cannabisnews.com: New Compound That Acts on Peripheral Receptors 










  New Compound That Acts on Peripheral Receptors 

Posted by CN Staff on August 11, 2003 at 14:42:52 PT
Press Release  
Source: PRNewswire 

Washington -- Results of a new study in mice and rats show that a compound which acts on a specific type of cell receptor found only outside the central nervous system decreases the animals' pain responses. But the researchers caution that studies investigating the safety and efficacy of this compound in humans have yet to be done. The scientists hope this approach may lead to the development of pain- relief drugs that lack the debilitating central nervous system side effects limiting the effectiveness of currently available pharmaceuticals.
"Chronic pain is one of the most significant disease states affecting Americans, in terms of economic and social impacts," says Dr. Nora D. Volkow, Director of the National Institute on Drug Abuse. "And, unfortunately, therapeutic options for the treatment of chronic pain are inadequate, partly because a number of drugs that can be used to treat pain have unpleasant side effects that limit their effectiveness, and partly because some of them have the potential for addiction and abuse."The study, funded by NIDA, part of the National Institutes of Health, will be published online the week of August 11 in the Proceedings of the National Academy of Sciences.Dr. T. Philip Malan, Jr., of the University of Arizona, Dr. Alexandros Makriyannis, of the University of Connecticut, and their colleagues, studied the activity of a new compound called AM124, which acts on CB2 cannabinoid receptors. "This is one of the two types of receptors on which THC, the active ingredient in marijuana, acts," Dr. Malan says. "The CB2 receptors are in peripheral sites with immune functions, while the CB1 receptors are in the central nervous system -- the brain and spinal cord. The beauty of having a compound that acts on the CB2 receptors is that you can get pain relief without the central nervous system side effects of THC, such as sleepiness and anxiety."The scientists tested the chemical on mice and rats with neuropathic pain, a complex chronic pain state resulting from nerve injury or disease. They found that this compound increased the ability of the animals to withstand chronic pain that mirrored human models of neuropathic pain."Although this is far from being in clinical trials in humans, any new avenue to treat pain is a very positive step," Dr. Malan says. "Almost 6 million people in the United States may experience neuropathic pain. At almost any given time, about 1 person in 4 is experiencing some type of pain and about 1 person in 8 has some type of chronic pain. Pain costs the U.S. economy $120 billion to $180 billion per year. Even though we have therapies, many people continue to experience pain despite receiving treatment. This may be partly because the side effects of many of the drugs we can use prevent patients from using the dose that provides the most intense relief."The next step, he says, is to test this compound in animals to assess its potential toxicity. "We don't even know how it works. It may act on peripheral nerves, but CB2 receptors have not yet been found there; it may act in some way to inhibit the release of chemicals like prostaglandins from immune cells that increase sensitivity to pain; or they may cause immune system cells to release substances that block the pain response."AM1241 was developed by Dr. Makriyannis.The National Institute on Drug Abuse is a component of the National Institutes of Health, U.S. Department of Health and Human Services. NIDA supports more than 85 percent of the world's research on the health aspects of drug abuse and addiction. The Institute carries out a large variety of programs to ensure the rapid dissemination of research information and its implementation in policy and practice. Fact sheets on the health effects of drugs of abuse and information on NIDA research and other activities can be found on the NIDA home page at: http://www.drugabuse.govComplete Title: New Compound That Acts on Peripheral Receptors May Be Promising Treatment for Some Nerve PainSource: PRNewswire Published: Monday, August 11, 2003Copyright 2003 PRNewswire Website: http://www.prnewswire.com Contact: http://www.prnewswire.com/news/CannabisNews -- NIDA Archiveshttp://cannabisnews.com/news/list/NIDA.shtml

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Comment #15 posted by Petard on August 12, 2003 at 12:49:36 PT
Freedom Fighter
I'm down in Lowsyana (Louisiana) where there are many cases of human infection and there were a few deaths last year from W. Nile. The sprays used here (and there is a VERY active program) are designed to have a VERY short half life and to be only active on insects. They still publish requests for anyone with a known breathing issue to remain indoors and to turn off their AC units while the trucks and personnel are in the area though just to be safe. One problem is they still don't know what type(s) of mosquito carry the virus. There are several species that are suspect, each having their own unique feeding patterns. Some day, some night, some 24 hour opportunists. They also use some chemical pellets in ponds, ditches, and creeks to kill larvae.Wouldn't it be ironic IF the impact of cannabinoids on immune systems somehow acted as either a preventative or corrective to the W. Nile virus? Might be possible considering the cancer trials that have shown, if I remember and interpret the data correctly, increased levels of apoptosis of damaged cells. W. Nile is hard on the elderly for exactly that reason, it causes apoptosis and the elderly are unable to replace the dying cells fast enough, and thus suffer overall loss of cellular life and subsequent organ function loss. Also why the very young are indeed able to develop immunity to W. Nile as their rapidly growing bodies are more than able to compensate for the apoptosis. 
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Comment #12 posted by freedom fighter on August 12, 2003 at 12:11:09 PT

petard
"Even with W. Nile Virus making it across the N. American continent today there are cautions in place against the chemical controls used against skeeters."In Colo, where now 5 people dead of West Nile Virus, many towns start to spray stuff in the air.. in hope to reduce the number of mosquitoes. They would pack a sprayin machine in back of a truck and drive around sprayin the stuff during the evening. I have no idea what stuff it is..scary thought!pazff
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Comment #11 posted by Petard on August 12, 2003 at 10:37:09 PT

Better living through Chemistry
Was the saying of the times in their childhod formative years for the people in charge of NIDA. We'll have to wait a few more years for the generation that modified the saying a bit to include ORGANIC Chemistry when that next generation realized synthetics ruined the environment and health and turned to organics instead. Until then the establishment generation will be stuck in the loop of synthetics. Remember, kids used to play in the clouds of DDT sprayed by mosquito control units till the dangers were absolutely proven. Even with W. Nile Virus making it across the N. American continent today there are cautions in place against the chemical controls used against skeeters. We've come some distance, still a long journey ahead though on medications of an organic content. 
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Comment #10 posted by mayan on August 12, 2003 at 02:43:37 PT

goneposthole...
...here's another article on that topic. Very interesting! Time for a tax revolt?Jury acquits pilot, who questioned IRS, of tax-evasion counts:
http://www.gomemphis.com/mca/local_news/article/0,1426,MCA_437_2169609,00.html
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Comment #9 posted by afterburner on August 11, 2003 at 21:11:57 PT:

Great Link, goneposthole 
The First Amendment Right to petition the government for redress of grievances before paying taxes: if any group has a grievance against the US Government for violation of the Constitution, it is the cannabis culture."No Answers, NO Taxes" 
     DC speech by Bob Schulz, 11/14/2002 http://www.givemeliberty.org/FreedomDrive/PostFD/SchulzSpeech.htmego transcendence, the government of Jefferson, Emerson, and Whitman, follows ego destruction, the government of monarchy where the king owns everything.
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Comment #8 posted by ben on August 11, 2003 at 20:00:58 PT

Lets hope thier playing catchup
I believe that NIDA is not going to let GW pharm get all the 
glory with Bayer Lets hope thier going play catch up.
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Comment #7 posted by goneposthole on August 11, 2003 at 18:27:57 PT

when will this stop?
This might be a bad analogy, but I think this analogy is a good one (Smothers Brothers reasoning). Hard to imagine how it all will stop, but may go something like this: IRS Loses A Big One
Memphis Pilot Acquitted Of Tax Evasion
Charged With Filing "False" W-4s On Friday, a Memphis federal jury acquitted FedEx pilot Vernice Kuglin of six counts of felony Tax Evasion and Willful Failure to File tax returns.Ms. Kuglin's attorneys, Tax Honesty Movement barristers Larry Becraft and Robert G. Bernhoft, told reporters that Kuglin was indicted seven months ago and had refused to plead the case out for a lesser sentence. During her testimony Kuglin testified that since 1995, she had sent numerous letters to the IRS requesting that they inform her of what law required her to pay the Individual Income Tax. To this day, she has not received an answer. At 1:30 Friday afternoon, the jury returned not guilty verdicts on all counts.After the jury had been excused the U.S. Attorney reportedly demanded that the Judge order the defendant to file her forms, pay her taxes and obey the law. The Judge reportedly replied "Sir, I don't work for the IRS." The case is: U.S. District Court, Western District of Tennessee (Memphis) # 03-CR-20111, USA v. Kuglin.http://www.givemeliberty.org/RTPLawsuit/Update08-09-03.htm 
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Comment #6 posted by FoM on August 11, 2003 at 16:49:12 PT

Related Article from Reuters Health
Cannabis Spin-Off Eases Nerve Pain, in Rats August 11, 2003 By Will Boggs, MDNEW YORK (Reuters Health) - A cannabis-like drug currently undergoing lab tests may hold out relief for people with painful nerve damage in their arms or legs, without causing the "high" that comes with smoking pot.The effects of cannabis and related compounds come from the interaction of the drug with so-called receptors, which are of different types within the brain and central nervous system as opposed to outside the brain in other areas of the body.The CB1 receptors in the brain cause the mental effects of the drug, while the "peripheral" CB2 receptors are responsible for the benefits that some patients with glaucoma or cancer, for example, get from cannabis.Now scientists have developed a drug that acts mainly on the CB2 receptors."By targeting a specific class of cannabinoid receptors, we have developed selective cannabinoid drugs (drugs with actions similar to those of THC, the active ingredient in marijuana) that should lack the undesirable central nervous system side effects (such as sedation and anxiety) and the abuse potential of non-selective cannabinoid drugs," Dr. T. Philip Malan Jr. told Reuters Health.Malan, from the University of Arizona in Tucson, and associates tested the drug, known as AM1241, in lab rats that develop an exaggerated sensitivity to heat and touch, mimicking neuropathic pain.They found that increasing doses of the drug increasingly blocked the animals' responses to touch and heat. These beneficial effects of AM1241 were completely reversed when the animals were given a drug that blocked CB2 receptors, but not one that blocked CB1 receptors, the researchers report in the Proceedings of the National Academy of Sciences.Drugs like AM1241 that activate CB2 receptors have been shown to reduce various types of pain, Malan explained. "We have emphasized their actions in neuropathic pain because there is a strong need for new therapies for neuropathic pain."Despite the promise, he did sound a note of caution. CB2 receptors are found on immune cells, "and drugs acting on CB2 receptors can inhibit immune cell function." He doesn't think this will cause harmful immune suppression, because other drugs with similar effects do not, but it still needs to be looked at.SOURCE: Proceedings of the National Academy of Sciences of the USA, August 11, 2003, online Early Edition.

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Comment #5 posted by The GCW on August 11, 2003 at 16:24:18 PT

Gotta love those names!
CB1 cannabinoid receptor.CB2 cannabinoid receptor.Who do You think put those there?
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Comment #4 posted by FoM on August 11, 2003 at 15:35:56 PT

Herbal Medicine
I use different assorted herbs everyday and I can afford them. Pills costs lots of money and I know if I needed to take drugs I would have to do without. Natural medicine is much safer then pills. I don't know why Cannabis hasn't been rescheduled. It bothers me too.
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Comment #3 posted by afterburner on August 11, 2003 at 15:35:15 PT:

Die, NIDA, Die...Die, NIH, Die...Die, HHS, Die
Don't fool with Mother Nature. This is how the world was plagued with heroin, in a vain attempt to remove the addictive qualities of opium. Heroin, of course, turned out to be far more addictive. Now, let's disassemble cannabis and synthesize the components, all the while keeping the cannabis plant illegal. Let's try to remove that pesky "high". Oh, wait, better wait 66 years, freeze funding for future studies, and then claim that more studies are necessary before any "product" can reach the market. Let's let another black market spring up, so that we can dangerously inflate the price, and then we don't have to worry about quality control. Maybe we can farm out underground production to a third world country where the pay is low, and the laws on environmental safety, worker safety, and consumer safety are lax. That should increase profits. And think of all the new prisons, the jobs in law enforcement, the guns and ammunition this will inspire. What a boost to the economy!Oh, but wait, if we can patent it, then we can fast-track it through NAFTA in just 3 years. The WTO will surely approve. Of course, nobody voted for them, but we're making the world safe for democracy. The National Institute on Drug Abuse is a component of the National Institutes of Health, U.S. Department of Health and Human Services. NIDA supports more than 85 percent of the world's research on the health aspects of drug abuse and addiction. Thus spake the health vampires. No wonder the people of the world are confused.
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Comment #2 posted by drfistusa on August 11, 2003 at 15:29:17 PT

of course! 
no way they want us to have free or cheap pain relief when they can patent a synthetic and make BILLIONS! which they kick plenty back for the reelection of their protectors.
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Comment #1 posted by NoahTao on August 11, 2003 at 14:56:20 PT:

Are they waiting?
This study shows that NIDA is aware of the fact that CB1 and CB2 receptors are useful in the treatment of pain management. Its strange to me that they accept that CB1 and CB2 are important in treating pain but yet they fight Cannabis with such a vengance. It makes me wonder if they are just waiting for a pharm company to invent a cannabis based medicine before accepting its use. Anyone else think this might be true?
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