Central serotonin-like activity of 6-chloro-2-[1-piperazinyl]-pyrazine (CPP; MK-212)

Clineschmidt, Bradley V.; McGuffin, Jodie C.; Pflueger, A. Barbara

doi:10.1016/0014-2999(77)90117-0

Cited by 45 publications

(11 citation statements)

References 23 publications

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“…"Senkyu," activates adrenergic and serotonin receptors. 31) In addition, it has an effect on platelet aggregation 18) and blood viscosity. 18) Furthermore, 2,5-dimethylpyrazine has effects on β-adrenergic receptors and uterine contraction.…”

Section: )mentioning

confidence: 99%

2-Ethylpyrazine Induces Vasodilatation by Releasing Nitric Oxide in the Endothelium

Ashigai

Ikeshima

Koizumi

et al. 2017

Biological & Pharmaceutical Bulletin

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Oxygen transportation and regulation of some physiological processes are facilitated by blood flow. Furthermore, blood flow is regulated by various factors such as nitric oxide (NO) and the autonomic nerve system. In modern life, many people suffer from chilliness (hiesho) because of mental stress and an excessive use air-conditioning systems, which induces vasoconstriction in the peripheral skin. In this study, we focused on pyrazine derivatives, particularly compounds that are used as food flavoring materials, and investigated their effects on vascular function and blood flow. We examined the vasodilatory effect of pyrazine derivatives in the rat thoracic aorta and found 2-ethylpyrazine (2-EP) to be the most active pyrazine compound. Additionally, we found that 2-EP induces vasodilatation through the activities of endothelium-derived relaxing factors. 2-EP activates NO synthesis through the effect of endothelial NO synthase in the endothelium. As a result, cyclic GMP levels rise in smooth muscle cells and vasodilatation is induced. We also confirmed that 2-EP increases peripheral blood flow in rats. From these results, we concluded that 2-EP induces vasodilatation by inducing the release of NO and increasing peripheral blood flow.

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Section: )mentioning

confidence: 99%

2-Ethylpyrazine Induces Vasodilatation by Releasing Nitric Oxide in the Endothelium

Ashigai

Ikeshima

Koizumi

et al. 2017

Biological & Pharmaceutical Bulletin

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“…The repetitive extrasystole threshold also increased after the intravenous administration of 5-methoxytryptophol, a compound occurring naturally in the pineal gland and closely related to melatonin, and 6-chloro-2-(l-piperazinyl)-pyrazine (MK-212), a synthetic agent chemically unrelated to melatonin or 5-methoxytryptophol but demonstrated to elicit distinct responses characteristic of serotonin receptor activation in the central nervous system (Clineschmidt et al, 1977). Melatonin, 5-methoxytryptophol, and MK-212 share a central serotonergic action and each raises the repetitive extrasystole threshold.…”

Section: Effects Of Mk-212 After Vagotomymentioning

confidence: 99%

“…Metergoline is a specfic serotonin antagonist, lacking activity at cholinergic, adrenergic, and histaminic receptor sites, and is effective in blocking central serotonergic reflex responses to MK-212 in rodents (Clineschmidt et al, 1977). Metergoline alone had no significant effect on the repetitive extrasystole threshold or heart rate, but blocked responses to MK-212.…”

Section: Effects Of Mk-212 After Vagotomymentioning

confidence: 99%

“…Mice receiving melatonin intraperitoneally (30 mg/kg) showed no alteration in gross behavior and no change in levels of norepinephrine in the heart or brain. Clineschmidt et al (1977) have shown that MK-212 produces a serotonin-like action in the central nervous system. When administered systemically to rats and mice, MK-212 elicited four distinct responses characteristic of serotonin-receptor activation in the brain.…”

Section: Effects Of Mk-212 After Vagotomymentioning

confidence: 99%

“…The aim of the present investigation was to identify chemical and endogenous compounds that act through the central serotonin system to raise the cardiac threshold without the assistance of enzyme inhibitors and to learn more about the mechanism of their action. Since administration of pineal gland hormone, melatonin, increases brain serotonin (Anton-Tay et al, 1968), it was relevant to examine its action on cardiac vulnerability, as well as effects of related compounds, namely, 5-methoxytryptophol and 6-chloro-2-(l-piperazinyl)-pyrazine (MK-212, Merck) (Clineschmidt et al, 1977).…”

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confidence: 99%

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Central serotonergic agents raise the repetitive extrasystole threshold of the vulnerable period of the canine ventricular myocardium.

Blatt¹,

Rabinowitz²,

Lown³

1979

Circulation Research

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1982

Chemistry of Heterocyclic Compounds: A Series of Monographs

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Central serotonin-like activity of 6-chloro-2-[1-piperazinyl]-pyrazine (CPP; MK-212)

Cited by 45 publications

References 23 publications

2-Ethylpyrazine Induces Vasodilatation by Releasing Nitric Oxide in the Endothelium

2-Ethylpyrazine Induces Vasodilatation by Releasing Nitric Oxide in the Endothelium

Central serotonergic agents raise the repetitive extrasystole threshold of the vulnerable period of the canine ventricular myocardium.

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