CAS 32854-75-4|Lappaconitine

Introduction：Basic information about CAS 32854-75-4|Lappaconitine, including its chemical name, molecular formula, synonyms, physicochemical properties, and safety information, etc.

Table of Contents

1. Names
2. Lappaconitine BiologicalActivity
3. Chemical & Physical Properties
4. Toxicological Information
CHEMICAL IDENTIFICATION
HEALTH HAZARD DATA
ACUTE TOXICITY DATA
5. Synonyms

Common Name	Lappaconitine
CAS Number	32854-75-4	Molecular Weight	584.700
Density	1.4±0.1 g/cm3	Boiling Point	720.7±60.0 °C at 760 mmHg
Molecular Formula	C₃₂H₄₄N₂O₈	Melting Point	217-218ºC
MSDS	/	Flash Point	389.7±32.9 °C

Names

Name	Lannaconitine
Synonym	More Synonyms

Lappaconitine BiologicalActivity

Description	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].
Related Catalog	Signaling Pathways >>Membrane Transporter/Ion Channel >>P2X ReceptorNatural Products >>AlkaloidResearch Areas >>Others
References	[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.

Description

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].

Related Catalog

Signaling Pathways >>Membrane Transporter/Ion Channel >>P2X ReceptorNatural Products >>AlkaloidResearch Areas >>Others

References

[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.

Chemical & Physical Properties

Density	1.4±0.1 g/cm3
Boiling Point	720.7±60.0 °C at 760 mmHg
Melting Point	217-218ºC
Molecular Formula	C₃₂H₄₄N₂O₈
Molecular Weight	584.700
Flash Point	389.7±32.9 °C
Exact Mass	584.309753
PSA	126.79000
LogP	2.13
Vapour Pressure	0.0±2.4 mmHg at 25°C
Index of Refraction	1.624
InChIKey	NWBWCXBPKTTZNQ-QOQRDJBUSA-N
SMILES	CCN1CC2(OC(=O)c3ccccc3NC(C)=O)CCC(OC)C34C1C(CC23)C1(O)CC(OC)C2CC4C1(O)C2OC
Storage condition	2-8C

Toxicological Information

CHEMICAL IDENTIFICATION

RTECS NUMBER :: AR5569552

CHEMICAL NAME :: Aconitane-4,8,9-triol, 20-ethyl-1,14,16-trimethoxy-, 4-(2-acetylamino)benzoate), (1-alpha,14-alpha,16-beta)-

CAS REGISTRY NUMBER :: 32854-75-4

BEILSTEIN REFERENCE NO. :: 0072755

LAST UPDATED :: 199612

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

Synonyms

LAPPACONITINE

(1a,14a,16b)-20-Ethyl-1,14,16-trimethoxyaconitane-4,8,9-triol 4-[2-(Acetylamino)benzoate]

acetyl-10-deoxysepaconitine

(1α,14α,16β)-20-Ethyl-8,9-dihydroxy-1,14,16-trimethoxyaconitan-4-yl 2-acetamidobenzoate

Benzoic acid, 2-(acetylamino)-, (1α,14α,16β)-20-ethyl-8,9-dihydroxy-1,14,16-trimethoxyaconitan-4-yl ester

N-Acetylpuberanidine

lappaconintine

Aconitum kusnezoffii Reichb

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