Forum: The Bleeding Edge

As I've posted out a few times, the patent on loperamide (US 3714159) contains a table (Table 1 on page 4) that gives the analgesic dose of many analogues. For loperamide it's 80mg/kg (so for the average person with no tolerance, that means about...

http://www.google.com/patents/US2783233?pg=PA1&dq=rapoport+%2210-hydroxy%22&hl=en&sa=X&ei=9J9wUJLkHIKT0QWag4CwCA&ved=0CDIQ6AEwAA#v=onepage&q=rapoport%20%2210-hydroxy%22&f=false The above link is to US Patent 2783233 in which morphine is...

I've noted that an number of papers which show that replacing the (S)tyrosine sub-unit of DAMGO with an (R)2,6-dimethyltyrosine increases affinity for the μ receptor by a factor of 357 and thus potency is increased x 187 (duration also goes up). ...

http://www.guardian.co.uk/science/2012/jul/21/chemputer-that-prints-out-drugs Chemistry professor Lee Cronin with the 'chemputer' he has adapted from a 3D printer. Photograph: Murdo Macleod The first step to Star Trek TNG's replicator is...

I've always been fascinated by the most unusual structure of tilidine and more specifically (1R,6S) nortilidine. I found an interesting derivative... In spite of them having the opposite stereoactivity - they both overlay levorphanol VERY...

The 2 methoxys overlay and the C=O of the ester function overlays the 6 C=O of methoxymetopon. (3R,4R) prodine is x13 more potent than MPPP but I would expect this derivative to be a fair bit stronger. There are examples of esters at the 3 position...

(or vice versa) My prayers of what to do with my life just got answered. :'( Requirements; get to Vancouver BC (lucky for us in the Pacific Northwest) Have been a junkie for 5 years Have used in the past year Two attempts at treatment...

http://en.wikipedia.org/wiki/Opioid#Table_of_morphinan_opioids Who better to unveil to, my last hour & a half spent adding an exhaustive table of all the molecular images for morphinan type opioids extant on Wikipedia, than those here at...

a few months back i lost someone very tragically. she was a mother... a nurse... and a beautiful person her family had enabled her to the point where it was normal to throw a pee pad under her while she was knocked out on a cocktail of fent,...

It's always been a competition (seemingly) amongst designers of opioids to see how few carbon atoms they could use in their structure. The common target was usually M potency. I remember that they made quite a big thing about tapentadol over this. ...

The above is a widely studied class of opioids. Example 2 is around x 500 morphine in potency. The question is - would they be considered analogues under the CsA act? Of course, one would expect the N-(2-furanylethyl) analogue to be still stronger...

I was doing some research today, like I sometimes do, and I discovered a antitussive commonly abused in Korea. It's called "Zipeprol"- it has opioid and non-opioid effects. It can cause siezures at high doses, but it seems pretty safe when used by...

NKTR-192 is Nektar Therapeutics' product candidate for the treatment of moderate to severe acute pain. NKTR-192 is a novel mu-opioid analgesic created using Nektar's advanced polymer conjugation technology to slow drug entry into the central nervous...

Sposed to say purinergic(could a mod edit the title?), accidently hit enter before I was ready to post. Not exactly new, from 2009. http://www.ncbi.nlm.nih.gov/pubmed/19442100 "The effects exerted by P1 and P2 as well as by A1 and A2...

In the BNF (British National Formulatry) oxymorphone is described as 7-9 x morphine in potency. N-phenylethyl noroxymorphone is described in 'Current Medicinal Chemistry' page 435 says that it is stronger than the parent compound (I take this to be...

I just read a message sent to me from one of the guys who edits the pharmacutical section of Wikipedia. He noted that the super-potent agonists (e.g. OHMEfentanyl) cause tachyphylaxis SO fast, that they practically start becoming antagonists after a...

One Mark P. Wentland has developed a biosteric replacement for the phenolic -OH in MOR+ compounds. It's simply a CONH2 & since the body cannot easily attach this group, the compounds are MUCH longer acting (while being very similar in potency). I...

I feel confident in stating that loperamide is not a good opioid. It doesn't pass the BBB too well & the ABC pumps it out of the brain pretty efficiently. However, it MAY be a useful precursor (assuming that it's safe - there is the issue of toxic...

Well, this thread has two purposes. One to talk about tolerance. Two things about tolerance...if I want to be able to continue my habit, I have got to find a way to fight it. I've been trying for years with different routines, and drugs, and...

Hello, I've made an intro post in H&G, but since I am hoping this area of the site(along with opiates in nature) will be most useful and interesting to me, I thought I should make myself known over here. Um..I'm an opiophile, like you. I'm sure...

The book 'Pain: current understanding, emerging therapies, and novel approaches to Treatment' by By Chas Bountra, Rajesh Munglani et al discusses a potent opioid now undergoing trial. It's Ki at the Mu receptor is 3.3 (morphine is 19.3) & it has...

we all know about o-desmethyltramadol and tapentadol but there are some really interesting tramadol analogs, some are around the strength of fentanyl. here are a few but I'm interested if anyone knows of others or of tapentadol analogs, if you do...

Recently I took some time to really read up on the 4,4 diphenylheptanone (methadone) class of analgesics. I have sampled quite a few & believe me, it's a good, synthetically simple scaffold capable of making potent, euphoric opioids. While methadone...

Don't know if this is only new to me, heard only of DXM and so on, yet. Thought it might be interesting to other people, too ... http://www.freepatentsonline.com/7250422.html /********************************************************* ...

Furanoeudesma-1,3-diene and curzarene There are myrrh terpene isolates available that are showing extremely strong potential. Anyone here have any experience with them? SWIM has tried (so far) up to 75mg oral, 50mg smoked and 50mg...

Morphine shot affects testosterone levels "The use of opioids puts a physiological block on the reproductive system and can induce a long-lasting absence of these essential hormones from the blood and the brain, Aloisi says. A lack of the...

I plan on making a powerful and comprehensive Narcotic Equivalence calculator when time permits (will probably be a long time from now). In theory, it could also be used for benzodiazepines or for conversion between any other class of drugs too. ...

aye boro, woody et al what do you make of this?http://en.wikipedia.org/wiki/RB-101 sounded interesting to me with my complete absence of chemistry knowledge apologies if this has been discussed before.

Beta-arrestin is a molecule which is directly involved in tolerance in family of GPCRs. The opioid receptors belong to that family. As expected, there are several studies showing arrestin is intimately related to opioid tolerance, for example: ...