Competitors of opiates
How to Relieve pain without side effects
And anesthesia is one of the most important tasks of medicine, and not an easy one. Recently , scientists have proposed another option for creating effective and safe painkillers that are not related to narcotic drugs.
The most effective painkillers, as is known, are opioids – substances capable of binding to the receptors of the same name, which play a crucial role in the formation of pain syndrome. But opioids are dangerous because they cause serious addiction, as well as other negative side effects: nausea, dizziness, constipation and slowing of breathing until stopping. In addition, with prolonged use, they quickly lose their effectiveness, and the inevitable increase in the dose leads to even more pronounced undesirable effects.
So researchers are looking for and developing alternative painkillers that are not related to the function of opioid receptors. And such means are quite real, because other receptor systems and regulatory molecular cascades are also involved in the perception of pain.
Of considerable interest is one of the numerous subtypes of adrenergic receptors (i.e. reacting to the hormones adrenaline and norepinephrine) – α2A-adrenoreceptor (α2AAR). Activation of this receptor in the cells of the central nervous system has an analgesic effect. There are already drugs targeting α2AAR (for example, dexmedetomidine), but they have a strong sedative, sedative and hypnotic effect, which limits their use to hospital conditions.
In search of a compound that will activate the α2AAR receptor without sedation, a group of scientists using bioinformatics methods tested more than 301 million different molecules from the ZINC15 virtual molecular library. They were looking for compounds that would bind specifically and firmly to the α2AAR receptor, but would differ from those already known. As a result, about 50 compounds were first selected for synthesis and testing, of which two remained that met the specified criteria.
After additional optimization, several compounds were synthesized, which were tested in experiments on "animal models" of pain syndrome. It turned out that all of them effectively reduce pain reactions caused by stimuli of different nature, and at the same time do not cause a sedative effect even in high doses. Additional advantages – all these compounds are relatively easy to produce, while they can be taken orally (by mouth).
Article by Fink et al. The structure-based discovery of nonopioid analgesics acting through the α2A-adrenergic receptor is published in the journal Science.
Of course, so far we are talking only about fundamental research, because the development of medicines is not a quick matter, and not all of the promising drugs come to the finish line. But the more such works there are, the higher the chance of sufferers to get quick and safe pain relief.
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