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Chronic pain is still a universal health burden worldwide.
Opioids are currently one of the most widely prescribed analgesics for the treatment of moderate to severe acute pain , but the use of these analgesics often exhibits serious adverse reactions, such as breathing Inhibition, nausea and constipation, as well as addiction and tolerance, especially neuropathic pain
.
Opioids are currently one of the most widely prescribed analgesics for the treatment of moderate to severe acute pain , but the use of these analgesics often exhibits serious adverse reactions, such as breathing Inhibition, nausea and constipation, as well as addiction and tolerance, especially neuropathic pain
.
Chronic pain is still a universal health burden around the world, and opioids are currently one of the most widely prescribed analgesics for the treatment of moderate to severe acute pain
Recently, Monash researchers have achieved a breakthrough achievement, issuing non-opioid drugs to pave the way for safe and effective treatment of pain
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The study, published in Nature magazine .
Recently, Monash researchers achieved a breakthrough achievement, issuing non-opioid drugs to pave the way for safe and effective treatment of pain
Neuropathic pain is pain directly caused by damage to the somatosensory system or disease.
It can be caused by injury to peripheral nerves, posterior root of spinal cord, spinal cord and some parts of the central nerve above it caused by trauma and/or disease
Neuropathic pain is pain directly caused by damage to the somatosensory system or disease.
For a long time, targeting the adenosine A1 receptor protein has been considered as a therapeutic target for non- opioid analgesics in the treatment of neuropathic pain .
In this study, the researchers used electrophysiology and preclinical pain models to verify a special class of molecules, which is called " positive change".
Adenosine (purple sphere) and allosteric ligand MIPS521 (pink, green and purple) activate human adenosine A1 receptor (blue) .
At the same time, another breakthrough in this research is the application of cryo-electron microscopy (cryoEM) to solve the high-resolution structure of the A1 receptor and its natural activator, adenosine and analgesic PAM , thus providing the first atomic-level snapshot.
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At the same time, another breakthrough in this research is the application of cryo-electron microscopy (cryoEM) to solve the high-resolution structure of the A1 receptor and its natural activator, adenosine and analgesic PAM , thus providing the first atomic-level snapshot.
The study author stated, “The world is under the control of the global opioid crisis, and there is an urgent need for non-opioid drugs that are both safe and effective
Original source
Positive allosteric mechanisms of adenosine A1 receptor-mediated analgesia , Nature (2021).
