I Like to Draw Pictures of Random Molecules

[SKL]

all these pure dopamine agonists (afa,etc) also scream psychosis to me
especially if they are tweaked to add a dash of nmda actvity as random molecule thread likes to do

 

[DotChem]

the first one may well be dissociative stim! PCP+(retro)Methylphenidate

 

[SKL]

the first one may well be dissociative stim! PCP+(retro)Methylphenidate

cool molecule
but a troubling genre
combine 2 major neurotransmitter models of schizophrenia
(as I was saying probably as you were posting this)
what could go wrong?????
(yes, PCP and diphenidine, inter alia, do this and surprise they make you crazy,
i.e. the 'therapeutic' window between tripping and eating someone's lungs is small)

 

[Nagelfar]

(....e. the 'therapeutic' window between tripping and eating someone's lungs is small)

In his defense, he thought she was a sock.

 

[DotChem]

In his defense, he thought she was a sock.

Oh fuck! serious? he thought she was a sock??..can't stop LMAO

 

[DotChem]

cool molecule
but a troubling genre
combine 2 major neurotransmitter models of schizophrenia
(as I was saying probably as you were posting this)
what could go wrong?????
(yes, PCP and diphenidine, inter alia, do this and surprise they make you crazy,
i.e. the 'therapeutic' window between tripping and eating someone's lungs is small)

weird you posted this at exact same time I was drawing these molecules. Actually I didn't intend nmda-like stims just tweaking MPH and realize after that you might end up with a NMDA-stim.
But then again its is really hard to tell what could go wrong? "random" molecules such as these may or may not have either activity...
eg Benocyclidine (designed as NMDA) is a PURE DRI with no NMDA Serotonin or NE ..etc completely unexpectedly!

 

[SKL]

yeah especially in this rough genre of heterocyclic/multicyclic compounds you can definitely get all sorts of weird affinities popping up
not like PEAs which are relatively predictable

 

[Fruitofknowledge]

Imagine taking all structure motifs that give synthetic certain synthetic opioids their potency and merging them all in to one. I took the structure of Anilidopiperidines like Carfentanil and Bentley compounds like Etorphine and did the hypothetical merger of structures to make a ultra-potent mu agonist! Stop you're mad, ha ha ha! If you replace the propanamide group of fentanyl with a acrylamide group it doubles the potency, if you add a fluorine atom at the ortho position of the benzene ring it doubles the potency of fentanyl. Research on Bentley compounds denotes that pentyl, butyl, and isopentyl on the 7 carbon on the cyclohexane ring are the most potent substitutes 4500, 5200, and 9200X the potency of morphine respectively. Adding a isopentyl instead of Etorphine's butyl group produces a compound almost twice the potency. Targeting substitutes that increase binding affinity and you get this!

 

[Fruitofknowledge]

R-4066 an open chain opioid drug which is an analogue of the opioid analgesic methadone, or more accurately Norpipanone, where the metabolically labile dimethylamino group has been replaced by a piperidinospiro group. Developed by Janssen Pharmaceutica,^[1] it is around 212x more potent than methadone as an analgesic in animal tests, with an effective oral dosage of 0.07 mg/kg, but is slightly shorter acting, with a duration of action of around 3 hours.

 

[SKL]

Imagine taking all structure motifs that give synthetic certain synthetic opioids their potency and merging them all in to one. I took the structure of Anilidopiperidines like Carfentanil and Bentley compounds like Etorphine and did the hypothetical merger of structures to make a ultra-potent mu agonist! Stop you're mad, ha ha ha! If you replace the propanamide group of fentanyl with a acrylamide group it doubles the potency, if you add a fluorine atom at the ortho position of the benzene ring it doubles the potency of fentanyl. Research on Bentley compounds denotes that pentyl, butyl, and isopentyl on the 7 carbon on the cyclohexane ring are the most potent substitutes 4500, 5200, and 9200X the potency of morphine respectively. Adding a isopentyl instead of Etorphine's butyl group produces a compound almost twice the potency. Targeting substitutes that increase binding affinity and you get this!

^yeah but would it be any fun? as a former opiate addict fentanyl sucks to begin with and a lot of the analogs are even worse ...

reminds me of this Shulgin quote:

The extension of the two-carbon chain of mescaline by alpha-methylation to the three carbon chain of TMA approximately doubled the potency of the compound. And it was felt to be a completely logical possibility that, by extending it one more carbon atom, to the four carbon chain of alpha-ethyl-mescaline, it might double again. And following that logical progression, the doubling of potency with each additional carbon atom, the factor would be 2 to the 7th power by the alpha-octyl (or 256x that of mescaline, or a milligram as active dose) and with a side chain of a 70-carbon alkyl group (alpha-heptacontylmescaline) it would take just a single molecule to be intoxicating. This was rich fantasy stuff. As an active compound, just where would it go in the brain? With an 80-carbon side-chain, would one-thousandth of a single molecule be enough for a person? Or might a single molecule intoxicate a thousand people? And how long a chain on the alpha-position might be sufficient that, by merely writing down the structure on a piece of paper, you would get high? Maybe just conceiving the structure in your mind would do it. That is, after all, the way of homeopathy.

 

[Fruitofknowledge]

I talked about Normethylphenethyltramadol and its desmethyl ether counter part as potential potent legal analogs not covered by the US Analog Act with a estimated potency of 1-1.4X for the first compound and 6-10X for the second compound. I received a post that it would fit into the addition binding pocket because its an open chain. Diampromide around morphine strength open chain fentanyl analog. If you remove the N-phenyl group off of fentanyl it almost abolishes all activity, where in fact tramadol and O-desmethyltramadol are way more active by there selves.

 

[Fruitofknowledge]

I talked about Normethylphenethyltramadol and its desmethyl ether counter part as potential potent legal analogs not covered by the US Analog Act with a estimated potency of 1-1.4X for the first compound and 6-10X for the second compound. I received a post that it wouldn't fit into the additional binding pocket, because its open chain structure. Diampromide around morphine strength open chain fentanyl analog. If you remove the N-phenyl group off of fentanyl it almost abolishes all activity, where in fact tramadol and O-desmethyltramadol are way more active by there selves. The open chain structure doesn't make a difference to binding etorphine, fentanyl and bromadol all have additional substitutes that reach the extra binding ''pocket''.

 

[Fruitofknowledge]

opioids I imagined

 

[Fruitofknowledge]

Opioids analogs I imagined

 

[Fruitofknowledge]

I can get my picture to paste!

 

[SKL]

your image links are an indecipherable mess, dunno where you are trying to post from
best thing to do is just upload to tinypic.com
also this site produces very attractive structures if you just IUPAC name your molecule

 

[roi]

Actually please use imgur.com.

Tinypic is so 1990.

 

[Friman1987]

PRO-LAD: https://en.wikipedia.org/wiki/PRO-LAD
OSU-6162 (PNU-96391): https://en.wikipedia.org/wiki/OSU-6162
UH-232: https://en.wikipedia.org/wiki/UH-232
5-OH-DPAT:https://en.wikipedia.org/wiki/5-OH-DPAT

 

[Dresden]

Opsin doesn't even require a strictly IUPAC name to do its magic. For most molecules, it accepts a wide variety of butchered, though still basically logical, monikers.

And Friman1987, please consider using http://opsin.ch.cam.ac.uk in the future, as the molecular sketches you're posting now are far too small and faint to be easily understood. Just a friendly suggestion (aka subtle command, lol).

As for the PiHKAL quote, I actually did get high once about 10 years ago after drawing this molecular structure

on a piece of paper with a Sharpie, never to be repeated. I'm sure other factors which I was not aware of were at play, though. Still, it was an all around awesome time and is actually one of the best memories of my life thus far.

 

[aced126]

Opsin doesn't even require a strictly IUPAC name to do its magic. For most molecules, it accepts a wide variety of butchered, though still basically logical, monikers.

And Friman1987, please consider using http://opsin.ch.cam.ac.uk in the future, as the molecular sketches you're posting now are far too small and faint to be easily understood. Just a friendly suggestion (aka subtle command, lol).

As for the PiHKAL quote, I actually did get high once about 10 years ago after drawing this molecular structure

on a piece of paper with a Sharpie, never to be repeated. I'm sure other factors which I was not aware of were at play, though. Still, it was an all around awesome time and is actually one of the best memories of my life thus far.

Expand on this event?

Also, the images Friman posts appear very large for me.