KSK19 – Novel histamine H3 receptor ligand reduces body weight in diet induced obese mice

Kotańska, Magdalena; Mika, Kamil; Reguła, Karolina; Szczepańska, Katarzyna; Szafarz, Małgorzata; Bednarski, Marek; Olejarz-Maciej, Agnieszka; Nowak, Katarzyna; Latacz, Gniewomir; Mogilski, Szczepan; Kuder, Kamil; Kieć‐Kononowicz, Katarzyna; Sapa, Jacek

doi:10.1016/j.bcp.2019.07.006

Cited by 15 publications

(17 citation statements)

References 29 publications

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“…Mice were fed on high-fat diet consisting of 40% fat blend (Labofeed B with 40% lard, Morawski Feed Manufacturer, Poland) for 15 weeks, water and 30% sucrose solution were available ad libitum [49, 50]. Control mice were fed on a standard diet (Labofeed B, Morawski Feed Manufacturer, Poland) and drank water only.…”

Section: Methodsmentioning

confidence: 99%

“…Glucose (1g/kg b.w.) was administrated ip [49, 50] and blood samples were taken from the tail vein at the time points: 0 (before glucose administration), 30, 60 and 120 minutes after administration. Glucose levels were measured with glucometer (ContourTS, Bayer, Germany, test stripes: ContourTS, Ascensia Diabetes care Poland Sp.…”

Section: Methodsmentioning

confidence: 99%

“…was injected ip and blood samples were collected at the time points: 0, 15 and 30 minutes from the tail vein and glucose levels were measured with glucometer (ContourTS, Bayer, Germany, test stripes: ContourTS, Ascensia Diabetes care Poland Sp. z o.o., Poland, REF:84239666) [49, 50]. The AUC was calculated using the trapezoidal rule.…”

Section: Methodsmentioning

confidence: 99%

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KD-64 – a new selective A_2Aadenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice

Kotańska

Dziubina

Szafarz

et al. 2020

Preprint

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The A2 adenosine receptors play an important role, among others, in the regulation of inflammatory process and glucose homeostasis in diabetes and obesity. Thus, the presented project evaluated of influence of the selective antagonist of A2A adenosine receptor – KD-64 as compared to the known non-selective antagonist – caffeine on these two particular processes. Two different inflammation models were induced namely local and systemic inflammation. Obesity was induced in mice by high-fat diet and the tested compounds (KD-64 and caffeine) were administrated for 21 days. KD-64 showed anti-inflammatory effect in both tested inflammation models and administered at the same dose as ketoprofen exerted stronger effect than this reference compound. Elevated levels of IL-6 and TNF-α observed in obese control mice were significantly lowered by the administration of KD-64 and were similar to the values observed in control non-obese mice. Interestingly, caffeine increased the levels of these parameters. In contrast to caffeine which had no influence on AlaT activity, KD-64 administration significantly lowered AlaT activity in the obese mice. Although, contrary to caffeine, KD-64 did not reduce diet-induced obesity in mice, it improved glucose tolerance. Thus, the activity of the selective adenosine A2A receptor antagonist was quite different from that of the non-selective.

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Section: Methodsmentioning

confidence: 99%

Section: Methodsmentioning

confidence: 99%

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KD-64 – a new selective A_2Aadenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice

Kotańska

Dziubina

Szafarz

et al. 2020

Preprint

Self Cite

View full text Add to dashboard Cite

show abstract

“…Metabolic disturbance induced with a high-fat/sucrose diet and its influence on body weight and spontaneous activity. Mice were fed on high-fat diet consisting of 40% fat blend (Labofeed B with 40% lard, Morawski Feed Manufacturer, Poland) for 15 weeks, water and 30% sucrose solution were available ad libitum [50,51]. Control mice were fed on a standard diet (Labofeed B, Morawski Feed Manufacturer, Poland) and drank water only.…”

Section: Obesity Studymentioning

confidence: 99%

“…Glucose (1g/kg b.w.) was administrated ip [50,51] and blood samples were taken from the tail vein at the time points: 0 (before glucose administration), 30, 60 and 120 minutes after administration. Glucose levels were measured with glucometer (ContourTS, Bayer, Germany, test stripes: ContourTS, Ascensia Diabetes care Poland Sp.…”

Section: Biochemical Analysismentioning

confidence: 99%

KD-64—A new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist—Caffeine does not reduce diet-induced obesity in mice

et al. 2020

Self Cite

View full text Add to dashboard Cite

The A 2 adenosine receptors play an important role, among others, in the regulation of inflammatory process and glucose homeostasis in diabetes and obesity. Thus, the presented project evaluated of influence of the selective antagonist of A 2A adenosine receptor-KD-64 as compared to the known non-selective antagonist-caffeine on these two particular processes. Two different inflammation models were induced namely local and systemic inflammation. Obesity was induced in mice by high-fat diet and the tested compounds (KD-64 and caffeine) were administrated for 21 days. KD-64 showed anti-inflammatory effect in both tested inflammation models and administered at the same dose as ketoprofen exerted stronger effect than this reference compound. Elevated levels of IL-6 and TNF-α observed in obese control mice were significantly lowered by the administration of KD-64 and were similar to the values observed in control non-obese mice. Interestingly, caffeine increased the levels of these parameters. In contrast to caffeine which had no influence on AlaT activity, KD-64 administration significantly lowered AlaT activity in the obese mice. Although, contrary to caffeine, KD-64 did not reduce diet-induced obesity in mice, it improved glucose tolerance. Thus, the activity of the selective adenosine A 2A receptor antagonist was quite different from that of the non-selective.

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Targeting Histamine and Histamine Receptors for the Precise Regulation of Feeding

Zheng

Chen

2021

Current Topics in Behavioral Neurosciences

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KSK19 – Novel histamine H3 receptor ligand reduces body weight in diet induced obese mice

Cited by 15 publications

References 29 publications

KD-64 – a new selective A_2Aadenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice

KD-64 – a new selective A_2Aadenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice

KD-64—A new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist—Caffeine does not reduce diet-induced obesity in mice

Targeting Histamine and Histamine Receptors for the Precise Regulation of Feeding

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KSK19 – Novel histamine H3 receptor ligand reduces body weight in diet induced obese mice

Cited by 15 publications

References 29 publications

KD-64 – a new selective A2Aadenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice

KD-64 – a new selective A2Aadenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice

KD-64—A new selective A2A adenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist—Caffeine does not reduce diet-induced obesity in mice

Targeting Histamine and Histamine Receptors for the Precise Regulation of Feeding

Contact Info

Product

Resources

About

KD-64 – a new selective A_2Aadenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice

KD-64 – a new selective A_2Aadenosine receptor antagonist has anti-inflammatory activity but contrary to the non-selective antagonist – caffeine does not reduce diet-induced obesity in mice