• N&PD Moderators: Skorpio | thegreenhand

Ketamine salts solubility

Status
Not open for further replies.
Their are quite a few studies on sublingual and buccal administration of benzodiazepines with the papers available on-line. The conclusion was that onset and bioavailability was almost identical to IV administration. Neither are instant which I suggest is because the drug has to cross the BBB and it's that which is the limiting factor.

They are the first to point out that it's an off-label ROA BUT at least it ensures that until administration, the drug is being stored in an approved format. Solutions (e.g. injectable formulations) generally require careful formulation and almost always have a much shorter shelf-life. I don't think they become dangerous, I just think that N-oxides (for example) form which slowly reduces the amount of active.

I mean, if it psychologically makes you feel better to have a nasal spray then by all means, but it seems like a lot of research is already out there and if sublingual essentially achieves the same goal, it requires no action. You just have to remember to hold them under your tongue.

Lol using Midazolam sublingual has similar issues as trying to use the tablets for nasal just bit less annoying as it has a lot of binders and fillers and doesn't taste good I'd imagine either... I just hope it doesn't taste awful like some benzodiazepines.

I also find using benzos in a solution sublingually instead of via a crushed pill into a powder then dumped under the tongue does appear to absorb quicker and more thoroughly but that might just be placebo on me lol idk... it makes sense though.


Also the studies for sublingual aren't a good ROA for every single benzo are you sure Midzoalm is 1 of them? I'd assume it is based on the fact it's suitable for nasal administration.


If Midazolam is a benzo suitable for sublingual ROA where do I find out 100% for sure the potenital absorbption % for sublingual ROA of Midazolam which I'll make a solution out of the pills for that? Actually I just remembered that Midazolam DOES have a lower oral bioavailability but I'm not sure the difference of the sublingual vs. intranasal bioavailaiblity % but if someone with knowledge on that subject can figure it out.

Midazolam is a bit weird in terms of ROA absorption % etc. compared to most other RX benzos these days I to make a cocaine nasal spray since I have some lying around and I've always wanted to make it for various reasons like less damage to the nostrils and more effective absorption potentially but my concern has always been on how do I correctly and acccurately measure the dose per spray even if I know exactly how pure it is? its roughly 84%. What information do I need to help determine the dose per spray of liquid with I'm assuming PURIFIed and not distilled water will work and i don't need any additional solvent for cocaine as I know it's super water soluble.
 
Last edited:



Yep - I just posted the first three mentioning midazolam but their are MANY. The key finding that sublingual was as effective as IV. Midazolam is particularly water-soluble (for a benzodiazepine) and so is the most suited to sublingual administration but the methodology has been applied to most of the more water-soluble examples.
 



Yep - I just posted the first three mentioning midazolam but their are MANY. The key finding that sublingual was as effective as IV. Midazolam is particularly water-soluble (for a benzodiazepine) and so is the most suited to sublingual administration but the methodology has been applied to most of the more water-soluble examples.

Okay thanks for the information. Now I'll definitely use sublingual route instead if it is indeed truly the same as I.V. or at least better absorption than a nasal spray. But I read conflicting information so I'm not sure what source of information to trust for a "verified" amount of absorption?
 
Last edited:
1-carbomethoxy-5-benzyl-2,3-dihydro-5,6,7-trihydro-1H-pyrrolizine.png


NEO-TORADOL
1-carbomethoxy-5-benzyl-2,3-dihydro-5,6,7-trihydro-1H-pyrrolizine

Looking for a stimulant.
 
  • Like
Reactions: izo
Long experience has taught me that any compound that takes more than four (efficient steps) to produce either requires a special production-line (if a lot is needed) or costs an absolute fortune (look at butorphanol - $284000/Kg even after 40 years of development.

I mean, a LOT of compounds listed are ALREADY listed as building-blocks with PubMed offering suppliers - but just ask for the price for a gram.

I was quoted $15000/g for 3,4-dihydro-2H-spiro[naphthalene-1,4'-piperidine] - and that's just an intermediate.

What you are paying for is someone who can has invested millions on equipment & who can reliably produce a stated compound for maybe $12000/Kg - that might seem a high profit margin but sometimes their theoretical route doesn't work and they make a loss. BUT you pay the quoted price.

Try getting a quote for something you have drawn that is already in PubMed. It will be thousands per gram - and that's people who have spent decades working in the field of supplying building-blocks.

Unless it's something active (and who knows since no rationale is given) and indeed HIGHLY active then it isn't going to happen.

Believe me, Chinese labs are not above just sending something else so you need instrumentation data and, obviously, the ability to read it.
 
^--Unless, you can get very good yields somehow. 👍 Would you consider the following to be impractical as well? Starting with 3,5-dimethoxybenzaldehyde, I guess.

1-(3,5-dimethoxy-4-pentylphenyl)-2-aminopropane.png


867-5309
1-(3,5-dimethoxy-4-pentylphenyl)-2-aminopropane

All I Know Is You've Got The Money, But That's Got Nothing To Do With A Good Time!

I Have Thoroughly Enjoyed Its 2C Homologue On More Than One Occasion.
 
Last edited:
1-phenyl-1-carboethoxy-2-methylaminopropane.png


NICOLE
1-phenyl-1-carboethoxy-2-methylaminopropane

Just 4 Steps Away From Ephedrine, A Natural Product.
 
1-phenyl-1-oxo-2-aminopropane.png


KHAT
1-phenyl-1-oxo-2-aminopropane

Just 5 Steps Away From

2-amino-1-phenyl-1-carbomethoxy-propane.png


DAWG
2-amino-1-phenyl-1-carbomethoxy-propane
 
Yeah - it's still 14 steps (if memory serves). Of course, cleaver chemists will use retrosynthetic strategy and MIGHT find a more efficient synthesis from some more common compound.

But I've been looking for 26 years. Nothing yet. But sooner or later one of the hundreds of intermediates I check on a weekly basis will suddenly become cheap. Most of drug design it just THAT mundane.
 
Last edited:
1-phenyl-2-isopropylaminopropane.png


ANDREA
1-phenyl-2-isopropylaminopropane

2 Steps:
1) Wacker allylbenzene
2) Reductive Amination Of P2P With Isopropylamine And NaBH3CN in methanol.

The N-isopropyl amp moiety is not completely male or female.
 
1-(1,3-benzodioxole-5-yl)-2-isopropylaminopropane.png


DAVE
1-(1,3-benzodioxole-5-yl)-2-isopropylaminopropane

Same 2 Steps With A Little Twist: Just Replace P2P With MDP2P from safrole.

There Is Also David Letterman, Dave Thomas From Wendy's, Davy Crockett, etc.
 
Last edited:
1-(4-methoxyphenyl)-2-isopropylaminopropane.png


EVAN_WILLIAMS
1-(4-methoxyphenyl)-2-isopropylaminopropane


Star Anise Flavor a la Jagermeister.
 
1-(naphthalene-2-yl)-2-(1-pyrrolidinyl)-1-oxo-pentane.png


RUSH_HOUR
1-(naphthalene-2-yl)-2-(1-pyrrolidinyl)-1-oxo-pentane

Ah, the faint scent of mothballs.
 
1-(3,4-dichlorophenyl)-2-aminopropane.png


LUKE (See also MXE.)
1-(3,4-dichlorophenyl)-2-aminopropane

This is one of the first drugs found in this thread that I tried. It was only so so (with mxe being much more remarkable) UNLESS combined with Adderall (a formula of amp), which I did. Next,

1-(3,4-dichlorophenyl)-2-methylaminopropane.png


JESUS_OF_NAZARETH
1-(3,4-dichlorophenyl)-2-methylaminopropane

Probably the best high ever. But is one way telepathy a side effect?

1-(3,4-dichlorophenyl)-2-ethylaminopropane.png


JUDAS
1-(3,4-dichlorophenyl)-2-ethylaminopropane

I whipped myself into a head bangers balling frenzy that night. Too much energy.

These Are All Technically Legal btw.
 
Last edited:
1-(3-pyridinyl)-2-aminopropane.png


HOMER
1-(3-pyridinyl)-2-aminopropane

1-(4-pyridinyl)-2-aminopropane.png


BARTHOLOMEW
1-(4-pyridinyl)-2-aminopropane
 

Above is the original paper discussing the extreme potency of BDPC. What is so fascinating is that Lednicer et al. were able to construct a Dreiding model which shows that the compound can perfectly overlay fentanyl.

'The two benzene rings can be directly superimposed (though the link to the rest of the molecule is rotated by 60'). The basic nitrogen atoms of the two molecules similarly fall in the exact same spot in space as do the extreme right-hand benzene rings. The hydroxyl
group in 1 falls in the middle of the amide function of fentanyl.'


I think this especially useful for students who struggle to visualize a chemical in 3D. When drawn in 2D two compounds may look entirely unrelated but in fact, overlay perfectly in 3D.

Other examples of this are U-47700 perfectly overlaying prodine or 4-phenyl phenapromide perfectly overlying fentanyl. I can extend this to other classes but I've stuck to the class of compound of with I am (fairly) certain of the 'salient features;.
 
N-methyl-2,3-methylenedioxy-morphinan.png


DXE
N-methyl-2,3-methylenedioxy-morphinan

N-methyl-2,3,4-trimethoxymorphinan.png


MARDI_GRAS
N-methyl-2,3,4-trimethoxymorphinan
 
N-methylmorphinan.png


AEON_FLUX
N-methylmorphinan

1,7-bisphenyl-(hexahydro-1H-pyrrolizine).png


BISQUIK_BISCUIT
1,7-bisphenyl-(hexahydro-1H-pyrrolizine)

1,7-bis(3,4-methylenedioxyphenyl)-(hexahydro-1H-pyrrolizine).png


SPUMANTE
1,7-bis(3,4-methylenedioxyphenyl)-(hexahydro-1H-pyrrolizine)

(6aR,10aR)-6,6-dimethyl-9-carbomethoxy-3-pentyl-6a,7,8,10a-tetrahydro-6H-benzo%5bc%5dchromen-1-ol.png


THC-LITE
(6aR,10aR)-6,6-dimethyl-9-carbomethoxy-3-pentyl-6a,7,8,10a-tetrahydro-6H-benzochromen-1-ol
 
Last edited:
Status
Not open for further replies.
Top