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All 6 posts Subject: Novel Cannabinoid Appears Promising for Treatme... Please login to post Down

longimanus
(Hive Bee)
08-31-04 20:19
No 528567
User Picture       Novel Cannabinoid Appears Promising for Treatme...

Novel Cannabinoid Appears Promising for Treatment of Chronic Pain
by Robert Mathias, NIDA NOTES Staff Writer

Trauma, infection, and deseases such as diabetes can damage nerves, causing pain that persists long after the acute condition has been resolved. Such chronic pain, called neuropathic to signify that it is caused by injuries to nerves themselves rather to surrounding tissues, is difficult to treat. The strongest analgesics, the opioids, such as morphine and fentanyl, often only partially control it. Moreover, the opioids` side effects, which include constipation, nausea, anxiety, sedation, and respiratory depression, make long-term dosing to control persistent, intractable pain problematic. The opioids` potential for physical dependance and addiction places additional constraints on long-term use.
Better relief may be on the way, however, for patients with chronic neuropathic pain as well as others. NIDA-funded researchers recently created and tested a new experimental analgesic compound that reduced pain caused by nerve damage in mice and rats without apparent undesirable side effects. Further, the compound also showed efficacy in inflammatory pain. If these preliminary findings hold up, the compound could fulfill a longstanding need for controlling pain due to neuropathy and also to conditions, such as cancer, that can cause pain through multiple mechanisms.

The rest (http://drugabuse.gov/NIDA_notes/NNvol19N2/Novel.html)

The compound from the article is known as AM1241 - (2-iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-indol-3-yl)methanone:
Molecule: AM1241 ("O=C(C4=CC(N(=O)=O)=CC=C4I)C1=CN(CC3N(C)CCCC3)C2=C1C=CC=C2")

Lilienthal
(Moderator)
08-31-04 20:35
No 528571
User Picture       That's a selective CB2 receptor ligand.

That's a selective CB2 receptor ligand. The psychoactive effects of THC are mediated by central CB1 receptors, the CB2 receptors are located peripherally.

See Medline (PMID=12917492) / DOI:10.1073/pnas.1834309100 for:
Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain: pain inhibition by receptors not present in the CNS. Proc. Natl. Acad. Sci. U S A 2003 100(18):10529-10533

Fastandbulbous
(Hive Bee)
09-01-04 02:16
No 528663
User Picture       Cannabinoid releif of neuropathic pain

I've found that cannabis provided relief from phantom limb pain when opiates etc did not (or at least did not very well), but to find that it was due to the CB2 receptors comes as a bit of a surprise for the following reason:

I have found one quality which is always associated with the pain relief effects, namely that of a distorted body image, and as that is an effect due to the central effects of THC at the CB1 receptor, you can see why I am a little surprised.
The distortion of body image seems to be associated with neuropathic pain relief in my experience as I have gained relief on one occasion after LSD, which as far as I've seen, has no affinty for any CB receptor (note: I didn't take the LSD to prevent the pain, it just happened that way).
Ketamine also gives pain-relief, but it's body image distortion is purely due to the blocking of all sensory input, as opposed to a more subtle effects of LSD

That is right, the Mascara Snake: Fast and bulbous

jsorex
(Hive Addict)
09-01-04 02:29
No 528675
User Picture       Actually many pain theories assosiate pain...

Actually many pain theories assosiate pain control with body image. For instance if you think that the pain is an entity like thing in your body it is easier to seperate it from your ego/subject and then you feel relieved. Perhaps the same type of thought could be applied here with your LSD and cannabis examples...

paranoid
(Quick-witted Quibbler)
09-01-04 04:23
No 528749
User Picture       My brother, who suffered from very painful...

My brother, who suffered from very painful spasms in one of his legs after being partially paralysed, found MJ to be of little use. However, that may have more to do with the fact it always made him very paranoid.

I've noticed that when I'm very stoned or on LSD/shrooms, I have this effect where I can be scratching my nose, and feel the hand and nose, yet at the same time feel entirely detached from it. It's as though someone else is scratching and I'm scratching someone else's nose at the same time.

Ok, hard to explain. But I think it may be related to the effect mentioned by Fastandbulbous - you know the pain is there, but become detached from it.

My ideal vacation - Juxtaposed along the precipice intersecting reality and fantasy (i.e. wanking).

longimanus
(Hive Bee)
09-01-04 06:10
No 528792
User Picture       cannabinoid analgesia

Most probably, IMHO, the analgesic action of the selective CB₂R agonists should be similar to that of, for example, ibuprofen. Nothing to do with psychological effects. (To be honest, at higher doses MJ I`ve felt pain, not relief. But that pain is something different from the usual one we know - it`s possibly just an illusion.)
Oh, yes - proofs for the above statement? I don`t have, I haven`t tried selective CB₂R agonists. But refering to the old indomethacin and its derivates:
Inhibitors of enzymes involved in anandamide metabolism including phenylmethylsulfonyl fluoride, superoxide dismutase, and indomethacin...
The selective CB2 receptor ligands JWH-015 and indomethacin morpholinylamide (BML-190)...

Whatever it means wink

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	All 6 posts		Subject: Novel Cannabinoid Appears Promising for Treatme...		Please login to post		Down


		longimanus (Hive Bee) 08-31-04 20:19 No 528567				Novel Cannabinoid Appears Promising for Treatme...
						Novel Cannabinoid Appears Promising for Treatment of Chronic Pain by Robert Mathias, NIDA NOTES Staff Writer Trauma, infection, and deseases such as diabetes can damage nerves, causing pain that persists long after the acute condition has been resolved. Such chronic pain, called neuropathic to signify that it is caused by injuries to nerves themselves rather to surrounding tissues, is difficult to treat. The strongest analgesics, the opioids, such as morphine and fentanyl, often only partially control it. Moreover, the opioids` side effects, which include constipation, nausea, anxiety, sedation, and respiratory depression, make long-term dosing to control persistent, intractable pain problematic. The opioids` potential for physical dependance and addiction places additional constraints on long-term use. Better relief may be on the way, however, for patients with chronic neuropathic pain as well as others. NIDA-funded researchers recently created and tested a new experimental analgesic compound that reduced pain caused by nerve damage in mice and rats without apparent undesirable side effects. Further, the compound also showed efficacy in inflammatory pain. If these preliminary findings hold up, the compound could fulfill a longstanding need for controlling pain due to neuropathy and also to conditions, such as cancer, that can cause pain through multiple mechanisms. The rest (http://drugabuse.gov/NIDA_notes/NNvol19N2/Novel.html) The compound from the article is known as AM1241 - (2-iodo-5-nitrophenyl)(1-((1-methylpiperidin-2-yl)methyl)-1H-indol-3-yl)methanone: Molecule: AM1241 ("O=C(C4=CC(N(=O)=O)=CC=C4I)C1=CN(CC3N(C)CCCC3)C2=C1C=CC=C2")



		Lilienthal (Moderator) 08-31-04 20:35 No 528571				That's a selective CB2 receptor ligand.
						That's a selective CB2 receptor ligand. The psychoactive effects of THC are mediated by central CB1 receptors, the CB2 receptors are located peripherally. See Medline (PMID=12917492) / DOI:10.1073/pnas.1834309100 for: Activation of CB2 cannabinoid receptors by AM1241 inhibits experimental neuropathic pain: pain inhibition by receptors not present in the CNS. Proc. Natl. Acad. Sci. U S A 2003 100(18):10529-10533



		Fastandbulbous (Hive Bee) 09-01-04 02:16 No 528663				Cannabinoid releif of neuropathic pain
						I've found that cannabis provided relief from phantom limb pain when opiates etc did not (or at least did not very well), but to find that it was due to the CB2 receptors comes as a bit of a surprise for the following reason: I have found one quality which is always associated with the pain relief effects, namely that of a distorted body image, and as that is an effect due to the central effects of THC at the CB1 receptor, you can see why I am a little surprised. The distortion of body image seems to be associated with neuropathic pain relief in my experience as I have gained relief on one occasion after LSD, which as far as I've seen, has no affinty for any CB receptor (note: I didn't take the LSD to prevent the pain, it just happened that way). Ketamine also gives pain-relief, but it's body image distortion is purely due to the blocking of all sensory input, as opposed to a more subtle effects of LSD That is right, the Mascara Snake: Fast and bulbous



		jsorex (Hive Addict) 09-01-04 02:29 No 528675				Actually many pain theories assosiate pain...
						Actually many pain theories assosiate pain control with body image. For instance if you think that the pain is an entity like thing in your body it is easier to seperate it from your ego/subject and then you feel relieved. Perhaps the same type of thought could be applied here with your LSD and cannabis examples...



		paranoid (Quick-witted Quibbler) 09-01-04 04:23 No 528749				My brother, who suffered from very painful...
						My brother, who suffered from very painful spasms in one of his legs after being partially paralysed, found MJ to be of little use. However, that may have more to do with the fact it always made him very paranoid. I've noticed that when I'm very stoned or on LSD/shrooms, I have this effect where I can be scratching my nose, and feel the hand and nose, yet at the same time feel entirely detached from it. It's as though someone else is scratching and I'm scratching someone else's nose at the same time. Ok, hard to explain. But I think it may be related to the effect mentioned by Fastandbulbous - you know the pain is there, but become detached from it. My ideal vacation - Juxtaposed along the precipice intersecting reality and fantasy (i.e. wanking).



		longimanus (Hive Bee) 09-01-04 06:10 No 528792				cannabinoid analgesia
						Most probably, IMHO, the analgesic action of the selective CB₂R agonists should be similar to that of, for example, ibuprofen. Nothing to do with psychological effects. (To be honest, at higher doses MJ I`ve felt pain, not relief. But that pain is something different from the usual one we know - it`s possibly just an illusion.) Oh, yes - proofs for the above statement? I don`t have, I haven`t tried selective CB₂R agonists. But refering to the old indomethacin and its derivates: Inhibitors of enzymes involved in anandamide metabolism including phenylmethylsulfonyl fluoride, superoxide dismutase, and indomethacin... The selective CB2 receptor ligands JWH-015 and indomethacin morpholinylamide (BML-190)... Whatever it means

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