| Identification | Back Directory | [Name]
Amezinium methylsulfate | [CAS]
30578-37-1 | [Synonyms]
lu1631
Risumic
regulton
Amezinium
Tenfortan
Supratonin
REGULTON (KNOLL)
Amezinium mesylate
RISUMIC (DAINIPPON)
ameziniometilsulfato
ameziniummetilsulfat
ameziniummetilsulfate
SUPRATONIN (GRUNENTHAL)
AMEZINIUM METHYL SULFATE
Amezinium Methyl Sulfate >
4-Amino-6-methoxy-1-phenylpyridazin-1-ium
4-amino-6-methoxy-1-phenylpyridazinium-methylsulfat
4-amino-6-methoxy-1-phenylpyridaziniummethylsulfate
4-amino-6-methoxy-1-phenyl-pyridaziniumethylsulfate
1-Phenyl-4-amino-6-methoxypyridazinium methyl sulfate
6-methoxy-1-phenylpyridazin-1-ium-4-amine methylsulfate
4-Amino-6-methoxy-1-phenylpyridazin-1-ium methyl sulfate
Pyridazinium, 4-amino-6-methoxy-1-phenyl-, methyl sulfate
Pyridazinium, 4-amino-6-methoxy-1-phenyl-, methyl sulfate (1:1) | [EINECS(EC#)]
250-248-0 | [Molecular Formula]
C12H15N3O5S | [MDL Number]
MFCD00865972 | [MOL File]
30578-37-1.mol | [Molecular Weight]
313.33 |
| Chemical Properties | Back Directory | [Melting point ]
176° (dec) | [storage temp. ]
Inert atmosphere,Room Temperature | [solubility ]
DMSO : ≥ 34 mg/mL (108.51 mM) | [form ]
powder to crystal | [color ]
White to Light yellow | [Merck ]
14,394 | [CAS DataBase Reference]
30578-37-1 |
| Safety Data | Back Directory | [RTECS ]
UR6066500 | [HS Code ]
2933.59.8000 | [Toxicity]
LD50 in mice, rats (mg/kg): 1630, 1410 orally; 40.4, 45.5 i.v. (Teschendorf) |
| Hazard Information | Back Directory | [Originator]
Regulton,Nordmark,W. Germany,1981 | [Definition]
ChEBI:Amezinium metilsulfate is an azaheterocycle sulfate salt of amezinium. It is a sympathomimetic drug which suppresses noradrenaline reuptake and thereby elevating blood pressure. It is used for the treatment of low blood pressure in patients undergoing dialysis. It has a role as an EC 1.4.3.4 (monoamine oxidase) inhibitor, an antihypotensive agent, a sympathomimetic agent and an adrenergic uptake inhibitor. It contains an amezinium. | [Manufacturing Process]
18.7 parts of 1-phenyl-4-aminopyridazone-(6) and 19 parts of dimethyl
sulfate in 400 parts of xylene are kept at 120°C for one hour while mixing
well. The reaction mixture is suction filtered, 28 parts (89.5% of the theory)
of 1-phenyl-4-amino-6-methoxypyridazinium methosulfate is obtained having
a melting point of 173°C to 174°C after recrystallization from acetonitrile. The
perchlorate has a melting point of 179°C to 182°C. | [Therapeutic Function]
Antihypotensive | [Enzyme inhibitor]
This sympathomimetic and antihypotensive drug (FW = 313.32 g/mol;
CAS 30578-37-1), also named 4-amino-6-methoxy-1-phenyl-py?ridazinium
methyl sulfate, amezinium-metilsulfate, LU 1631, and Regulton, increases
the arterial blood pressure and heart rate of anaesthetized animals and of
pithed rats by stimulating vascular a-adrenoceptors and cardiac b1-
adrenoceptors. This action is unaffected by ganglionic blockade with
hexamethonium. The a-adrenergic blocking drug phentolamine
antagonizes the blood pressure increasing effect of amezinium, and the b-
adrenergic blocking drug propranolol antagonizes the heart rate increasing
effect. Noradrenaline depletion by pretreatment with reserpine reduces the
pressor effect of amezinium to approximately the same extent as it reduces
the effect of tyramine. It completely abolished the heart rate increasing
effect. Under such conditions, high doses of amezinium reduced the heart
rate. Amezinium is taken up by adrenergic neurons. Amezinium also
inhibits intraneuronal monoamine oxidase, with IC50 values of 5 μM and
>1mM for MAO-A and MAO-B, respectively. | [storage]
Store at -20°C |
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