With the opioid epidemic underway, the question of how to reverse direction is on everyone’s mind. Governments are succumbing to pressure; passing decriminalization measures, and opening safe use sites, but none of this attacks the problem. Though a ketamine answer exists, its been all but ignored in terms of the general public, which is 100% unaware of this. And now, a new pain pill is under research, but is still completely untested. What is BnOCPA, and how does it measure up?
There’s a new non-opioid painkiller under research called BnOCPA, and it might be a very much needed alternative to the current and awful opioid situation. We’re a cannabis and psychedelics news site which specializes in breaking news and ongoing stories in these industries, and beyond. We provide the Cannadelics Weekly Newsletter for readers to stay updated, as well as obtain access to an array of product promotions on vapes and other smoking devices, edibles, and cannabinoid compounds including the super-popular Delta 8 & HHC. Head to our ‘best of’ lists for more info, and buy yourself some awesome new swag.
Why it matters
There are a ton of pharma products on the market, and plenty for pain. Aside from opioids, which dominate the scene, we’re pretty used to our Tylenol, and NSAIDS like aspirin, and ibuprofen. For the entirety of my life, the process has been to pop a pill for pretty much anything. Skin your knee? Take a pill. Got a headache? Take a pill. That time of the month? Take a pill. It’s a wonder anyone knows what pain feels like anymore.
Prior to our new-age pharma world, if you hurt yourself, you just had to deal with it. Or use the natural medicine version, which, let’s be honest, isn’t the worst. All those opioids that are causing so much problem, are all based on compounds from the poppy plant, and those compounds have existed, and been implored in local medicine traditions, for as long as people have lived in organized communities.
In light of the massive addiction and death numbers of late, it’s a wonder people are more willing to pop the pill, than simply tough it out. After all, it was standard once to have children without an epidural, or to cut off diseased limbs without an anesthetic. While I’m not saying progress isn’t good, I am saying that in this case, it came with a cost. Obviously, the logic of ‘we didn’t need it before, so we don’t need it now’ isn’t the best, but it’s not worthless either. It mainly fails because if nothing else, we live way longer than humans used to, meaning an increase in pain related issues from aging, and overall more years to experience accidents and mishaps.
As of right now, that issue of trying to get away from the pain, is manifesting in the form of overdose deaths from opioids. According to preliminary data released by the CDC in May of this year, 2021 had approximately 107,622 overdose deaths. And while we don’t know the exact breakdown of causes, we know that of 2020’s 93,000 overdose deaths, that over 68,000 were opioid related. That’s a lot of people dying from drugs prescribed by a doctor. How prevalent are these prescriptions? As of a 2021 analysis, in 2019, 22.1% of all US adults with chronic pain, obtained an opioid prescription within the last three months of the question. In 2017, it accounted for 191 million prescriptions.
BnOCPA – What is this stuff?
Right now, when it comes to dealing with chronic and extreme pain, opioids are the go-to prescription medication, though this has shown to be a very bad idea in terms of addiction rates to the medications, and accompanied overdoses. Opioids are synthetically made compounds based on the poppy plant. When compounds are taken directly from the plant, they’re called opiates, but when made synthetically, but based on the compounds of the plant, they’re opioids. Opioids include drugs like fentanyl and the main component of Oxycontin, oxycodone.
Opioids assert their action by attaching to opioid receptors in the nervous system, and gastrointestinal tract. The three main opioid receptor classes are mu, kappa, and delta – μ, κ, δ, though there are 17 of these receptors currently known about. They operate as heavy pain relievers, as well as anesthetics; with prescription uses for things like diarrhea and cough suppression as well.
BnOCPA is a newly made synthetic compound that recently came to global attention with the results of a recent investigation. BnOCPA, or benzyloxy-cyclopentyladenosine, is a G-protein-coupled receptor agonist (GPCRs). Research into this compound was carried out by a group of investigators based out of the University of Warwick’s School of Life Sciences (in conjunction with University of Bern, University of Cambridge, Coventry University, Monash University, and different industrial organizations). According to their study, Selective activation of Gαob by an adenosine A1 receptor agonist elicits analgesia without cardiorespiratory depression, this compound:
“…is a potent and powerful analgesic but does not cause sedation, bradycardia, hypotension or respiratory depression.” This occurs because of “BnOCPA’s unique and exquisitely selective activation of Gob among the six Gαi/o subtypes, and in the absence of β-arrestin recruitment.”
They go on to explain that the compound “demonstrates a highly-specific Gα-selective activation of the native A1R,” which “sheds new light on GPCR signalling,” and which “reveals new possibilities for the development of novel therapeutics based on the far-reaching concept of selective Gα agonism.” This is different from other adenosine receptors, like the A1 receptors, which though showing potential in this realm, are weighed down by side effects of sedation and cardiorespiratory depression.
How does BnOCPA differ from opioids?
When it comes to extreme, chronic pain, medications like Advil and Tylenol can’t help much, and we know this because enough time has gone by to understand where their abilities end. Different kinds of pain medication vary in how much coverage they can realistically provide. When looking at other options to opioids, this has to be considered, because the medication must be strong enough to solve the problem, while not including the negative side effects that lead to overdose and death.
Opioid receptors are also G-protein-coupled receptors, meaning opioids attach to the same kinds of receptors as this new compound, BnOCPA. But that doesn’t mean the two different compounds create the same response, and there’s a particular reason why. G-proteins cause a lot of different effects, and drugs like opioids inadvertently set off several kinds of them because they’re not selective in where they bind. The pain-relieving effects are therefore included with unwanted effects (or side effects), as well.
BnOCPA functions a bit differently in that its way more selective about where it binds, thus only triggering one kind of G-protein. This ability for selection can minimize the amount of side effects that come with the medication, hence the aforementioned ability for pain control, without causing sedation or respiratory depression. As sedation and respiratory depression lead to overdose when too much of a drug creating these actions is taken, the ability to get around this means a possible way to treat pain, without worrying about a death toll.
According to lead researcher Dr. Mark Wall, “The selectivity and potency of BnOCPA make it truly unique and we hope that with further research it will be possible to generate potent painkillers to help patients cope with chronic pain.”
This finding came unexpectedly. Says Professor Bruno Frenguelli of the research team, “This is a fantastic example of serendipity in science. We had no expectations that BnOCPA would behave any differently from other molecules in its class, but the more we looked into BnOCPA we discovered properties that had never been seen before, and which may open up new areas of medicinal chemistry.”
What do we actually know beyond these statements? Unfortunately, nothing. While it sounds super awesome thus far, it should be remembered that this is one study on a compound that’s never been used before. It must be researched further, and undergo a slew of testing, including human trials, before anything further is known for sure. We don’t know what kind of pain it can handle, how safe it is for long term use, or if there is an addiction potential. Right now, the only thing we know is that an untested compound was created, that might provide an alternative to opioids.
Why not ketamine?
I harp on this a lot, but for good reason. Yeah, there’s a massive issue right now with opioids killing people. So massive that to cope with it, some locations are giving up and decriminalizing the drugs, or instituting programs like safe use sites to try to minimize deaths. However, despite all measures, overdose rates are very clearly rising, indicating that nothing is getting better, and that even bigger problems should be expected in the future.
So, yeah, its great that alternatives are getting some attention, but let’s be honest for a second, BnOCPA is new, and untested. Maybe it provides a better option, but we won’t know that for quite some time, because long term data requires a lot of time, or its not long term data. We can only know those answers by people using it through time, or studies that follow long-term use. Meaning since we have this problem right now, if there is another method that is tested, and safe, and which might provide extra benefits, like long-lasting relief between administration sessions, it should be used. Immediately. Right?
Well, we have a drug that is comparable to opioids in terms of chronic and acute pain management. One which, like BnOCPA, has that ability for pain relief without causing sedation or cardiac depression, and which actually has the capacity to work for months after administration (find me an opioid that lasts the amount of time its supposed to, let alone longer). And yet here we are talking about a new and untested compound, instead. Maybe BnOCPA does work, is safe, and isn’t addictive, but you know what we already know works, is safe, and isn’t addictive? Ketamine.
The real question when a story like this comes out, isn’t whether BnOCPA can provide a better option to opioids, but why we aren’t talking about the already tested and safe medications we actually have access to now. Sure, its great to create and research new compounds, but when it comes to an answer to the opioid epidemic, and one that is accessible immediately, BnOCPA isn’t it. However, ketamine is.
The pharma world is a confusing place, and its not always clear why one thing is pushed and another is not. While BnOCPA might be a new contender in the opioid battle, if we really want to win this war, we need to use all the artillery in our arsenal. And right now, a new and untested compound doesn’t compare to one that’s been around since the 60’s, with accumulated use and safety information since that time.
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