intraperitoneal injection of LD50 was 9.1mg/Kg, and the intravenous injection of LD50 was 6.9mg/Kg. |
| adverse reactions | individual patients had urticaria, Palpitations, chest tightness, dizziness, etc., which disappeared soon after drug withdrawal. |
| storage | protected from light and sealed. |
| uses | for gastrointestinal ulcers, gastritis, hepatitis, cholecystitis, rheumatism, sciatica, toothache, postoperative pain, cancer pain and other symptoms. A selective blocker of TTX-sensitive sodium channels that does not affect the activation threshold of sodium channels. |
Last Update：2024-04-09 15:16:53
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Mobile: 18021002903
QQ: 3008007409
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