Astavats
Bluelighter
^That sums up things nicely lol
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The Large and Nifty Not-quite-advanced Drug Chemistry, Pharmacology and More Thread
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MurphyClox
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^DREAD! Aweeeesome shit 
How do you name it? May I suggest something like Dreadaine...or no, BETTER: Benzene! YES! Holy, I'm genius. Goddamnit. Fuck Kekulé!
How do you name it? May I suggest something like Dreadaine...or no, BETTER: Benzene! YES! Holy, I'm genius. Goddamnit. Fuck Kekulé!
dread
Bluelighter
Well I'm still not satisfied, so I think I'm going to add a methylenedioxy or two to make it even awesomer.
P A
Bluelighter
Does dextroamphetamine (and its many DAR/NER cousins) significantly elevate extracellular levels of serotonin in clinically used dosages?
dread
Bluelighter
Would the malonate ester of psilocin form zwitterions?
MurphyClox
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Did I get it right: Esterify the phenolic OH with malonic acid, while leaving malonic acid's 2nd COOH untouched?!
Then the answer would most probably be: Yes, zwitterionic structure is expected.
- Murphy
dread
Bluelighter
Yes you got it right and thanks for the answer.
Next I'm wondering how this would affect the stability & pharmacodynamics of the compound... but I guess there's no real answer for that...
Astavats
Bluelighter
Can anyone give me binding affinity/data of atropine, hyoscyamine, or scopolamine on any opioid receptor subtypes (mu/kappa/delta)? I'm sure it's to a quite negligible extent but if it's been published I want to see it. I'd appreciate any help.
All the best.
All the best.
pharmakos
Bluelighter
i was thinking that since these chemicals tend to cohere they might actually end up forming structures on our receptors. perhaps different crystalline shapes cause different reactions. don't all the best drugs produce the prettiest crystals in the laboratory?
oh, p.s. "pseudo-crystal" is what i would call a crystal in its infancy... a nucleus that would form a crystal under different circumstances.
okay, perhaps this is a better way to put the abstract concept that's in my head into words.....
2C-I, for instance, likes to form crystals, no? crystals aren't too key to the concept... all that's necessary for this idea is the knowledge that 2C-I molecules tend to stick to each other.
we're (fairly?) sure that one 2C-I molecule will bind to one spot on one 5HT receptor, right?
well, will other 2C-I molecules stick to that one molecule that's stuck to the receptor?
MurphyClox
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Ahhhh, now I get what you mean. 
The answer is NO, several 2C-X-molecules won't stick together in solution, and we are talking about solution only.
On the one hand are crystals of 2C-X not stable in an aqueous environment. Consequence: They dissolve when water hits them. Sounds trivial, but it isn't. Remember that there are numerous compounds whose crystals are stable (read: insoluble ) in water, e.g. barium sulfate.
On the other hand - even if 2C-X-crystals would be insoluble in water - does it take more than two or three molecules of the same kind to gain of the stabilizing properties of a crystalline structure.
Peace! - Murphy
The answer is NO, several 2C-X-molecules won't stick together in solution, and we are talking about solution only.
On the one hand are crystals of 2C-X not stable in an aqueous environment. Consequence: They dissolve when water hits them. Sounds trivial, but it isn't. Remember that there are numerous compounds whose crystals are stable (read: insoluble ) in water, e.g. barium sulfate.
On the other hand - even if 2C-X-crystals would be insoluble in water - does it take more than two or three molecules of the same kind to gain of the stabilizing properties of a crystalline structure.
Peace! - Murphy
Imperial Tacohead
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This is probably a silly question, but I'm curious. Reading about the various uses of coca teabags, I've seen several people describe a method whereby they stick a bag in their mouths to chew or suckle, along with a bit of baking soda to "activate" the alkaloids. What does "activate" mean in this context? And why don't I read about people adding baking soda to their tea for the same purpose?
MurphyClox
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When chewing this stuff people are trying to absorb the active ingredients through the mouth's mucosa. For this you need the freebase form (lipophilic), which is liberated by the action of a base (=soda).
When drinking the tea, you want the ingredients to be in the form of salts, because these are more water-soluble. The alkaline pH of the small intestines turns them into the freebase form, ready for absorption.
- Murphy
When drinking the tea, you want the ingredients to be in the form of salts, because these are more water-soluble. The alkaline pH of the small intestines turns them into the freebase form, ready for absorption.
- Murphy
P A
Bluelighter
I've done plenty of reading on scopolamine and its derivatives, mostly as it relates to CNS actions, not pharmacochemistry, but to my limited knowledge, if the Devil's Breath has any affinity for opioid subtypes, it's most likely clinically and recreationally negligible.
Wish I could help definitively, but I have to warn you - don't get your hopes up for any decisive responses. I've asked a few questions here regarding pharmacophoric binding profiles before, and have been fully ignored. Pretty disappointing (and surprising), given the title "Advanced Drug Discussion," but apparently these boards are occupied mostly by little more than bored theoretical drug chemists without extensive access to pharm data.
Astavats
Bluelighter
Thanks for your response P A, I don't disagree with you about ADD but rather blame the "not-so Advanced" threads going around. The "what about this hybrid molecule...by the way I have no basis SAR or reasoning" or "silly named compound by vendor" threads aren't helping.
The reason I ask is a long story, but in short curiosity and to prove something to someone.
The reason I ask is a long story, but in short curiosity and to prove something to someone.
MurphyClox
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^In contrary to the pathetic babble of P A, the reason why nobody answered to your question could simply be that nobody knows the answer. ![:\](https://bluelight.org/xf/BL_Images/Orig_Emoji/wrygrin.gif "wry grin :\")
I'm neither bored nor do I not have extensive access to 'pharm data'. Actually, my access is quite extended. But - like most others here - do I have to set priorities and can not spend hours for searching some minor information for somebody I hardly know. Anyway, I made an exception and spend some hours (well, 2, to be exact) in search for an answer. And the answer is (as said above): We simply don't know.
I couldn't find a single hint that the binding of either atropine (resp. hyoscyamine) or scopolamine at the opioid-receptors was studied at any time. Both are well known and described in detail as muscarinergic ligands, but that's it so far.
A single source - albeit unreliable - states a Ki of 16200 for atropine; unit not given (haha), but it's nM I assume. Hot ligand was naloxone. Receptor-subtype is stated as "mainly µ-type" (LOL!). But as I said: The source is highly unreliable (European patent No. 289070 from 1988).
Peace! - Murphy
I'm neither bored nor do I not have extensive access to 'pharm data'. Actually, my access is quite extended. But - like most others here - do I have to set priorities and can not spend hours for searching some minor information for somebody I hardly know. Anyway, I made an exception and spend some hours (well, 2, to be exact) in search for an answer. And the answer is (as said above): We simply don't know.
I couldn't find a single hint that the binding of either atropine (resp. hyoscyamine) or scopolamine at the opioid-receptors was studied at any time. Both are well known and described in detail as muscarinergic ligands, but that's it so far.
A single source - albeit unreliable - states a Ki of 16200 for atropine; unit not given (haha), but it's nM I assume. Hot ligand was naloxone. Receptor-subtype is stated as "mainly µ-type" (LOL!). But as I said: The source is highly unreliable (European patent No. 289070 from 1988).
Peace! - Murphy
MurphyClox
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An own question this time:
Can somebody comment on the biological activity of "ICP" (1-(3-indolyl)-1-phenylcyclohexane), i.e. the indol-3-yl-analogue to PCP?
Active? Subjective effects?
Thanks in advance!
- Murphy
Can somebody comment on the biological activity of "ICP" (1-(3-indolyl)-1-phenylcyclohexane), i.e. the indol-3-yl-analogue to PCP?
Active? Subjective effects?
Thanks in advance!
- Murphy
As far as binding affinities go, why not take a look at something like the PDSP Ki database rather than asking someone to do the grunt work of looking up your stuff for you? If that's not working out for you, there's a stickied list of helpful resources that you could try, too.
I don't pretend to know a lot about chemistry, but I imagine that the information you're looking for is either going to be published in a paper somewhere (and thus accessible via one of these binding affinity databases), or you'll have to do the assay yourself. I doubt there's some secret database of 'pharm data' privy to only certain individuals. If there were, I doubt they'd be allowed to leak information from it in any case.
I don't pretend to know a lot about chemistry, but I imagine that the information you're looking for is either going to be published in a paper somewhere (and thus accessible via one of these binding affinity databases), or you'll have to do the assay yourself. I doubt there's some secret database of 'pharm data' privy to only certain individuals. If there were, I doubt they'd be allowed to leak information from it in any case.
Astavats
Bluelighter
Thank you Murphy, I appreciate it. I was afraid there would be no data/research on it so I'll gladly take this much you've dug up.
If this is in response to my post, then for the reason I was not aware of these sources. I've done the 'grunt work' myself searching and found nothing so I figured I would ask others who know more for help. I'm here to learn and nothing else. If this was not directed at me please overlook this.
If this is in response to my post, then for the reason I was not aware of these sources. I've done the 'grunt work' myself searching and found nothing so I figured I would ask others who know more for help. I'm here to learn and nothing else. If this was not directed at me please overlook this.
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On rereading my post, I realize that I came off as being a bit more caustic than I'd intended -- sorry about that.
The post wasn't directed at you specifically, more at the problem that you and P A were discussing of not being able to find binding affinities. Also, you're welcome. That database I mentioned is unfortunately pretty poorly normalized; things go by strange names and there are multiple apparently identical entries in some of the drop-down fields. I'm sure there are better ones out there.
The post wasn't directed at you specifically, more at the problem that you and P A were discussing of not being able to find binding affinities. Also, you're welcome.
That database I mentioned is unfortunately pretty poorly normalized; things go by strange names and there are multiple apparently identical entries in some of the drop-down fields. I'm sure there are better ones out there.
Astavats
Bluelighter
Understandable, no worries. Any direction at my beginner level pharma/chem intellect is always a helpful one. Going to check out your suggestions now. All the best!
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