Amezinium methylsulfate

Modify Date: 2025-08-25 13:12:03

Amezinium methylsulfate structure	Common Name	Amezinium methylsulfate
	CAS Number	30578-37-1	Molecular Weight	313.33000
	Density	N/A	Boiling Point	N/A
	Molecular Formula	C₁₂H₁₅N₃O₅S	Melting Point	N/A
	MSDS	N/A	Flash Point	N/A

Use of Amezinium methylsulfate

Amezinium metilsulfate has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition ofnoradrenaline and tyramine uptake. Target: alpha and beta-1 receptorsAmezinium metilsulfate is a sympathomimetic drug used for the treatment of low blood pressure. Cardiovascular effects of the new sympathomimetic Amezinium metilsulphate are investigated in 25 patients compared with a control group (n = 25). During spinal/epidural anaesthesia 5 mg amezinium is given i.v. if blood pressure dropped greater than 20 mmHg. from starting-point. A significant recovery of blood pressure (epidural anaesthesia: syst 21%, diast 9%; spinal anaesthesia: syst 13%, diast 6.6%) and a decrease in heart rate (6.8% resp. 4,5%) are thought due to peripheral vasoconstriction. Amezinium proves a stimulating drug for alpha- and beta 1-receptors by stabilising the systemic blood pressure in spinal/epidural anaesthesia.

Name	6-methoxy-1-phenylpyridazin-1-ium-4-amine,methyl sulfate
Synonym	More Synonyms

Description	Amezinium metilsulfate has multiple mechanisms, including stimulation of alpha and beta-1 receptors and inhibition ofnoradrenaline and tyramine uptake. Target: alpha and beta-1 receptorsAmezinium metilsulfate is a sympathomimetic drug used for the treatment of low blood pressure. Cardiovascular effects of the new sympathomimetic Amezinium metilsulphate are investigated in 25 patients compared with a control group (n = 25). During spinal/epidural anaesthesia 5 mg amezinium is given i.v. if blood pressure dropped greater than 20 mmHg. from starting-point. A significant recovery of blood pressure (epidural anaesthesia: syst 21%, diast 9%; spinal anaesthesia: syst 13%, diast 6.6%) and a decrease in heart rate (6.8% resp. 4,5%) are thought due to peripheral vasoconstriction. Amezinium proves a stimulating drug for alpha- and beta 1-receptors by stabilising the systemic blood pressure in spinal/epidural anaesthesia.
Related Catalog	Signaling Pathways >> GPCR/G Protein >> Adrenergic Receptor Research Areas >> Cardiovascular Disease
References	[1]. Schaps D, et al. Therapeutic use of amezinium methylsulfate--a new, long acting, sympathomimetic--in paraspinal conduction anesthesia. Anasth Intensivther Notfallmed. 1984 Oct;19(5):235-9.

Molecular Formula	C₁₂H₁₅N₃O₅S
Molecular Weight	313.33000
Exact Mass	313.07300
PSA	126.83000
LogP	1.70410

Amezinium methylsulfate MSDS(Chinese)

CHEMICAL IDENTIFICATION

RTECS NUMBER :: UR6066500

CHEMICAL NAME :: Pyridazinium, 4-amino-6-methoxy-1-phenyl-, methyl sulfate

CAS REGISTRY NUMBER :: 30578-37-1

LAST UPDATED :: 199806

DATA ITEMS CITED :: 17

MOLECULAR FORMULA :: C11-H12-N3-O.C-H3-O4-S

MOLECULAR WEIGHT :: 313.36

HEALTH HAZARD DATA

ACUTE TOXICITY DATA

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 1330 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,72,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 282 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1471,1988

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 24 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1471,1988

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 1330 mg/kg

TOXIC EFFECTS :: Behavioral - altered sleep time (including change in righting reflex) Behavioral - convulsions or effect on seizure threshold Lungs, Thorax, or Respiration - dyspnea

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1471,1988

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Subcutaneous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 282 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,72,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - mouse

DOSE/DURATION :: 24100 ug/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: NIIRDN Drugs in Japan (Ethical Drugs). (Yakugyo Jiho Co., Ltd., Tokyo, Japan) Volume(issue)/page/year: -,72,1995

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 100 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 18,310,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Mammal - dog

DOSE/DURATION :: 60 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 18,310,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 800 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 18,310,1982

TYPE OF TEST :: LD50 - Lethal dose, 50 percent kill

ROUTE OF EXPOSURE :: Intravenous

SPECIES OBSERVED :: Rodent - rabbit

DOSE/DURATION :: 25 mg/kg

TOXIC EFFECTS :: Details of toxic effects not reported other than lethal dose value

REFERENCE :: MDACAP Medicamentos de Actualidad. (J.R. Prous, S.A., Apartado de Correos 540, 08080 Barcelona, Spain) V.1- 1965- Volume(issue)/page/year: 18,310,1982 ** OTHER MULTIPLE DOSE TOXICITY DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 10920 mg/kg/52W-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Endocrine - changes in thyroid weight Related to Chronic Data - changes in prostate weight

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1507,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

SPECIES OBSERVED :: Rodent - rat

DOSE/DURATION :: 21 gm/kg/30D-C

TOXIC EFFECTS :: Kidney, Ureter, Bladder - other changes in urine composition Endocrine - other changes Related to Chronic Data - death

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1481,1988 ** REPRODUCTIVE DATA **

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 16380 mg/kg

SEX/DURATION :: male 13 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Paternal Effects - testes, epididymis, sperm duct Reproductive - Paternal Effects - prostate, seminal vesicle, Cowper's gland, accessory glands

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1529,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 3375 mg/kg

SEX/DURATION :: female 17-22 day(s) after conception lactating female 21 day(s) post-birth

TOXIC EFFECTS :: Reproductive - Effects on Newborn - other neonatal measures or effects Reproductive - Effects on Newborn - growth statistics (e.g.%, reduced weight gain) Reproductive - Effects on Newborn - behavioral

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1581,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 11340 mg/kg

SEX/DURATION :: male 9 week(s) pre-mating

TOXIC EFFECTS :: Reproductive - Fertility - pre-implantation mortality (e.g. reduction in number of implants per female; total number of implants per corpora lutea) Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1543,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1980 mg/kg

SEX/DURATION :: female 7-17 day(s) after conception

TOXIC EFFECTS :: Reproductive - Maternal Effects - other effects Reproductive - Effects on Embryo or Fetus - fetotoxicity (except death, e.g., stunted fetus) Reproductive - Specific Developmental Abnormalities - musculoskeletal system

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1557,1988

TYPE OF TEST :: TDLo - Lowest published toxic dose

ROUTE OF EXPOSURE :: Oral

DOSE :: 1625 mg/kg

SEX/DURATION :: female 6-18 day(s) after conception

TOXIC EFFECTS :: Reproductive - Effects on Embryo or Fetus - fetal death

REFERENCE :: YACHDS Yakuri to Chiryo. Pharmacology and Therapeutics. (Raifu Saiensu Shuppan K.K., 2-5-13, Yaesu, Chuo-ku, Tokyo 104, Japan) V.1- 1972- Volume(issue)/page/year: 16,1573,1988

HS Code	2933990090

Chloridazon

CAS#:1698-60-8

Amezinium methy...

CAS#:30578-37-1

Literature: Arzneimittel-Forschung/Drug Research, , vol. 31, # 9 A p. 1529 - 1533

5-Amino-2-pheny...

CAS#:13589-77-0

Dimethyl sulfate

CAS#:77-78-1

~62%

Amezinium methy...

CAS#:30578-37-1

Literature: Reicheneder; Burger; Koenig; Kropp; Lietz; Thyes; Wiersdorff Arzneimittel-Forschung/Drug Research, 1981 , vol. 31, # 9 A p. 1529 - 1533

1-Phenyl-4,5-di...

CAS#:1698-53-9

Dimethyl sulfate

CAS#:77-78-1

Amezinium methy...

CAS#:30578-37-1

Literature: Angewandte Chemie, , vol. 92, # 10 p. 802 - 815

Precursor 4
CAS#:1698-60-8 Chloridazon CAS#:13589-77-0 5-Amino-2-pheny... CAS#:77-78-1 Dimethyl sulfate CAS#:1698-53-9 1-Phenyl-4,5-di...
DownStream 0

HS Code	2933990090
Summary	2933990090. heterocyclic compounds with nitrogen hetero-atom(s) only. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0%

Supratonin

Amezinio metilsulfato [Spanish]

Amezinii metilsulfas [INN-Latin]

Regulton

Ameziniummetilsulfat [German]

amexinium methyl sulfate

Metilsulfate d'amezinium [INN-French]

4-amino-6-methoxy-1-phenyl-pyridazinium methyl sulfate

Amezinium Methyl Sulfate

EINECS 250-248-0

Amezinium methylsulfate

amezinium metilsulfate

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