Metabolites of 3-hydrazino-6-[bis-(2-hydroxyethyl) amino]pyridazine dihydrochloride in rat urine

Beretta, Elena; Cristina, Tito; Ferrari, Pietro; Tuan, G.; Zerilli, L. F.; Martinelli, E.

doi:10.1007/bf03189396

Cited by 4 publications

(1 citation statement)

References 3 publications

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“…In a previous study (10) in rats given unlabelled DL ISO-IT, in addition metabolites I and II there was found another product less polar than I, identified as 3-[bis-(2-hydroxyethyl)amino] -6-isopropoxypyridazine which is absent from human urine.…”

Section: Discussionmentioning

confidence: 99%

Disposition and metabolism of 3-hydrazino-6-[N,N-bis(2-hydroxyethyl)amino] pyridazine dihydrochloride in man

Assandri

Perazzi

Buniva

et al. 1979

European Journal of Drug Metabolism and Pharmacokinetics

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Three healthy volunteers (two men and one woman) were given single oral doses of 14 mg of 14C-labelled 3-hydrazino-6-[N N-bis(2-hydroxyethyl)amino] pyridazine dihydrochloride, a new anti-hypertensive agent. The drug was absorbed well, and peak levels of i4C-activity in the plasma, reached after 1.5-2.0 hrs, ranged between 98 and 161 ng eq/ml. The plasma half-lives of total radiocarbon calculated from the decline in the concen tration curves between 2 and 8 hrs varied between 1.4 and 2.1 hr. This phase of rapid decline was followed by a second one with a slower rate of disappearance of 14C. Approximately 40% of the radioactivity in the whole blood was confined to the plasma. Within 6 days an average of 102% of the administered dose was recovered, 57% being excreted in the urine and 45% in the faeces. Of the total radioactivity excreted in the urine, more than 70% was eliminated within the first 8 hrs. In the 24-hr urine, the radioactivity due to the two identified metabolites, 3-rbis (2 hydroxyethyljamino1pyridazine and 3-methyl-6-rbis (2-hydroxyethyl)amino] -s-triazole [4,3-b] pyridazine, did not account for more than 28% of the total radioactivity. Moreover, the second metabolite was shown to derive from another one present in the urine in substantial quantity (38%). It cannot be stated with certainty whether or not any unchanged drug was excreted in the urine.

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Section: Discussionmentioning

confidence: 99%

Disposition and metabolism of 3-hydrazino-6-[N,N-bis(2-hydroxyethyl)amino] pyridazine dihydrochloride in man

Assandri

Perazzi

Buniva

et al. 1979

European Journal of Drug Metabolism and Pharmacokinetics

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Studies on the metabolism of cadralazine in rat

Simonotti¹,

Zanol²,

Parravicini³

et al. 1982

European Journal of Drug Metabolism and Pharmacokinetics

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metabolism in rat; TLC-MS analysis; GC-MS quantitation; synthesis of 3-pyrazolylpyridazine derivatives as standards. SUMMARYThe metabolism of cadralazine I was studied after oral administration to rat. Besides consistent amount of unchanged drug, three metabolites were separated in urine by TLC and GC and their structures elucidated by mass spectrometry in comparison with synthetie samples. A specific and sensitive method was developed to detect the decarbethoxylated metabolite III at nanogram levels.

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Advances in Pyridazine Chemistry

Tišler

Stanovnik

1990

Advances in Heterocyclic Chemistry Volume 49

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Metabolites of 3-hydrazino-6-[bis-(2-hydroxyethyl) amino]pyridazine dihydrochloride in rat urine

Cited by 4 publications

References 3 publications

Disposition and metabolism of 3-hydrazino-6-[N,N-bis(2-hydroxyethyl)amino] pyridazine dihydrochloride in man

Disposition and metabolism of 3-hydrazino-6-[N,N-bis(2-hydroxyethyl)amino] pyridazine dihydrochloride in man

Studies on the metabolism of cadralazine in rat

Advances in Pyridazine Chemistry

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