Recently discovered groups of molecules are able to reduce pain without having the sedative effects that limit the use of opiates. These molecules act on the same receptors as clonidine and the dexmedetomidinebut they have no chemical bond and might not create addiction. Note that these two extremely powerful analgesics are rarely used outside of hospitals because they are very sedating.
The study aims to find analgesics that can be used with opioids. According to researchers from the University of California at San Francisco, the new molecules are the best alternatives to narcotics. The development of a drug that works in combination with a much lower dose of the opiate would be the goal.
It would better solve the problems of about 50,000 Americans with chronic pain and many others around the world.
Molecules never synthesized before
Allan Basbaum looked at an adrenergic receptor called alpha2a. He discovered that the latter was related to pain relief. Thanks to this, Brian Shoichet tried to find substances that could activate it.
For this purpose, he has browsed a virtual library of more than 300 million molecules to find those that would bind firmly to the receptor. He excluded too large molecules incompatible with the small receiver and sorted using a computer model the remaining tens of thousands. After many tests, he managed to reduce the number of molecules to six. These candidates were tested on three mouse models for acute and chronic pain. Each of the tests turned out to be a success.
None of these painkillers has not been synthesized so far. In addition, they concentrate in the brain and bind tightly to receptors.
“We have shown that it is possible to separate the analgesic and sedative effects linked to this receptor, which makes it a very promising target for drug development. »
Towards the development of a new painkiller
Despite the tests being successful, Brasbaum stresses that more research needs to be done before using them in a clinical trial. Researchers have yet to determine the effects of using these molecules on the long term. However, he believes the compound is not going to be addictive.
“Substance abuse occurs when the drug generates a reward, which has not been proven. »
Opioids are known to help fight pain related to surgery or cancers. However, people with chronic pain, joint pain, back pain and inflammatory diseases do not benefit from these treatments. Thus, the production of new painkillers could completely change the outlook for these patients.
SOURCE: SCITECH DAILY