Ideas on increasing the potency of drugs chemically.
I will open up with a quote from nbk2000 on Roguesci – in which he makes an interesting referance to some work on the Hive:
nbk2000
September 9th, 2004, 07:30 PM
The Hive bees have supposedly been dinking around with fluorination of cocaine alkaloids, to greatly increase the potency, 40x or more.
Nicotine is an alkaloid, though a different type, and could perhaps be amiable to such molecular tweaking.
As the lethal dose of nicotine is ~3mg, if you made it 10x more toxic, that'd be .3mg per adult, which is on order of VX.
now... Thats what I am getting at. I understand alkaloids are merely bioactive organic compounds. Nicotine is an alkaloid. Cocaine contains alkaloids. Now I also understand Methyl groups are the smallest and fit best through the Blood Brain Barrier. So let me explain...
The first theoretical step would be to Methylate the compound via transesterification – you replace the ethyl, propyl, etc groups with the smaller methyl group. Correct me if another group would work better. In my mind it appears this would make the compound absorb faster, give it lower Molar Weight (which may lower its BP – though I may be mistaken again). This makes it more Bioavailable (or whatever the term is).
Next we flourinate the fuck outta the poor alkaloid. I will presume this means we freebase it and react it with HF or something – or can someone please explain how to do this if I am wrong? Are we flourinating like as if we are nitrating except with F- rather than NO3-? Or are we merely making a flouride salt?
Now we should have the same alkaloid, just far more potent (and toxic) and far more bioavailable.
Dont shoot me for my mistakes – instead correct them!
NOTE: I am NOT a pharmacologist... YET. Teach me and I shall learn fast.
I will open up with a quote from nbk2000 on Roguesci – in which he makes an interesting referance to some work on the Hive:
nbk2000
September 9th, 2004, 07:30 PM
The Hive bees have supposedly been dinking around with fluorination of cocaine alkaloids, to greatly increase the potency, 40x or more.
Nicotine is an alkaloid, though a different type, and could perhaps be amiable to such molecular tweaking.
As the lethal dose of nicotine is ~3mg, if you made it 10x more toxic, that'd be .3mg per adult, which is on order of VX.
now... Thats what I am getting at. I understand alkaloids are merely bioactive organic compounds. Nicotine is an alkaloid. Cocaine contains alkaloids. Now I also understand Methyl groups are the smallest and fit best through the Blood Brain Barrier. So let me explain...
The first theoretical step would be to Methylate the compound via transesterification – you replace the ethyl, propyl, etc groups with the smaller methyl group. Correct me if another group would work better. In my mind it appears this would make the compound absorb faster, give it lower Molar Weight (which may lower its BP – though I may be mistaken again). This makes it more Bioavailable (or whatever the term is).
Next we flourinate the fuck outta the poor alkaloid. I will presume this means we freebase it and react it with HF or something – or can someone please explain how to do this if I am wrong? Are we flourinating like as if we are nitrating except with F- rather than NO3-? Or are we merely making a flouride salt?
Now we should have the same alkaloid, just far more potent (and toxic) and far more bioavailable.
Dont shoot me for my mistakes – instead correct them!
NOTE: I am NOT a pharmacologist... YET. Teach me and I shall learn fast.
