Marsanidine and 7-Me-marsanidine, the new hypotensive imidazolines augment sodium and urine excretion in rats

Wróblewska, Magdalena; Kasprzyk, Joanna; Sączewski, Franciszek; Kornicka, Anita; Boblewski, Konrad; Lehmann, Artur; Rybczyńska, Apolonia

doi:10.1016/s1734-1140(13)71085-5

Cited by 14 publications

(10 citation statements)

References 17 publications

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“…This further suggests marsanidine and 7-fluoro-marsanidine were able to exert their sedative effects probably at the level of LC. Future studies will investigate the nature and duration of sedation exerted by these new drugs; however, this observation supports ours and others' previous findings that these ligands are potent ␣ 2 -AR agonists [35,43]. Given that the drugs were administered in the rats peripherally via i.p.…”

Section: Discussionsupporting

confidence: 86%

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The effect of 7-fluoro-marsanidine, a novel α2-adrenoceptor agonist, on extracellular noradrenaline in rat frontal cortex: A microdialysis study

Ferdousi

Lalies

Wasilewska

et al. 2015

Neuroscience Letters

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Section: Discussionsupporting

confidence: 86%

“…Our group previously reported about marsanidine, an imidazoline based ␣ 2 -AR agonist, that was antihypertensive and diuretic in rats [3,43]. It was also shown that the hypotensive effects of marsanidine were blocked by the ␣ 2 -AR antagonist RX821002 [3].…”

Section: Introductionmentioning

confidence: 99%

The effect of 7-fluoro-marsanidine, a novel α2-adrenoceptor agonist, on extracellular noradrenaline in rat frontal cortex: A microdialysis study

Ferdousi

Lalies

Wasilewska

et al. 2015

Neuroscience Letters

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“…In our previous SAR analysis on marsanidine‐like ligands D , it has been revealed that substitution at the C‐7 atom of the indazole ring with chlorine, fluorine, or methyl group led to compounds with high cardiovascular properties, wherein the greatest hypotensive activity was noted for the congener bearing a fluorine that is 7‐F‐marsanidine of type D . A similar trend was found for indoles 3 as 7‐F‐substituted derivative 3g displayed the largest hemodynamic effects in the respective 3a–j series (Table ).…”

Section: Resultsmentioning

confidence: 63%

1‐[(Imidazolidin‐2‐yl)imino]‐1H‐indoles as new hypotensive agents: synthesis and in vitro and in vivo biological studies

Kornicka

Wasilewska

Sączewski³

et al. 2016

Chem Biol Drug Des

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A series of 1-[(imidazolidin-2-yl)imino]-1H-indole analogues of hypotensive α -AR agonists, 1-[(imidazolidin-2-yl)imino]-1H-indazoles, was synthesized and tested in vitro for their activities at α - and α -adrenoceptors as well as imidazoline I and I receptors. The most active 1-[(imidazolidin-2-yl)imino]-1H-indoles displayed high or moderate affinities for α - and α -adrenoceptors and substantial selectivity for α -adrenoceptors over imidazoline-I binding sites. The in vivo cardiovascular properties of indole derivatives 3 revealed that substitution at C-7 position of the indole ring may result in compounds with high cardiovascular activity. Among them, 7-fluoro congener 3g showed the most pronounced hypotensive and bradycardic activities in this experiment at a dose as low as 10 μg/kg i.v. Metabolic stability of the selected compounds of type 3 was determined using both in vitro and in silico approaches. The results indicated that these compounds are not vulnerable to rapid first-phase oxidative metabolism.

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“…18 The well-established mydriasis model according to Koss 3 was applied. The activity of marsanidine and 7-methylmarsanidine was compared to clonidine, a reference imidazoline drug stimulating brain α 2 -adrenoceptors.…”

Section: Introductionmentioning

confidence: 99%

Are Alpha-2D Adrenoceptor Subtypes Involved in Rat Mydriasis Evoked by New Imidazoline Derivatives: Marsanidine and 7-Methylmarsanidine?

et al. 2017

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The imidazoline compounds may produce mydriasis after systemic administration to some species (rats, cats, and mice). In mydriatic activity of imidazolines, α2D-adrenoceptors subtype(s) seems to be involved. In this study, the pupil dilatory effect evoked by 2 newly synthesized imidazoline derivatives—α2-adrenoceptor agonists: marsanidine and 7-methylmarsanidine—was compared. The compounds were tested alone as well as in the presence of α2-adrenoceptor antagonists (nonselective, yohimbine, and selective toward the following α2-adrenoceptor subtypes—α2A-2-[(4,5-dihydro-1H-imidazol-2-yl)methyl]-2,3-dihydro-1-methyl-1H-isoindole maleate (BRL44408), α2B-2-[2-(4-(2-methoxyphenyl)piperazin-1-yl)ethyl]-4,4-dimethyl-1,3-(2H,4H)-isoquinolindione dihydrochloride (ARC239), α2C-JP1302, α2D-2-(2,3-dihydro-2-methoxy-1,4-benzodioxin-2-yl)-4,5-dihydro-1H-imidazole hydrochloride [RX821002]). The agonists were studied in male Wistar rats and were administered intravenously in cumulative doses. The antagonistic compounds were given in a single dose before the experiment with marsanidine or 7-methylmarsanidine. Pupil diameter was measured with stereoscopic microscope equipped in green light filter. Marsanidine and 7-methylmarsanidine exerted marked mydriatic effects. BRL44408, JP1302, and ARC239 did not cause significant parallel shift to the right of the dose–effect curves obtained for both imidazolines. In case of yohimbine and RX821002, the marked parallel shifts of dose–response curves were observed, with the antagonistic effects of RX821002 more pronounced. In vivo pharmacodynamics experiment suggests that α2D-adrenoceptor subtype is mainly engaged in mydriatic effects evoked in rats by imidazoline derivatives, in particular by clonidine.

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Marsanidine and 7-Me-marsanidine, the new hypotensive imidazolines augment sodium and urine excretion in rats

Abstract: Our study indicates that the new hypotensive imidazoline compounds of marsanidine and 7-Me-marsanidine increase diuresis and natriuresis in rats. However, the effect of 7-Me-marsanidine is markedly more potent, probably due to its moderate affinity to the I1-imidazoline receptor.

Cited by 14 publications

References 17 publications

The effect of 7-fluoro-marsanidine, a novel α2-adrenoceptor agonist, on extracellular noradrenaline in rat frontal cortex: A microdialysis study

The effect of 7-fluoro-marsanidine, a novel α2-adrenoceptor agonist, on extracellular noradrenaline in rat frontal cortex: A microdialysis study

1‐[(Imidazolidin‐2‐yl)imino]‐1H‐indoles as new hypotensive agents: synthesis and in vitro and in vivo biological studies

Are Alpha-2D Adrenoceptor Subtypes Involved in Rat Mydriasis Evoked by New Imidazoline Derivatives: Marsanidine and 7-Methylmarsanidine?

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