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Author: Subject: dopamine vs mu activation
International Hazard

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[*] posted on 22-3-2016 at 16:24
dopamine vs mu activation

A little background- I do some volunteer work at the state prison. Over the years I've spoken with many opiate/opioid addicts. What I have learned is that craving is more about dopamine than mu receptors. Natural mu agonists in the brain recover faster than dopamine receptors. Methadone was the treatment of choice for many years but hasn't worked that well. Methadone patients seem to stay depressed. It's hard to sort this out because the setting, methadone clinics, are inherently depressing. Lot's of control. Lots of suspicion. Methadone patients are treated poorly in most environments. Definitely second class citizens or non-citizens. The message is, "you're not a citizen." For bikers that may be a source of pride but for the guys I have talked to and worked with, it's a harsh message. I'm convinced that methadone is a poor substitute for opiates. On the other hand the experience some of them have had with buprenorphine indicates a higher level of dopamine production. I think that's why it has been successful as a treatment despite the pain involved in getting on it. In case you're not aware buprenorphine is a mixed agonist/antagonist. The addict has to be in withdrawal to get on buprenorphine. I have a nephew by marriage that went through hell to get on it. He started with back pain and buying pills online. The expense was more than street drugs. He got on suboxone, a buprenorphine formulation with naltrexone added. That was 10 years ago and he hasn't relapsed which is a much better record than the usual methadone patient. I think people don't stay on methadone or supplement it with street drugs because of the lack of dopamine. From a chemical perspective the interest is in mu/dopamine probes. The easiest most accessible molecules are the fentanyl and pethidine types. Manipulation of these can lead to mixed agonist/antagonist medicines. For example mirfentanil is a specific antagonist to fentanyl. But it is also a strong analgesic with low respiratory depression.

Attachment: jm00106a051.New heterocyclakyl-4-propionalido-4-piperidinyl Methyl Ester and.pdf (1.8MB)
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[Edited on 23-3-2016 by chemrox]

Attachment: New 4-(Heteroanilido)piperidines, Structurally Related to the Pure Opioid Agonist .pdf (1.1MB)
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"When you let the dumbasses vote you end up with populism followed by autocracy and getting back is a bitch." Plato (sort of)
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International Hazard

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[*] posted on 1-4-2016 at 14:30

I've got no affection for the average junkie. Experience has taught me that they are usually terrible people. At least they are, when they are in the throes of addiction. That being said, they aren't going away any time soon. And, new enthusiasts, quickly take the place of those lost to attrition. Folks in psychic or physical pain, go searching for relief. Bet on it.

Gotta come up with better treatments. Had a currently "clean" friend, recommend Ibogaine. Helped her a lot. Sadly, treatment isn't legal here in the U.S..

Finding ways to boost endogenous opioids is my personal preference. Those long runs, long bike rides, and long hours in the more than make you look good. They are kinda painful...and they make you feel good.

Some passages in the above Ibogaine text, suggest that Ibogaine may increase receptor sensitivity or boost endogenous opioids. Perhaps, creating a scenario,
wherein the body can quell its own pain.

[Edited on 1-4-2016 by zed]

[Edited on 1-4-2016 by zed]

[Edited on 1-4-2016 by zed]
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Hazard to Others

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[*] posted on 21-4-2016 at 14:04

Honestly you gotta treat the underlying causes and get someone to value their lives. My theory on this is simple; humans exist in patterns of behavior as they draw comfort from predictability and routine, all patterns can be changed by noticing them and workin actively to change them, addiction is a corrupt pattern of behavior, addiction patterns can be changed by actively working to correct them. Addiction has no real answer as everyone has different reasons

The ones who get clean from methadone and suboxone were able to change their patterns after getting supplemented and assimilate back into normal life without opiates because the new pattern of behavior is Reinforced through time and repeat positive experiences. But that's just my take on it

Dopaime and neurotransmitters as well as receptor sites do get "repaired" over time that's why withdrawals end and even lingering after effects stop. If you spend more then a month in prison after using a short acting full agonist such as heroin you should be done with withdrawals in 7 days and past the lingering effects in a few months. That should mean receptor sites have been fully upgraded

[Edited on 21-4-2016 by szuko03]

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Redneck Overlord

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[*] posted on 21-4-2016 at 15:44

Addiction is a "tough row to hoe". I know this from bitter personal experience. Never liked opioids, thank God, but I did my first 100mg dose of desoxyephedrine intravenously. I was 18 and on active duty in the USMC. I finally "outgrew" it about a year ago. I'm 52. I was never a thief, but I damn sure was a dope head. It takes MANY MONTHS to fully shake the effects. It ain't a crime problem, its a public health issue.

@chemrox--BLESS YOU for volunteering at the State Prison. It really does more than you know for those guys. I know, I've done a number of years in the aggregate. (California H85481 and T01093).

“Travel is fatal to prejudice, bigotry, and narrow-mindedness, and many of our people need it sorely on these accounts. Broad, wholesome, charitable views of men and things cannot be acquired by vegetating in one little corner of the earth all one’s lifetime.”


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