Lappaconitine

Lappaconitine, isolated from Aconitum sinomontanum Nakai, was characterized as analgesic principle.IC50 value:Target:In vitro: In vivo: Lappaconitine was characterized as analgesic principle by our laboratory. The results suggest that lappaconitine can produce analgesia, possibly through a decrease in cellular calcium availability and PAG may be involved in the Ca2+ antagonistic effect on lappaconitine analgesia [1]. Changes in lappaconitine levels in blood, brain and spinal cord following subcutaneous (s.c.) injection were correlated with the analgesic activity at intervals up to 90 minutes after injection. The equianalgesic doses of lappaconitine (ED50 by the s.c. route and additive ED50 by the i.c.v. plus i.t. route) gave closely similar concentrations of the drug in brain and spinal cord. These results indicate that a simultaneous action of lappaconitine on supraspinal and spinal sites is likely to be important for the analgesia produced by systemically administered lappaconitine [2].

Signaling Pathways >> Membrane Transporter/Ion Channel >> P2X Receptor

Natural Products >> Alkaloid

Research Areas >> Others

[1]. Guo X, et al.Effects of central Ca2+ on analgesic action of lappaconitine. Zhongguo Yao Li Xue Bao. 1989 Nov;10(6):504-7.

[2]. Ono M, et al. Pharmacological studies of lappaconitine: supraspinal-spinal interaction in antinociception. Archives Internationales de Pharmacodynamie et de Therapie [1991, 309:32-41]

[3]. Heubach JF, et al. Cardiac effects of lappaconitine and N-deacetyllappaconitine, two diterpenoid alkaloids from plants of the Aconitum and Delphinium species. Planta Med. 1998 Feb;64(1):22-6.

Adenosine 5'-triphosphate disodium salt | KN-62 | A-740003 | A 438079 | af-353 | AZD9056 hydrochloride | PSB-12062 | A-317491 | A 804598 | A 839977 | Gefapixant | GW791343 | CE-224535 | JNJ-54175446

DATA ITEMS CITED :

4

MOLECULAR FORMULA :

C32-H44-N2-O8

MOLECULAR WEIGHT :

584.78

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - rat

DOSE/DURATION :

9900 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 8,301,1987

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Oral

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

20 mg/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 7,337,1951

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intraperitoneal

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

10500 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

CYLPDN Zhongguo Yaoli Xuebao. Acta Pharmacologica Sinica. Chinese Journal of Pharmacology. (China International Book Trading Corp., POB 2820, Beijing, Peop. Rep. China) V.1- 1980- Volume(issue)/page/year: 8,301,1987

TYPE OF TEST :

LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :

Intravenous

SPECIES OBSERVED :

Rodent - mouse

DOSE/DURATION :

6900 ug/kg

TOXIC EFFECTS :

Details of toxic effects not reported other than lethal dose value

REFERENCE :

APTOA6 Acta Pharmacologica et Toxicologica. (Copenhagen, Denmark) V.1-59, 1945-86. For publisher information, see PHTOEH Volume(issue)/page/year: 7,337,1951