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MK-212
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MK-212
MK-212, also known as 6-chloro-2-(1-piperazinyl)pyrazine (CPP), is a serotonin receptor agonist of the arylpiperazine family. It is specifically described as a non-selective serotonin 5-HT2 receptor agonist or as a "relatively selective serotonin 5-HT2C receptor full agonist. The drug promotes the secretion of serum prolactin and cortisol in humans.
MK-212 did not produce hallucinogenic effects in humans at doses of up to 40 mg orally. However, in other research, it occasionally produced LSD-like effects in alcoholic patients at a dose of 20 mg. In addition, subsequent studies found that MK-212 at 20 mg significantly increased ratings of feeling high and feeling strange.
MK-212 is an agonist of the serotonin 5-HT2 receptors, including the serotonin 5-HT2C, 5-HT2B, and 5-HT2A receptors, in that order of potency. It is a full agonist of the serotonin 5-HT2C receptor, a moderate-efficacy partial agonist of the serotonin 5-HT2B receptor, and a partial to full agonist of the serotonin 5-HT2A receptor. The drug shows similar potency in activating the serotonin 5-HT2C and 5-HT2B receptors and around 10- to 30-fold lower relative potency in activating the serotonin 5-HT2A receptor. It also shows low affinity for the serotonin 5-HT1A and 5-HT1B receptors. The comprehensive receptor interactions of MK-212 have been studied.
In a 1977 study by Clineschidt and colleagues, they dosed mice with varying concentrations of MK-212, and observed its effects. The result correlated very well to binding of indolealkylamine receptors, such as the serotonin and tryptamine receptors, which shows four characteristics. Namely, increased frequency of muscle twitching, head twitches, "an increase in the strength of the crossed extensor reflex in the acutely spinalized rat", and the cause of complex motor syndrome. In a later study, MK-212 dose-dependently induced the head-twitch response when combined with the selective serotonin 5-HT2C receptor antagonist SB-242084. In contrast to the preceding findings, MK-212 has been found to dose-dependently suppress the head-twitch response induced by the serotonergic psychedelic DOI, suggesting that serotonin 5-HT2C receptor activation may inhibit the head-twitch response.
MK-212 was first described in the scientific literature by 1977.
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MK-212
MK-212, also known as 6-chloro-2-(1-piperazinyl)pyrazine (CPP), is a serotonin receptor agonist of the arylpiperazine family. It is specifically described as a non-selective serotonin 5-HT2 receptor agonist or as a "relatively selective serotonin 5-HT2C receptor full agonist. The drug promotes the secretion of serum prolactin and cortisol in humans.
MK-212 did not produce hallucinogenic effects in humans at doses of up to 40 mg orally. However, in other research, it occasionally produced LSD-like effects in alcoholic patients at a dose of 20 mg. In addition, subsequent studies found that MK-212 at 20 mg significantly increased ratings of feeling high and feeling strange.
MK-212 is an agonist of the serotonin 5-HT2 receptors, including the serotonin 5-HT2C, 5-HT2B, and 5-HT2A receptors, in that order of potency. It is a full agonist of the serotonin 5-HT2C receptor, a moderate-efficacy partial agonist of the serotonin 5-HT2B receptor, and a partial to full agonist of the serotonin 5-HT2A receptor. The drug shows similar potency in activating the serotonin 5-HT2C and 5-HT2B receptors and around 10- to 30-fold lower relative potency in activating the serotonin 5-HT2A receptor. It also shows low affinity for the serotonin 5-HT1A and 5-HT1B receptors. The comprehensive receptor interactions of MK-212 have been studied.
In a 1977 study by Clineschidt and colleagues, they dosed mice with varying concentrations of MK-212, and observed its effects. The result correlated very well to binding of indolealkylamine receptors, such as the serotonin and tryptamine receptors, which shows four characteristics. Namely, increased frequency of muscle twitching, head twitches, "an increase in the strength of the crossed extensor reflex in the acutely spinalized rat", and the cause of complex motor syndrome. In a later study, MK-212 dose-dependently induced the head-twitch response when combined with the selective serotonin 5-HT2C receptor antagonist SB-242084. In contrast to the preceding findings, MK-212 has been found to dose-dependently suppress the head-twitch response induced by the serotonergic psychedelic DOI, suggesting that serotonin 5-HT2C receptor activation may inhibit the head-twitch response.
MK-212 was first described in the scientific literature by 1977.
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