Ketamine salts solubility

[Generation *DMT*]

Who won the world series this year 2023?

 

[someguyontheinternet]

My limited knowledge of diprenorphine is that it's restricted use is due to it's side-effects, specifically hallucinations and dysphoria.

Is it a kappa agonist?

 

[AlsoTapered]

https://www.researchgate.net/publication/364198495_Chemoenzymatic_Synthesis_of_Optically_Active_Ethereal_Analog_of_iso-Moramide-A_Novel_Potentially_Powerful_Analgesic

An interesting modification of dextromoramide. It's a shame that the most facile synthesis still involves an SN2 reaction which results in a mixture of positional isomer. The PLUS side is that both the (R) and (S) enthiomers are virtually equal in activity so the raecemate is very likely a reasonable target.

Dextromoramide is generally accepted as being x3 morphine in potency and the above apparently has slightly higher affinity although interestingly, since it's an in-silico design, the researchers calculate in the energy lost due to binding rather than the more traditional Ki. I would be interested to know if the Ki can be calculated by energy value and vice versa.

 

[Rectify]

So, like um, what do we get for $20.00?

 

[Rectify]

The Texas Rangers won the World Series in 2023.

 

[Rectify]

 

[Rectify]

PURPLE_GRAPE_FLAVOR
2-aminobenzoic acid

THE_GRAPE_APE
1-(2-aminophenyl)-2-aminopropane

If It Smells Good, Then Do It.

 

[AlsoTapered]

^ not a new compound at all. However the potency in vivo is nowhere near as high as is suggested by in vitro. ED50 32ug/kg in guinea pigs. In humans it is not that potent (fentanyl level potency)
Patent is 1972 to Sanko company, Chem Pharm Bull (Japan) 2050-2057 (1970)

I don't understannd this obsession with in vitro potency over everything, are you playing some kind of smackhead top trumps?

Safer opioids would be a good thing and super potent /= safer
Dezocine based compounds with reduced respiratory depression and or ceiling effect would be a better approach if harm reduction really was your priority

I never claimed it was a new compound and actually included hotlinks to the references.

I am simply attempting to provide anyone interested with ALL the hotlinks I have access to so that they can study the various classes of opioid.

Sorry for the late response, I missed your post.

BTW elsewhere I have repeatedly stated that hugely potent opioids are extremely dangerous. Many people still rely on eyeballing doses so anything more than about ten times morphine in potency carries the extreme risk of overdose. When you reach compounds like carfentanil that are now on the street, it's reaching the limits of dilution when in a solid format. There are ways but it's not much of a surprise to realize that such compounds, compounds which find legitimate use in veterinary are produced as solutions.

It's also worth noting that potency varies between individuals and so while the press is keen to list carfentanil as x10000 morphine, the variability can be quite massive. It's a known issue within the field of anesthesia.

 

[Rectify]

A_REAL_ASS_KICKER
2-(4-methoxyphenyl)-1-aminocyclohexane

FASTER_PUSSYCAT
N-allyl-2-phenyl-1-aminocyclohexane

HARVARD
N,N-di-allyl-lysergamide

BILLY
2-(4-methylphenyl)-1-methylaminocyclohexane

YANA
1-(3,4-methylenedioxyphenyl)-4-aminocyclohexane

 

[AlsoTapered]

https://www.erowid.org/archive/rhodium/pdf/cocaineanalogs.pdf

Above is a link to a fantastic paper which not only comprehensively documents the QSAR of every cocaine homologue documented, but it also correctly identifies the fact that methylphenidate and mazindol which chemically distinct, produce psychostimulation via the same pathways.

The other major class of psychostimulants are the amphetamines but people sometimes don't recognize that desoxypipradrol and homologues, nomifensine and homologues and various other stimulants such as fencamfamine (and homologues), phenmetrazine (and homologues) and even the 1,2-diaryl-2-amino-ethan-1-one derivatives all contain within them the alpha methyl phenylethylamine (amphetamine) scaffold within them*.

*In a few examples the benzene ring is replaced by other aromatic rings but such a modification appears to universally reduce activity.

 

[AlsoTapered]

Is it a kappa agonist?

[6-O-methyl-11C]Diprenorphine - Molecular Imaging and Contrast Agent Database (MICAD) - NCBI Bookshelf

A good question. The thing is, diprenorphine (M-5050) was discovered in 1965 as part of Dr. Kenneth W. Bentley's extensive QSAR study of the ethenomorphinans which he and his team began studying in 1962 and which are generally referred to as 'Bentley compounds'.

What I've just noted is that it was a Belgian researcher who decided that applying the Diels-Alder reaction to as many natural compounds as they could think of. Obviously nature is a great source of dienes and so thebaine and oripavine were interesting targets as a decade before US researchers had noted that modification of the C-ring in phenanthracene opioids could significantly increase activity.

What it's important to know is that what Bentley was originally seeking was a cheaper alternative to codeine specifically for use in compound analgesics such as co-codamol. After all, if one could replace 8.4mg of codeine phosphate with, say, 1μg of etorphine (M-99), at scale it would prove to be a worthwhile saving. Obviously the logic was that being compound analgesics, the paracetamol would stop someone from simply eating a whole box full of tablets...

But of course he was disappointed that very few of the compounds discovered were active orally. In fact it was 7-PET and not etorphine that ended up being the candidate but by that point it was recognized that people had worked out how to extract the codeine from co-codamol and the same technique would have allowed 7-PET to be extracted and that would not be a good thing.

I believe a lab accident in 1965 in which almost the entire team were accidentally poisoned by one of the more potent homologues that meant that someone in the team decided that finding an effective antidote was an important task and diprenorphine had displayed the most potent antagonist activity of the series.

I feel it's a terrible loss that their is almost no record of the events surrounding the discovery and development of these compounds. Snippets have been written including how buprenorphine was tested - members of the team were used as subjects which is when they discovered that nausea and vomiting were a particular issue.

It's worth noting that etorphine is always supplied with an equal amount of diprenorphine to treat accidental poisonings. In nations where carfentanil is used to sedate large animals... diprenorphine is also supplied as a treatment for such accidents.

 

[Rectify]

U4EUH
5-phenyl-2-amino-4,5-dihydro-3-aza-4-methylfuran

MUFFIN
5-phenyl-2-amino-4,5-dihydro-3-aza-4-methylthiophene

RALPH
5-phenyl-2-amino-3-aza-4-methylcyclopent-2-ene

MOSS
5-(4-methoxyphenyl)-2-amino-3-aza-4-methylcyclopent-2-ene

STERLING
5-(4-methylphenyl)-2-amino-3-aza-4-methylcyclopent-2-ene

BUTTERS
5-(3,4-methylenedioxyphenyl)-2-amino-3-aza-4-methylcyclopent-2-ene

CARMEN
4,5-dihydro-5-(3,4-methylenedioxyphenyl)-2-amino-3-aza-4-methylthiophene

PANCHO
4,5-dihydro-5-(4-methoxyphenyl)-2-amino-3-aza-4-methylthiophene

LEFTY
4,5-dihydro-5-(4-methylthiophenyl)-2-amino-3-aza-4-methylthiophene

DEXTER
4,5-dihydro-5-(4-methylphenyl)-2-amino-3-aza-4-methylthiophene

TERRA_INCOGNITA
4,5-dihydro-5-(3,4,5-trimethylphenyl)-2-amino-3-aza-4-methylthiophene

BERSERKEN
4,5-dihydro-5-(2,5-dimethoxy-4-bromophenyl)-2-amino-3-aza-4-methylthiophene

BOYSENBERRY
4,5-dihydro-5-(2,5-dimethoxy-4-methylphenyl)-2-amino-3-aza-4-methylfuran

For All I Know, This Series Is As Toxic As Anything.

 

[Rectify]

JAIME_SETH_EVANS_TROXLER
1-phenyl-1-(methylthio)-2-methylaminopropane

He's A Smooth Operator!

JIM_AARON_BAAL_EMORY
1-(3,4-methylenedioxyphenyl)-1-(methylthio)-2-methylaminopropane

Think Applebee's.

CH2=CH-CH2-S-CH2CH=CH2

ALLICIN_WONDERLAND
diallylsulfide

Antimicrobial found in Garlic.
Wards off vampiristas.
May be an anesthetic gas.

 

[Rectify]

ALFRED_NOBEL
N-(2,2-dichloroacetyl)-1-(2,5-dimethoxy-4-nitrophenyl)-1-hydroxy-3-oxo-2-aminopropane

Oral antibiotic (ring activated chloramphenicol analog).

Plan B:

ALEXANDER_FLEMING
N-(2,2-dichloroacetyl)-1-(2,5-dimethoxy-4-nitrophenyl)-1-amino-3-oxo-2-aminopropane

KING_ANDRIEUX_THE_X
1-(3,4-methylenedioxyphenyl)-2-methylamino-1,3-dioxopropane

I was looking for a robust antibiotic with recreational and anti-Parkinson characteristics. Don't know what I found.

 

[Rectify]

SIMPLY_ANDREW
1-phenyl-2-aminopropane

He Who Understands AMP Understands All Things.

 

[Rectify]

NEW_CAR_SMELL_AMPHETAMINE
1-(3,4-dimethylphenyl)-2-methylaminopropane

EMILY_STORY_JOHNSON_PENNINGTON
1-(2-methoxy-3,4-dimethylphenyl)-2-aminopropane

 

[Rectify]

JASON_LINKIN_PARK_JONES
1-(2-methoxy-4,5-dimethylphenyl)-2-aminopropane

THE_JASON_MNEMONIC: July August September October November

 

[Rectify]

 

[AlsoTapered]

Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil

Tetrahedron Letters 2010-jun vol. 51 iss. 22, 2010

Author(s): Sandra Malaquin; Mouhamad Jida; Jean-Claude Gesquiere; Rebecca Deprez-Poulain; Benoit Deprez; Guillaume Laconde

Library Genesis

libgen.li

Anyone wondering why carfentanil is now becoming common on the streets of North America need look no further. It's worth noting that the scope of the synthesis allows for the pendent benzene to be swapped for other aromatics AND the inclusion of a beta-hydroxy moiety which renders the products 6-8x more potent.

 

[Rectify]

JAMES
2-propylamino-1-phenyl-1-methoxypropane

One Time, Beavis & Butthead Said, "We're Sorry, James, You Suck."

I Would Try It, Though.