Ketamine salts solubility

[Pomzazed]

I can look at famous ppl and inuit their spirit molecu

I am not famous, but please look if you can see my molecules
(Note; i am not a fan of phenehtylamines and tryptamines, im more of a ‘binoids type)

 

[Limpet_Chicken]

My bad Sekio, should have spotted that.

To bring some intelligent debate into this otherwise shit-filled mire; have psi-DOC or psi-DOI/psi-DOB been tested?

 

[sekio]

Fully half of the drugs described in this Book II are of the classical 2,4,5-trisubstitution pattern, and it is becoming evident that every one of them will have a 2,4,6-trisubstituted counterpart that bids fair to be an active psychedelic. Diligence could thus easily double the number of known psychedelics.

Nichols looked at the psi-3CD-FLY/DFLY compounds [ref] and sez that PSI-DOM is about 1/3 the binding affinity than DOM at 5ht2a.

 

[S.J.B.]

A daily single dose of a novel modafinil analogue CE-123 improves memory acquisition and memory retrieval
Corresponding authors: Gert Lubeck, Jana Aradska (Department of Neuroproteomics, Paracelsus Medical University, Salzburg, Austria)
Behavioural Brain Research 2018, Volume 343, Pages 83-94
Published online February 1st, 2018
https://doi.org/10.1016/j.bbr.2018.01.032

Abstract:

Dopamine reuptake inhibitors have been shown to improve cognitive parameters in various tasks and animal models. We recently reported a series of modafinil analogues, of which the most promising, 5-((benzhydrylsulfinyl)methyl) thiazole (CE-123), was selected for further development. The present study aims to characterize pharmacological properties of CE-123 and to investigate the potential to enhance memory performance in a rat model. In vitro transporter assays were performed in cells expressing human transporters. CE-123 blocked uptake of [3H] dopamine (IC50 = 4.606 uM) while effects on serotonin (SERT) and the norepinephrine transporter (NET) were negligible. Blood-brain barrier and pharmacokinetic studies showed that the compound reached the brain and lower elimination than R-modafinil. The Pro-cognitive effect was evaluated in a spatial hole-board task in male Sprague-Dawley rats and CE-123 enhances memory acquisition and memory retrieval, represented by significantly increased reference memory indices and shortened latency. Since DAT blockers can be considered as indirect dopamine receptor agonists, western blotting was used to quantify protein levels of dopamine receptors D1R, D2R and D5R and DAT in the synaptosomal fraction of hippocampal subregions CA1, CA3 and dentate gyrus (DG). CE-123 administration in rats increased total DAT levels and D1R protein levels were significantly increased in CA1 and CA3 in treated/trained groups. The increase of D5R was observed in DG only. Dopamine receptors, particularly D1R, seem to play a role in mediating CE-123-induced memory enhancement. Dopamine reuptake inhibition by CE-123 may represent a novel and improved stimulant therapeutic for impairments of cognitive functions.

 

[S.J.B.]

Synthesis and Pharmacological Evaluation of Novel C‑8 Substituted Tetrahydroquinolines as Balanced-Affinity Mu/Delta Opioid Ligands for the Treatment of Pain
Corresponding author: Henry I. Mosberg (Department of Medicinal Chemistry, College of Pharmacy, University of Michigan, Michigan, United States)
ACS Chemical Neuroscience 2018, Volume 9, Issue 7, Pages 1840-1848
Published online April 20th, 2018
https://doi.org/10.1021/acschemneuro.8b00139

Abstract:

The use of opioids for the treatment of pain, while largely effective, is limited by detrimental side effects including analgesic tolerance, physical dependence, and euphoria, which may lead to opioid abuse. Studies have shown that compounds with a mu-opioid receptor (MOR) agonist/delta-opioid receptor (DOR) antagonist profile reduce or eliminate some of these side effects including the development of tolerance and dependence. Herein we report the synthesis and pharmacological evaluation of a series of tetrahydroquinoline-based peptidomimetics with substitutions at the C-8 position. Relative to our lead peptidomimetic with no C-8 substitution, this series affords an increase in DOR affinity and provides greater balance in MOR and DOR binding affinities. Moreover, compounds with carbonyl moieties at C-8 display the desired MOR agonist/DOR antagonist profile whereas alkyl substitutions elicit modest DOR agonism. Several compounds in this series produce a robust antinociceptive effect in vivo and show antinociceptive activity for greater than 2 h after intraperitoneal administration in mice.

Table 2. Effects of Alkyl and Halogen Substitutions on Affinity, Potency, and Efficacy

NSFW:

Table 3. Effects of Aryl, Carbonyl, and Amino Substitutions on Affinity, Potency, and Efficacy

NSFW:

Most of the compounds were tested for antinociceptive activity in vivo via the mouse warm water tail withdrawal test (10 mg/kg, intraperitoneal injection). Compounds 7b, c, e, and n were found to be fully efficacious, 7f was partially active, and the others has no activity.

---

It is worth noting that there is an FDA-approved drug for irritable bowel syndrome, eluxadoline, which combines MOR agonism with DOR antagonism:

Has anyone had the chance to encounter this compound? If so, how does it compare to other opioids?

 

[Dresden]

Pomzazed,

Ok, but 1st, let me ask, do you like to drink alcohol or not really? I've got 2 in mind, but answering that question will settle the decision for me!

I ran into

LOGAN MICHAEL REESE JUSTIN TIMBERLAKE

this AM @ Wal-Mart. He's a great guy!

AMP

POMZAZED

This one's a *bit* of a gamble, but hey, no guts, no glory, right?!

 

[Pomzazed]

@Dresden, no i dont like EtOH so much, same to other “aliphatic” alcohols.

The latter molecule looks yummy tho! Friedel crafts the cyclohexenone with that phenol with TFA looks nice...

 

[Limpet_Chicken]

What about say, tertiary pentyl alcohol pomzazed? I found that one quite nice. Would love to try 1-ethynyl-cyclohexan-1-ol too from the sound of it. Wonder what the cyclopentyl homolog of that, 1-ethynyl-cyclopentan-1-ol would be like.

Pomzazed-do you mean the molecule that idiot 'discovered' with his speshul magical fairy ability to sense vibrations and determine a person's 'spirit molecule', you know, as a special magical indigo child, might have some bioactivity of interest?

I think dresden's magic indigo child 'talent' is washing off on me.

I can sense it! I can sense his airy fairy magical unicorn spirit-molecule.

C4H4AsH, the carbon and hydrogen atoms prior to the heteroatom arranged in a ring structure otherwise identical to pyrrole, with a pair of double bonds between the 2,3 position and between the 4,5-position, the terminal H is attached directly to the heteroatom.

(I'm wondering if by giving this description, this so-called 'chemist' who can see special vibrations in people because of his fwuffy-wuffy majick in-dee-goh child special status will get it, or whether as I predict, his special talents will utterly desert him, without his reading the manual for chemdraw or something then using wikipedia.)

 

[Limpet_Chicken]

And you can inuit somebody's 'spirit molecule'?

Sorry, most of us here are western, and don't go around eating seal blubber for a snack.

 

[Dresden]

I had a friend who was musically trained as a child. I asked him what my voice's tone or key or whatever it is called was. He told me to yell loudly. I did. He then instantly told me it was E minor. This finding is based on frequency. Organic drug molecules also have a frequency. So just respect my gift for what it is or go away. Either way, just be nice. E = hf. It's not magic or an exact science. It's art. And you don't have to be nice or respectful, but this is my thread, and you are making yourself look like a real asshole by relentlessly trolling me. I'm not an aspiring drug designer. I am an established one.

 

[Dresden]

DINO

JAMES DEAN

DEENA

PAULA

MORGAN

 

[Limpet_Chicken]

Established drug designer? did you go to study under a hillbilly for that?

Or do you do it all by magic? Sorry but make claims like that and you, given your prior activity have to be called out on that.

I for one, reckon you are talking shite. And established drug designer? go on? for who? because I think you are lying.
'established drug designer' doesn't mean some idiot drawing random rubbish and giving it airy fairy names, and in plenty of cases ripping off the work of Sasha Shulgin (for fucks sake! Shulgin! you are one tasteless piece of odious garbage to do that!) and giving it a new name what with your special magic powers and that.

It means someone who goes to work, studies molecules and how they may interact with clinical targets, much of the time running screenings of a great many permutations of molecules, and thousands of tiny chemical variations on such a base molecule possible drug candidate for some purpose, and then doing so for the next molecule in a huge set, along with all the 'replace this hydrogen with fluorine, change a chalcogen or halogen here, lengthen or shorten THIS alkyl group, change an ester for an ether for a thioether for a......'

And using molecular modelling software, using it to pick your candidates based on steric, van der waals, salt-bridge, halogen bonding,hydrogen bonding etc. interactions and how docking a molecule with the protein target may alter the 3D conformation of the protein, giving the drug-protein complex a whole new lot of studies needing to be calculated in energy-minimized conformation.

And of course there are the 'orbitals are for mathematicians, chemistry is for those who love to COOK!' actual real chemists. Those who are smart, intelligent, but don't work for big pharma. You are neither. You. Are. Garbage. And a liar.

 

[Limpet_Chicken]

If you AREN'T telling lies, and taking us all for a bigger pack of cretins than you already for god only knows what reason have been permitted to keep on taking us for, and ARE an established drug designer...

Go on then. Prove it. What have you designed. What field of work are you in. What qualifications have you got relevant to such a career? (no, 'magic' does NOT count)

Prove to us you are really what you say you are. Because this thread could really benefit with a real pharmaceutical chemist's input to clean it up, foster intellectual discourse, because some foolish little twat started it, unfortunately, and worse it wasn't stamped down by the mods as the garbage it is.

A real pharmaceutical chemist, an expert, ESTABLISHED genius chemist, I'm sure they could turn this travesty of a thread around and start some intellectual discourse, to help make something of this thread, rather than for some insufferable and logic-devoid reason, the mods providing a bucket for somebody to vomit in.

Jesus fucking christ. Thank fuck! thank FUCK we now have our own established drug designer, maybe their qualifications will help us turn this from a fucking bucket full of spasmodically beshitten cretinous gastrointestinal trash, into something people could read and not only not want to drop the OP into a vat of acid, but even CONTRIBUTE to.

 

[Dresden]

Go Away.

Now,
Everybody Loves Raymond.

RAYMOND

I dunno, but I would imagine this molecule can kick some ass. LimpetChicken, be my guest.

 

[Pomzazed]

^ that should work. 4’-methoxycocaine isnt devoid of activity so methylphenidate analog should follow.
At least, one of the weird metabolite of cocaine is 4’-methoxy-3’-hydroxycocaine.(minor)
Apartt fron the major metabolites of N-desmethylcocaine, Methylecgonine, Benzoylecgonine.

 

[Limpet_Chicken]

You still have not backed up your claim to be in drug design. It still has absolutely zero substance WHATSOEVER; and given your repetitive posting of utter, total garbage about drugs that all you have been able to do in any such instance, is to 'assign' a trivial name to the structure devoid of meaning, prancing about as if you are Sasha Shulgin himself, whilst being able to give not ONE trip report. If you were anything but a liar,regarding being a 'drug designer' then you would have actually MADE, and tested these garbage molecules, and given us trip reports as feedback. Being a drug designer. well, it might surprise you Dresden; but it involves actually designing drugs. Drawing pictures, deciding what name you will pull from out of your arse and not even making educated reasoning as to WHY these specific molecules have been drawn; what activity you expect they would have and why doesn't make you a 'drug designer'.

Tell us, just how many of these compounds you have actually synthesized, how many have undergone biossay? or am I right in my belief that you have, in reality, not synthesized a single one of them much less ever tasted, and that all you have ever done is depict structures using chemdraw or similar and given them meaningless names.

The way you have acted, posting this meaningless dreck, that justifies our asking you to back up your claims. So, back up your lofty claims, or admit to us all, that you are a liar and stop with the posting of this damnable, disgraceful spammy and meaningless garbage. I find it absolutely unbelievable that this spamming of total fucking shit and lies has been allowed in ADD. Its fucking shocking to be honest, that this GARBAGE has been allowed to continue.

So, the time for you to prove the truth of your words, or for you to admit to us all that you are, in actual fact, telling us all lies and stop the shitspeak.

 

[Dresden]

Who do you think you are talking to like that? I don't have to explain or prove shit to you, punk. Fuck off.

 

[Limpet_Chicken]

Christ, I told you to back up a claim you yourself made. If you say it, you ought to be able to back it up. Show some knowledge, not necessarily claim to have done a specific (potentially incriminating) act at a given time or place, just knowledge, you have shown and contributed nothing.`

'sblood, I just took a fucking dump, the kind that feels like its going to go on until judgement day, and while I might barely able to STAND, I would still want you nowhere near my lab. From your posting history, I SERIOUSLY doubt any of the 'named' 'spirit molecules' could be made by you, you'd be a borohydride reduction away from taking yourself up in a pyrophoric fireball

Edit for the brain dead among us-I speak to you, dresden, worthless son of a gutterbegotten tu'penny syphilitic whore, trash born and to trash you will return. If I speak false in my doubt of you, prove otherwise. You won't. You have neither the honour nor the brains. Now, for the love of fucking christ, just do one already and stop befouling this otherwise good subforum with your mewling shitspeak, because I am fucking tired of it, and tired of you, you crow-born guttersnipe.

 

[Dresden]

BETH(ANY)

JOYCE

PHIL(IP)[IANS]

CHARLES

 

[Limpet_Chicken]

Second to last is already well known, its propylhexedrine.