Amezinium methylsulfate - CAS 30578-37-1
Catalog number: 30578-37-1
Category: Inhibitor
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Molecular Formula:
C11H12N3O.CH3O4S
Molecular Weight:
313.33
COA:
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Targets:
Adrenergic Receptor
Description:
Amezinium methylsulfate, a sympathomimetic drug used for the treatment of low blood pressure, increases the arterial blood pressure and heart rate of anaesthetized animals and of pithed rats by stimulating vascular alpha- and cardiac beta 1-adrenoceptors.
Appearance:
Solid powder
Synonyms:
6-methoxy-1-phenylpyridazin-1-ium-4-amine methylsulfate;AMEZINIUM METHYL SULFATE;SUPRATONIN (GRUNENTHAL);RISUMIC (DAINIPPON);REGULTON (KNOLL);4-amino-6-methoxy-1-phenyl-pyridaziniumethylsulfate;4-amino-6-methoxy-1-phenylpyridazinium-methylsulfat;4-amino-
Solubility:
Soluble to ≥ 34 mg/mL in DMSO
Storage:
Store in a cool and dry place and at 0 - 4℃ for short term (days to weeks) or -68℃ for long term (months to years).
MSDS:
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Shelf Life:
2 years
Melting Point:
1676 °C (decomp)
InChIKey:
ZEASXVYVFFXULL-UHFFFAOYSA-N
InChI:
1S/C11H11N3O.CH4O4S/c1-15-11-7-9(12)8-13-14(11)10-5-3-2-4-6-10;1-5-6(2,3)4/h2-8,12H,1H3;1H3,(H,2,3,4)
Canonical SMILES:
COC1=[N+](N=CC(=C1)N)C2=CC=CC=C2.COS(=O)(=O)[O-]
1.[The Shy-Drager syndrome].
Freistühler M1, Passenberg P, Bürger M. Dtsch Med Wochenschr. 1992 Jul 24;117(30):1146-8.
For 15 years a now 70-year-old woman had been having occasional episodes of circulatory collapse which 7 years ago were diagnosed as being caused by severe idiopathic orthostatic hypotension. These episodes had recently become much more frequent and she was hardly able to be upright for more than one minute. In the Schellong test the blood pressure fell from 80/50 mm Hg when lying to 70/30 mm Hg on standing, the pulse rate remaining unchanged at 60/min. The standing test had to be abandoned after 90 seconds. Serum catecholamine concentrations (epinephrine 65 ng/l, norepinephrine 100 ng/l) did not rise on standing (epinephrine 25 ng/l, norepinephrine 105 ng/l). 24-hour urinary excretion of vanillyl mandelic acid was at the lower limit of normal (2.2 mg). The autonomic dysfunction of circulatory control suggested a Shy-Drager syndrome. Other signs of autonomic failure included gastroparesis, decreased tear and sweat secretion and transitory urinary incontinence.
2.[Therapeutic use of amezinium methylsulfate--a new, long acting, sympathomimetic--in paraspinal conduction anesthesia].
Schaps D, Seitz W, Mehler D, Tholen A, Goroll D. Anasth Intensivther Notfallmed. 1984 Oct;19(5):235-9.
Cardiovascular effects of the new sympathomimetic ameziniummetilsulphate were investigated in 25 patients compared with a control group (n = 25). During spinal/epidural anaesthesia 5 mg amezinium was 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%) were thought due to peripheral vasoconstriction. Amezinium proved a stimulating drug for alpha- and beta 1-receptors by stabilising the systemic blood pressure in spinal/epidural anaesthesia.
3.Disposition and metabolism of [14C]-amezinium metilsulfate in rats.
Nambu K1, Yoshida K, Kagemoto A, Matsumoto K, Miyazaki H, Hashimoto M, Esumi Y, Jin Y, Gunji S, Iwabuchi M, et al. Arzneimittelforschung. 1988 Jul;38(7):909-18.
Disposition and metabolism of [14C]-amezinium metilsulfate (4-amino-6-methoxy-1-phenylpyridazinium methylsulfate, Risumic) were systematically studied in rats after intravenous (5 mg/kg) or oral (20, 100 mg/kg) administration. After oral administration at 20 mg/kg, blood level reached the maximum (Cmax) of 0.65 microgram eq/ml at 3 h (tmax) and decreased with t1/2 of 8.1 h. Levels in plasma and most tissues elevated to the Cmax at 3 h. The liver level was the highest (61 times as high as plasma level) of all examined tissues. Most tissue levels decreased thereafter essentially in parallel with plasma levels. The findings by whole-body autoradiography essentially agreed with those by radiometry. In lactating rats, milk levels were virtually similar to plasma levels. [14C]-Amezinium metilsulfate radioactivity in fetus and fetal blood was around 0.3 microgram eq/g, being about 1/10 level of maternal plasma level. About 24, 72 and 42% were excreted in urine, feces and bile, respectively.
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CAS 30578-37-1 Amezinium methylsulfate

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