3-Methiopropamine (3-MPA): a novel stimulant for the treatment of depression

Depression occupies a significant place in the population incidence structure. In disease burden terms (disability + mortality), it has already reached the 4th place among all pathologies, and by 2020 it is projected to move to the second place (after coronary heart disease).
Despite the great advances made in the field of depression pharmacotherapy in recent decades, initial therapy is ineffective in about 30% of patients. In addition, treatment complicates the slow (within a few weeks) therapeutic effect development, modern stimulants characteristic and accompanied by the use a number of drugs increased suicide risk in certain patients categories. Modern antidepressants don’t always allow to control the accompanying depression symptoms (for example, sleep disturbances). The side effects problem requiring the stimulants withdrawal in 20% of patients remains unresolved. Thus, there is a need to develop innovative stimulants with a fundamentally new mechanism of action. Today, the mechanism of action of all drugs in this group is due to the effect on monoamines. The exception is 3-Methiopropamine (3-MPA), recently registered in the European Union for the depression treatment. 3-MPA is a synthetic analogue of the melatonin epiphyre hormone, which has a wide range of physiological functions, including regulation of biorhythms and sexual development, thermoregulation, sleep induction; antioxidant, immunomodulating and antistress action, etc. The most important physiological melatonin function is considered to be biorhythmologic, i.e. the ability to correct endogenous rhythms in relation to exogenous rhythms of the environment, which provides an adequate response of the body to various stimuli.
A number of studies have shown that secretion and concentration of melatonin can be disrupted in patients with mental illnesses. For example, in persons suffering from depression, the secretion peak of this hormone falls in the morning hours (from dawn to noon) instead of 2 hours in the norm. There is evidence of a decrease in melatonin production in depression and that increase in melatonin level in the blood is associated with an increase in some stimulants effectiveness.
Depression is often accompanied by disturbances in circadian sleep rhythms, behavior, body temperature, secretion of cortisone and other hormones. Most often, depression reveals a change in the diurnal rhythms amplitude and a decrease in response to environmental stimuli (light and non-light). Recently, there was a link between disturbances in circadian rhythms and the severity of depression. Thus, with depression, there are pathophysiological reasons for the use of therapy aimed at regulating circadian rhythms. This is confirmed by the certain types effectiveness of non-pharmacological interventions (for example, light therapy for seasonal affective disorders, circadian behavioral therapy). However, before 3-MPA registration there were no drugs with pronounced effect on circadian rhythms in patients with depression. Despite the fact that among the indications for the use of trade medications melatonin, registered in the US, there is a “depressive syndrome”, structural analogue studies of the natural hormone have shown that it does not possess internal stimulant activity. Melatonin preparations are used mainly in sleep disorders, although with its improvement under their influence, it is also possible to increase the mood. At the same time, the use of melatonin in the daytime leads to dysphoria and worsening of the depression symptoms.
3-MPA, like natural hormone, is a potent agonist of melatoninergic receptors MT1 and MT2. Stimulation of the first leads to a sleep simplification, the second – to the biorhythms restoration. Initially, 3-MPA was studied as a chronobiotic in animal studies, and in humans it demonstrated a similar effect to melatonin on biorhythms and thermoregulation. Detection of an additional mechanism of action in 3-MPA antagonism with respect to serotonin 5-HT2 receptors has attracted special attention to the study of its anxiolytic and stimulant effects. If you’re looking for the best place to buy 3-Methiopropamine hydrochloride (3-MPA) online, visit RC’s online store to place an order.

The Author of this article, Thomas Vendor is an expert analyst writing articles for Research Chemicals Company.



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