Ketamine salts solubility

[Skorpio]

would be nice if anyone has access and can get them...

Do you know how to upload pdfs?

Alternately you can use scihub (the scihub.se link just worked for me, but I usually Google it so I can find current links). I had to use it to get the third paper.

 

[izo]

Do you know how to upload pdfs?

if i remember correctly upload for files is disabled now on bluelight.

 

[Skorpio]

if i remember correctly upload for files is disabled now on bluelight.

The go the scihub route.

 

[izo]

how great is that, didnt knew this site before...

 

[Skorpio]

how great is that, didnt knew this site before...

It's a godsend. Sometimes it is easier to use scihub than going through the labrynthine institutional login pages journals use (of course its not standardized).

It was started by a very cool Kazakh programmer, Alexandra Elbakyan, in 2011 and uses institutional login credentials that fell off the back of a truck to get everybody access to the papers. Once a paper is accessed, a copy of it is stored on the scihub server so that it is permenantly available. Journals obviously hate her with quite a passion, and have tried to sue her multiple times for millions (4.8 and 15 million).

Also, I have real issues with how academic publishing works.

Researchers do the experiments and write the papers, then pay to submit to a journal. Then somebody in the field reviews the paper for free, and if you pass reviews/are able to make enough changes the journal edits your manuscript and publishes it.

This paper will probably cost 20-30 dollars if you want to buy it, and that money goes to the journal. There are no royalties in scientific publishing, the researcher just gets two things from the journal: credibility and circulation.

Now these things are honestly pretty valuable, as publishing in a good journal will make it more likely for you to get grant money, and getting into a really big journal (Science, Nature, and Cell are the ones that most people I know read religiously, in addition to more specialized lower impact journals such as the Journal of Biological Chemistry, or the American Chemical Society journal or my favorite,, PNAS (their slogan is "please don't make fun of our name")) will pretty much ensure that everybody who keeps up to date with the literature will see it.

That being said, I feel like the credibility offered by established high impact journals is intangible, as opposed to editing and distributing the articles which takes overhead. Some part of me wishes researchers got royalties after the cost of distribution and some amount of profit were generated.

Rant over.

 

[izo]

Scihub cannot get this article but it look interesting:

Discriminative Stimulus Effects of Substituted Tryptamines in Rats​

ACS Pharmacol Transl Sci. 2020 Dec 29;4(2):467-471.
doi: 10.1021/acsptsci.0c00173. eCollection 2021 Apr 9.

Discriminative Stimulus Effects of Substituted Tryptamines in Rats - PubMed

Novel synthetic compounds have been available for decades as quasi-legal alternatives to controlled substances. The hallucinogen-like effects of eight novel substituted tryptamines were evaluated to determine their potential abuse liability. Male Sprague-Dawley rats were trained to discriminate...

pubmed.ncbi.nlm.nih.gov

Abstract​

Novel synthetic compounds have been available for decades as quasi-legal alternatives to controlled substances. The hallucinogen-like effects of eight novel substituted tryptamines were evaluated to determine their potential abuse liability. Male Sprague-Dawley rats were trained to discriminate 2,5-dimethoxy-4-methylamphetamine (DOM, 0.5 mg/kg, i.p., 30 min) from saline. 4-Acetoxy-N,N-diethyltryptamine (4-AcO-DET), 4-hydroxy-N-methyl-N-ethyltryptamine (4-OH-MET), 4-hydroxy-N,N-diethyltryptamine (4-OH-DET), 4-acetoxy-N-methyl-N-isopropyltryptamine (4-AcO-MiPT), 4-acetoxy-N,N-dimethyltryptamine (4-AcO-DMT), 4-hydroxy-N,N-dimethyltryptamine (4-OH-DMT, psilocin), 5-methoxy-N-methyl-N-isopropyltryptamine (5-MeO-MiPT), 4-acetoxy-N,N-diisopropyltryptamine (4-AcO-DiPT), and 4-hydroxy-N,N-diisopropyltryptamine (4-OH-DiPT) were tested for their ability to substitute for the discriminative stimulus effects of DOM. All test compounds fully substituted for DOM with potencies less than or equal to that of DOM. 4-OH-MET, 4-OH-DET, 4-OH-DMT, and 4-AcO-DMT decreased response rate at doses that fully substituted. Because the test compounds produced DOM-like discriminative stimulus effects, they may have similar abuse liability as DOM. 4-Acetoxy substituted compounds were less potent than 4-hydroxy substituted compounds, and the N,N-diisopropyl compounds were less potent than the dimethyl, diethyl, N-methyl-N-ethyl, and N-methyl-N-isopropyl compounds.

 

[Gaffy]

PROTAGONE

 

[Gaffy]

SWINGER FINGER
If you know what I meany mean

PRICY KWEAK

 

[Rectify]

THE WHITE NORSE HORSE
4-(phenylcarbonyloxy)-piperidine

MEGATRON
2-ethylamino-2-(3-methoxyphenyl)-bicyclo[2.2.2]octane

THE FLYING MONKEY
1-(3-pyridinyl)-N-methyl-2-azabicyclo[2.2.1]heptane

CALVIN
N-methyl-5-phenyl-3-azabicyclo[2.2.1]heptane

THE REDEEMER
N-ethyl-5-(3,4-methylenedioxyphenyloxy)-3-azabicyclo[2.2.1]heptane

IDIOT SAVANT
N-methyl-5-phenyloxy-3-azabicyclo[2.2.1]heptane

JIM / GEM
1-(2-azabicyclo[2.2.2]octane-1-yl)-1-carbomethoxy-1-phenylmethane

CAREY
1-(2-azabicyclo[2.2.2]octane-3-yl)-1-carbomethoxy-1-phenylmethane

MORGASMIC
1-(2-azabicyclo[2.2.2]octane-3-yl)-1-carbomethoxy-1-(3,4-methylenedioxyphenyl)methane

 

[Skorpio]

​

​

Pharmacological and behavioral divergence of ketamine enantiomers: implications for abuse liability​

Abstract​

Ketamine, a racemic mixture of (S)-ketamine and (R)-ketamine enantiomers, has been used as an anesthetic, analgesic and more recently, as an antidepressant. However, ketamine has known abuse liability (the tendency of a drug to be used in non-medical situations due to its psychoactive effects), which raises concerns for its therapeutic use. (S)-ketamine was recently approved by the United States’ FDA for treatment-resistant depression. Recent studies showed that (R)-ketamine has greater efficacy than (S)-ketamine in preclinical models of depression, but its clinical antidepressant efficacy has not been established. The behavioral effects of racemic ketamine have been studied extensively in preclinical models predictive of abuse liability in humans (self-administration and conditioned place preference [CPP]). In contrast, the behavioral effects of each enantiomer in these models are unknown. We show here that in the intravenous drug self-administration model, the gold standard procedure to assess potential abuse liability of drugs in humans, rats self-administered (S)-ketamine but not (R)-ketamine. Subanesthetic, antidepressant-like doses of (S)-ketamine, but not of (R)-ketamine, induced locomotor activity (in an opioid receptor-dependent manner), induced psychomotor sensitization, induced CPP in mice, and selectively increased metabolic activity and dopamine tone in medial prefrontal cortex (mPFC) of rats. Pharmacological screening across thousands of human proteins and at biological targets known to interact with ketamine yielded divergent binding and functional enantiomer profiles, including selective mu and kappa opioid receptor activation by (S)-ketamine in mPFC. Our results demonstrate divergence in the pharmacological, functional, and behavioral effects of ketamine enantiomers, and suggest that racemic ketamine’s abuse liability in humans is primarily due to the pharmacological effects of its (S)-enantiomer.

Pharmacological and behavioral divergence of ketamine enantiomers: implications for abuse liability - Molecular Psychiatry

Ketamine, a racemic mixture of (S)-ketamine and (R)-ketamine enantiomers, has been used as an anesthetic, analgesic and more recently, as an antidepressant. However, ketamine has known abuse liability (the tendency of a drug to be used in non-medical situations due to its psychoactive effects)...

www.nature.com

This paper demonstrates a significant role in the mu opioid receptor in s ketamines pharmacology. Goes into a lot more detail of the different isomers respective assays. The behavioral effects of s ketamine are striking in how much they are reversed by naloxone for example. (also r ketamine exhibiting different shapes of curves on the tests, which really demonstrates that it has fundamentally different pharmacology rather than acting as a weaker s ket).

 

[izo]

to whoever who is interested, i found it interesting:

1970 - Central and peripheral effects of anticholinergic compounds​

Abstract: The pharmacological effects of aryl and cycloalkylaryl glycolates of piperidin, tropine and quinuclidin have been studied in relation to atropine and scopolamine. Peripheral effects (heart rate, salivation, pupil size) have been studied in dogs in relation to their behavioural effects under standardized conditions. The anticholinergic activity was further investigated on the mouse pupil and on the blood-pressure response to acetylcholine in cats anaesthetized with pentobarbital. In dogs all the glycolates elicited behavioural effects, especially on locomotion, similar to those seen following atropine and scopolamine. Even high doses of methyl atropine produced effects indistinguishable from those produced by atropine and scopolamine. The most active compounds affected behaviour at a dose of 10 pg per kilogram body weight given subcutaneously. All compounds elicited anticholinergic activity i.e. tachycardia, mydriasis, inhibition of salivation and block of AcCh response. The most potent compounds on behaviour were quinuclidinylesters of phenyl andlor thienyl glycolic acid which also had the strongest and most prolonged classical anticholinergic effects. The results indicate that behavioural effects are related to anticholinergic activity but that other factors such as lipid-solubility and metabolism interfere with the central activity.

Central and peripheral effects of anticholinergic compounds - PubMed

Central and peripheral effects of anticholinergic compounds

pubmed.ncbi.nlm.nih.gov

 

[Rectify]

CHRISTIAN DIOR
1-(piperidin-2-yl)-1-carbomethoxy-1-(2-methoxy-4,5-methylenedioxyphenyl)methane

I *really* like carbomethoxy functional groups.

In other news, I think I fried my brain a year or two ago with OREILLYIUM (4-oxonium amphetamine.hcl), which doesn't even really get you high. Now I have to take copious amounts of stimulants just to feel normal.

TOXICITINE
1-methyl-2-(1-methylpyridinium-3-yl)pyrrolidine

Investgational New Agricultural Pesticide

I Wouldn't Touch That One With A 10 Foot Pole!

WHOLISTIC ADDICTIVE NOOTROPE WAN NAW
1-methyl-2-carbomethoxy-2-(3-pyridinyl)pyrrolidine

Because Addictive Drugs Are FUN And Worth Money![/]

Walk A Mile For A Camel?

BLOOMIN YUM YON
1,3,7-tricarbomethoxyxanthine

CADDY SHACK KIEL O'NEIL
1,3,7-triacetylxanthine

The ICE Man Comet(h)

 

[izo]

1972 - Handbook of Psychopharmacology, Vol 11 Chapter 1 Amphetamines Structure-Activity Relationships

Amphetamines: Structure-Activity Relationships

Amphetamine is a unique drug with respect to the simplicity of its structure and the multiplicity of its biological effects. Pharmacologically, amphetamine possesses central stimulant, anorexic, vasoconstrictor, and hyperthermic properties. Biochemically, amphetamine...

link.springer.com

1972 - Handbook of Psychopharmacology, Vol 11 Chapter 1 Amphetamines Structure-Activity Relationships.djvu

drive.google.com

 

[Gaffy]

FLUFFY GOOFY DOOF

 

[Gaffy]

HOOKLADY BEEFY DOOF

 

[Gaffy]

Investigational Antipsychotic
CAPTIVANYL

 

[Rectify]

H2N-NH-CH2CH3

Designer Jet Fuel
ethylhydrazine

THE BOOK OF AMOS (SOMA)
1,1-bis(3,4,5-trimethoxyphenyl)-2-aminoethane

 

[Rectify]

PIP
6-(3-(1-carbomethoxy-1-phenylmethyl)-2-azacyclohexyl)-3-propylthio-2-carbomethoxy-7-oxo-azabicyclo[3.2.0]hept-2-ene

Investigational Stimulatory Antibiotic

NORM ANDY
1-(2,3-dimethylphenyl)-2-aminopropane

Psychiatric Adjuvant

 

[Rectify]

HANDSOME DEVIL
pseudo-NBzOMe-MPH
1-aza-6-(2-methoxyphenyl)-2-(1-carbomethoxy-1-phenylmethyl)cyclohexane

DEXTER AMPACIDE
(2S,6S)-6-(1-aza-2-methyl-3-phenylpropyl)-3-propylthio-2-carbomethoxy-7-oxo-(azabicyclo[3.2.0]hept-2-ene)

Investigational Stimulatory Antibiotic

(excitotoxicity encourages lethalic properties)

PROFESSOR X

 

[Gaffy]

Lots of new ones incoming, active at a tenth of a millligram. Watch out with those.

FRIKKADY

NOMYDOL