Author Topic: 6Momo Propionic Ester Morpines from Pods By Jon @ WD's (Read 837 times)

jon · « **Reply #40 on:** October 02, 2009, 10:21:29 PM »

nope the cooler the better no need for solvents can use solvents on basic material but meconate salts solvents will just precipitite out the real problem here is watching the temp while evaping the water solution it has to be well under 80 C more like 70 or lower swij fucked off 120$ of morphine learning that.
the acylation is best run below 100 C too as heat and time can ruin your shit.
try70-80 C run 6 hours.
last time swij dicked with this shit he was banging into stuff nodding off while walking and falling into things passing out and coming to like the next day bee careful.
oh and the bruises and injuries sustained man this stuff just does you wrong.
that's heroin.
to answer the proportion question 10 cc per gram is good rule of thumb although literature states you can get away with much less like 3/1 stochiometry this is done in solvents usually acetone and only on the morphine base.
swij is ambivalent about this stuff it's good if your laid up and about to die in a hospice but if your up and about you can easily injure yourself because you can't feel pain until the next day.
be warned.

2bfrank · « **Reply #41 on:** October 03, 2009, 01:32:09 AM »

Dam, I dont konw if hes fucked this up, so here goes, the small amount, as discussed, brown syrypiy goo...he added to that about 8ml of the anhydride, and a pinch of sodium acetate(dry) but baring in mind, the small scale shouldn't produce to much propanoic acid, but he just added a pinch, so he sat it in boiling H2O, and did this for hours, and the mix, hardly caused condensation onthe sides of the glass, in frustration he added 4 ml of dry dry DCM, and this has reduced its densness, Dont know if tha has fucked it, and done in frustration, late at night, bit waked to, so hell put it back on the boiling water, check regularly so that the temp doesn't hit over 80, but it shouldn't get that..So has he fucked it or not.. youve mentioned no solvent that canform salt, so perhaps hes cool..the only problem, is, when Ive had it sitting submerged in hot water, simmering hot, the temp didn't even hit 70, thought to change to oil, but with baby sitting.and temp testing

No its sitting at 75C, just one thing, is keeping moisture out of the mix worthwhile, Ive left it open, to remove the DCM, and perhaps will put a condenser with drying tube, I dont want to fuck this up, albeit a tester hence SMALL scale..

jon · « **Reply #42 on:** October 03, 2009, 03:06:15 AM »

your good if some geasy mexican can pull this shit off it aint that technical really.
those temps are right you could let it go 3 hours or longer.

2bfrank · « **Reply #43 on:** October 03, 2009, 03:31:30 AM »

WTF are you talking about, I am mexican, and so what if Im greasy,,FUCK YOU>.

hypnos · « **Reply #44 on:** October 08, 2009, 03:01:34 AM »

when you say "hot" ipa,, about what temp are we talkiing about?

jon · « **Reply #45 on:** October 08, 2009, 03:05:06 AM »

umm use your judgemeny if it's dry boiling if it has water heat it in a vessel on a water bath add ipa stir and mix very well
decant the ipa off and repeat until no more color.
check out my other post in the psychoactive forum on aussie poppy seed at $5 a pound you can extact a gram of morphine at a cost of $50 cheaper than pods.

hypnos · « **Reply #46 on:** October 08, 2009, 03:31:17 AM »

matey you are a man after my heart!!!!! are you also a happy camper in d land of oz?

2bfrank · « **Reply #47 on:** October 08, 2009, 11:49:32 AM »

Quote from: jon on October 08, 2009, 03:05:06 AM

umm use your judgemeny if it's dry boiling if it has water heat it in a vessel on a water bath add ipa stir and mix very well
decant the ipa off and repeat until no more color.
check out my other post in the psychoactive forum on aussie poppy seed at $5 a pound you can extact a gram of morphine at a cost of $50 cheaper than pods.

Thats how frank went, but as a tester, and yep.

jon · « **Reply #48 on:** October 09, 2009, 04:21:19 AM »

well swij is'nt from oz but helping out a fellow researcher down there he stumbled on this little tidbit seems they don't wash thier seeds as they do in other places hopefully the authorities din't change this.
the problem extracting the goods from poopy seed seems to be the oils carried with it some have employed a technique where they dissolve the extract in water and heat with parrafin wax to remove the oils from the extract a crude way of washing something in organic chemistry i suppose.

jon · « **Reply #49 on:** October 11, 2009, 06:29:53 AM »

hey all read this paper now in the reducing process swij mentioned a lot of morphine can be ruined if you follow swij's previous advice so he offers this as a correction to save a lotof cussing believe me swij's already been there until he figured out it was'nt a function of temperature as much as it was ph.

http://books.google.com/books?id=qw4P5AABgmEC&pg=PA605&lpg=PA605&dq=morphine+degradation+pseudomorphine&source=bl&ots=7AGQoFbolB&sig=4gYuZU4a55ygjgy4mBTLabPtD8A&hl=en&ei=T_vPSr62N8vf8QbQgYn_Aw&sa=X&oi=book_result&ct=result&resnum=8&ved=0CB8Q6AEwBzgU#v=onepage&q=morphine%20degradation%20pseudomorphine&f=false

hypnos · « **Reply #50 on:** October 11, 2009, 11:23:52 PM »

once again matey you are on d money!!! however it is clear that temps over 80c+ are not particularlybeneficial yes i dig!!!!
i'm surprised in all the data around the place on opiates in general that this degradation due to ph is not mentioned elsewhere....

aslso the article mentioned using sodium pyrosulphate as a 'stabiliser'...hmmmmmmm....tho they are talking of the hydrochloride
are all esters affected similarly? maybe not but i'm not sure where to look (except here!!)
i cant find much WTSE+limited time i have at d mo to "play"

hypnos · « **Reply #51 on:** October 12, 2009, 03:43:00 AM »

and.. jon have you come across this??

.There is much debate on the best preparations of poppy tea. Many claim that boiling rapidly is the best, others insist on strictly cold water, and even more[who?] stand behind steeping in hot water. Some methods call for citric acid or acetic acid (vinegar) to be used during extraction. The purpose of the addition of citric and/or acetic acid is to lower the ph level of the neutral water (ph7) down to a slightly acidic ph of 6.5 which is optimal for morphine extraction.

. Addition of nicotinic acid, otherwise known as Niacin and Vitamin B3, would give rise to 3-mononicotinylmorphine, related to morphine in a similar way, viz. 3,6 dinicotinylmorphine is a painkiller known as nicomorphine (Vilan) which is also three times stronger than morphine and gives rise to 6-MNM by means of hydrolysis.

i had been lookin at a nicotanimide=>pyridine synthesis links for a little while

at d mo i dont have a functioning lab(or computer!!)at home--i have yet to find an suitably downwind site

but every day i get closer....woohoo!!!

jon · « **Reply #52 on:** October 12, 2009, 10:10:00 AM »

man i can tell uou this afte much trial and error for chemcial processing use ph 4 water any higher and morphinegets killed regardless of temps because swij pulled high vacumand still saw a pile of worthless goop.
keep the ph 4 and you'l have no problems reducing your water extract.
i even tried it and it worked no morphine ruined this way.
it cost swij a lot of coin to teach you this.
antioxidationats like nahso3 are even better in combination with low ph in fact one can lower ph with nahso3 and no woriies about morhine degradtion.
believe it or don't but after you blow several hundred dollars you'll see i'm right.

Sedit · « **Reply #53 on:** October 14, 2009, 04:06:49 AM »

Quote

d mo

Care to clearify what this means? I would have to assume that it stands for at the moment but I could be wrong and herein lies the problem. For future reference can we please do away with 90% of the abreviations? Im sure I am no saint in this area but it would still look alot cleaner and more professional if everyone would take the extra time to produce well written and thought out post. You are still pretty new hypnos so I want you to know Im not comming down on you as you seem like a useful member but the cleaner these form of chemistry sites appear the more acceptance they will recieve though out the chemistry community. If we start to slack we will lose many potential members that will just look at us as another useless drug synthese website. Let us try to rise above the common notion of the current state of affairs for our brand of chemistry.

Thank you,
Vespiary Staff.

jon · « **Reply #54 on:** October 14, 2009, 04:34:16 AM »

nicotonic acid can be made into it's coreesponding anhydride by trating witha lower boiloing anhydride heting this to give the mixed anhydride.
and distiling off the resultant lower acid.
the reason this is so sgood is because of the lipohilicity of the aromatic ring
benzoic anydride works just as well and is off the shelf (not watched)

hypnos · « **Reply #55 on:** October 14, 2009, 10:16:04 PM »

no worries sedit,,,its just "d" slack aussie txter in me coming out in my typing every now and then

as you say,,,i 'am new' to online forums and i am still getting the hang of posting appropriatley....sorry about that

hypnos · « **Reply #56 on:** April 23, 2010, 05:29:08 AM »

now look what you've done

gotta laugh tho

'Bakers may be at occupational risk of poppy-seed addiction'
Abstract from: The Lancet Volume 350, Number 9079 [6] 716-7 September 1997
MA King & et al Poppy tea and baker’s first seizure

“Doctors treating a baker who had a seizure at work suspected
drug-abuse which the patient denied until his business partner told them
that the bakery's weekly order of poppy seeds had gone up from 3 kg to
25 kg. The baker then admitted to drinking up to 2 L of tea made from
about 4 kg of poppy seed every day, a practice he was introduced to
during his apprenticeship. Mark King and colleagues from Victoria,
Australia, report this case in a Research Letter this week, and remark on
the patient's extraordinary drug tolerance since his daily consumption was
the equivalent of 280 mg of morphine, On admission his blood morphine
concentration was nearly 3 mg/L-heroin addicts who die of an overdose
have mean concentrations of 0-6 mg/L. He was admitted to a
rehabilitation programme where the poppy tea was replaced with
slow-release oral morphine.”

jon · « **Reply #57 on:** April 27, 2010, 02:09:04 AM »

no bullshit the water extracts of australian poppy seed are white in other words you can see the latex coming off the seeds tasmanian seeds really have high alkaloid content.

Balkan Bonehead · « **Reply #58 on:** March 23, 2013, 01:14:03 AM »

Quote from: jon on September 23, 2009, 04:56:14 PM

90 c will kill the alkaloids

I have heard this before, but I assume it is just lore with no basis in fact that hot water will degrade morphine. It doesn't make much sense considering that opium is sometimes smoked and the morphine survives being vaporized.

Tsathoggua · « **Reply #59 on:** March 24, 2013, 12:19:01 AM »

AFAIK they are indeed sensitive, but before toady knew better, he just used to toss his pods by the handful into a pan, boil it up with a couple of Amanita muscaria caps (cured and dried to detoxify them of course), and drank the resulting abominably stinking brew with a load of sugar and a held nose.

Gods...that stench...there is nothing quite like it. Turns his stomach just thinking about it, most abominable, revolting stench he can bring to mind. Makes chlorine bleach, chloroform, putrescine and mercaptans smell like bloody candy by comparison

He can't wait to give this a shot (pun intended). Needs to get all that poppy seed planted on some nice, remote waste ground. NH3SO4, plus some added potassium phosphate? any good as a fert, jon?

Back on track...

6-MAM and heroin have interesting pharmacological properties. There has been some relatively recent search for the receptor(s) involved, as it appears that 6-MAM in particular, and H (unsure if H has direct affinity for this target or if its simply acting as a prodrug for 6-MAM), the crosstolerance to morphine is incomplete (which might well explain the relatively limited popularity of opioid maintenance/detox facilities which use other opioids, compared to those which provide addicts with limited quantities of pure pharmaceutical diamorphine in injectable format)

Toady has been looking into this particular target of late in the context of his preliminary investigations into iodobenzoylnaltrexamide, IBnTXA acts as a splice-variant specific agonist at a post-translationally modified splice variant of hMOR1, derived from exon-1. Its a truncated 6-transmembrane GCPR with a hacked-down C terminus IIRC (Could bee wrong, and it bee the N-terminus but don't think so)

This seems to prevent the shift between Gi/Go coupling to (GalphaS?) in the case of allodynic pain (neuropathy, which as toady can testify, courtesy of some unsuccessful surgical intervention that left him with probably permanent nerve damage), and Gbetagamma, as the last few 500-kilobase or so of hMOR1 appears to act as a regulatory site, conferring different affinity/efficacy for opioid peptides vs alkaloid ligands (sans, IIRC, actually changing selectivity for the ligands in question) and IIRC modulating coupling of the different G-proteins with their effectors on the intracellular side of things), which, as tolerance progresses, there is a shift in G-protein coupling thus converting a lot of the previous inhibitory signalling, GABAaR suppression of inhibition etc. to favouring the activation of a population of excitatory Mu-ORs (possible that this might explain a lack of euphoria or reinforcement seen with iodobenzoylnaltrexamide? that is, sensitization of MORs and inducement of DA release in the nucleus accumbens that contributes in regular opioids to conditioned place preference, reinforcement, addiction, and that euphoria we bees all know and love from our poppy flower honey?

In addi(c

)tion, Toadface has a quick question. He isn't sure from context during his reading weather the GABAergic suppression of inhibition referred to, is meant to mean, in this specific context, suppressing the inhibition of GABAaRs themselves, leading to more GABAergic activity or suppressing the inhibition of; as is usually meant by 'suppression of inhibition'. GABAaR-mediated inhibitory signalling, leading to DA release* and greater release of other neurotransmitters besides. Could anyone clarify this for him perchance?

*this happens with cannabinoid CB1 agonists, despite the atypical retrograde signalling mechanism of CB1 agonism, activating presynaptic CB1Rs via endogenous cannabinoid ligands of various kinds released postsynaptically which then amongst other actions on other receptors and voltage-gated ion channels of this that and t'other flavor, this suppression of suppression turning up the volume controls on DA release, etc. etc.

In exon-1 -/- mice, they lost responsivity to morphine, and DAMGO (potent MOR1/MOR2 opioid agonist peptide) but retained it to M6G

Proc Natl Acad Sci U S A. 2011 Dec 6;108(49):19778-83. doi: 10.1073/pnas.1115231108.
Truncated G protein-coupled mu opioid receptor MOR-1 splice variants are targets for highly potent opioid analgesics lacking side effects. iodobenzoylnaltrexamide itself appears to possibly not possess a huge amount of euphoria, if its euphorigenic

h ttp://ww w. ncbi.nlm.nih.gov/pubmed/22106286?dopt=Abstract

(free full text)

h ttp://ww w.ncbi.nlm.nih.gov/pmc/articles/PMC3477067/ (full, free)

J Mol Signal. 2012; 7: 13.
doi: 10.1186/1750-2187-7-13
PMCID: PMC3477067
The roles played by highly truncated splice variants of G protein-coupled receptors

PLoS One. 2008 Feb 6;3(2):e1554. doi: 10.1371/journal.pone.0001554.
High-affinity naloxone binding to filamin a prevents mu opioid receptor-Gs coupling underlying opioid tolerance and dependence.
PMID: 18253501

ht tp://w ww.ncbi.nlm.nih.gov/pubmed/18253501

Proc Natl Acad Sci U S A. 2011 Dec 6;108(49):19778-83. doi: 10.1073/pnas.1115231108. Epub 2011 Nov 21.
Truncated G protein-coupled mu opioid receptor MOR-1 splice variants are targets for highly potent opioid analgesics lacking side effects.

PMID:
22106286 (been manually fixing it, but anybee know why pubmed likes to put the PMID and the actual PMID number on different lines when copypasta'ed even when they are in line on their home webpage? its irritating.

h ttp:// www.ncbi.nlm.nih.gov/pmc/articles/PMC2894766/
Mol Pain. 2010; 6: 33.
Published online 2010 June 2. doi: 10.1186/1744-8069-6-33
PMCID: PMC2894766
A novel alternatively spliced isoform of the mu-opioid receptor: functional antagonism

h ttp://ww w.ncbi.nlm.nih.gov/pmc/articles/PMC3186080/

Pharmacol Rev. 2011 December; 63(4): 1001–1019.
doi: 10.1124/pr.111.004598
PMCID: PMC3186080
Functional Selectivity at the ?-Opioid Receptor: Implications for Understanding Opioid Analgesia and Tolerance

http://www.ncbi.nlm.nih.gov/pubmed/22106286?dopt=Abstract (the ones here before the Toad's requests here are all selected for separation in the thread because he thought they will bee of interest either to those working on novel opioids, specifically relevant to mono-acylated 6-position morphinans), or for those wishing to learn some real juicy, bleeding-edge opioid SAR

ht tp://w ww.ncbi.nlm.nih.gov/pubmed/20726836 (something on filamin-A high affinity binding by antagonists at nano/picomolar plasma concentrations and tolerance, got to bee quick here, little PC time left)

Br J Pharmacol. 2010 November; 161(5): 986–1001.
doi: 10.1111/j.1476-5381.2010.00824.x
PMCID: PMC2998681
Spinal or systemic TY005, a peptidic opioid agonist/neurokinin 1 antagonist, attenuates pain with reduced tolerance
ht tp://w ww.ncbi.nlm.nih.gov/pmc/articles/PMC2998681/

Pain Res Treat. 2012; 2012: 145965.
Published online 2012 March 21. doi: 10.1155/2012/145965
PMCID: PMC3324919
Effects of Combined Opioids on Pain and Mood in Mammals
h ttp://ww w.ncbi.nlm.nih.gov/pmc/articles/PMC3324919/

PLoS ONE. 2009; 4(1): e4282.
Published online 2009 January 27. doi: 10.1371/journal.pone.0004282
PMCID: PMC2628740
Naloxone's Pentapeptide Binding Site on Filamin A Blocks Mu Opioid Receptor–Gs Coupling and CREB Activation of Acute Morphine

h ttp://ww w.ncbi.nlm.nih.gov/pmc/articles/PMC2628740/

Toady would bee grateful if these references could perhaps bee supplied: (he puts them in this thread due to context and for accesibility to other bees looking at this and monoacyl morphinan esters, rather than generically in the reference req. thread)

J Pain. 2008 Aug;9(

:700-13. doi: 10.1016/j.jpain.2008.03.005. Epub 2008 May 12.
Oxycodone plus ultra-low-dose naltrexone attenuates neuropathic pain and associated mu-opioid receptor-Gs coupling

Neurochem Res. 1996 Nov;21(11):1347-51.
PMID: 8947924
Modulatory effects of Gs-coupled excitatory opioid receptor functions on opioid analgesia, tolerance, and dependence.
h ttp://ww w.ncbi.nlm.nih.gov/pubmed/8947924

Pain. 2000 Feb;84(2-3):121-31.
Antagonists of excitatory opioid receptor functions enhance morphine's analgesic potency and attenuate opioid tolerance/dependence liability.
PMID: 10666516

ht tp://w ww.ncbi.nlm.nih.gov/pubmed/10666516

Neuroscience. 2005;135(1):247-61.
Ultra-low-dose naloxone suppresses opioid tolerance, dependence and associated changes in mu opioid receptor-G protein coupling and Gbetagamma signaling.
PMID: 16084657

h ttp://w ww.ncbi.nlm.nih.gov/pubmed/16084657

Brain Res. 2008 Sep 22;1231:16-24. doi: 10.1016/j.brainres.2008.07.015. Epub 2008 Jul 12.

Low doses of cyclic AMP-phosphodiesterase inhibitors rapidly evoke opioid receptor-mediated thermal hyperalgesia in naïve mice which is converted to prominent analgesia by cotreatment with ultra-low-dose naltrexone.

ht tp://ww w.ncbi.nlm.nih.gov/pubmed/18656459
PMID: 18656459

Neurosignals. 2005;14(4):194-205.
Is paradoxical pain induced by sustained opioid exposure an underlying mechanism of opioid antinociceptive tolerance?
ht tp://w ww.ncbi.nlm.nih.gov/pmc/articles/PMC2628740/
PMID:16215302

Psychopharmacology (Berl). 2005 Jun;180(1):1-11. Epub 2005 Apr 14.
Effector antagonism by the regulators of G protein signalling (RGS) proteins causes desensitization of mu-opioid receptors in the CNS
PMID:
15830230
htt p://ww w.ncbi.nlm.nih.gov/pubmed/15830230

Neuropharmacology. 2003 Jul;45(1):82-95.
The GBeta5 subunit that associates with the R7 subfamily of RGS proteins regulates mu-opioid effects.
h ttp://ww w.ncbi.nlm.nih.gov/pubmed/12814661

Thats your lot for now guys, hope some of the provided full texts are of use/interest.
So if the requested papers could bee found for Toady, he would bee grateful.,

Author Topic: 6Momo Propionic Ester Morpines from Pods By Jon @ WD's (Read 837 times)

jon

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