From: BME Subject: Dermorphin Date: 1997/08/06 Newsgroups: alt.drugs.chemistry,alt.drugs.hard,alt.drugs,rec.drugs.chemistry, rec.drugs.misc,sci.med.pharmacy --Dermorphin-- I recently ran across this compound in a chemical catalog. A blurb mentioned that it is a mu agonist, a la morphine. This immediately piqued my interest. So, I ran Medline search. (Abstract @ end of post) Be amazed at what I found, apparantly dermorphin is ...30X more potent than morphine ...Slower to produce tolerance ...Less hellish in withdrawal ...Naturally occuring ...UNSCHEDULED by the DEA Is this amazing or what? Does anyone have any experience with this? Have opiate users been touched by the hand of God? Read this abstract: Title Production of antinociception by peripheral administration of [Lys7]dermorphin, a naturally occurring peptide with high affinity for mu-opioid receptors. Author Negri L; Lattanzi R; Melchiorri P Source Br J Pharmacol, 1995 Jan, 114:1, 57-66 Abstract 1. The opioid activity of the amphibian peptide, [Lys7]dermorphin, was studied in rats and mice. When administered intracerebroventricularly (i.c.v.), intravenously (i.v.) or subcutaneously (s.c.) it produced a long lasting analgesia. Its antinociceptive potency exceeded that of morphine 290 times by i.c.v. injection, and 25-30 times by peripheral administration. 2. The dose-response curves of [Lys7]dermorphin antinociception were shifted to the right by the pretreatment with naloxone (0.1 mg kg-1, s.c.) or with the mu 1-selective antagonist, naloxonazine (10 mg kg-1, i.v. 24 h before peptide injection). 3. The peptide also displayed potent antinociceptive effects in a chronic inflammatory pain model (rat Freund's adjuvant arthritis). In this pain model, systemic administration of the peptide raised the nociceptive threshold more in inflamed than in healthy paw. 4. High central and peripheral doses of [Lys7]dermorphin in rats produced catalepsy. The cataleptic response was antagonized by naloxone but left unchanged by naloxonazine pretreatment. 5. In rats and mice, central or peripheral administration of [Lys7]dermorphin induced a significantly slower development of tolerance to the antinociceptive effect than did morphine. 6. Upon naloxone precipitation of the withdrawal syndrome, [Lys7]dermorphin-dependent mice made fewer jumps and lost less weight than the morphine-dependent animals. Withdrawal hyperalgesia did not develop in [Lys7]dermorphin-dependent mice. 7. In conclusion, [Lys7]dermorphin seems to be a unique opioid peptide having a high penetration into the blood-brain barrier despite its low lipid solubility. This peptide causes fewer side-effects than other opioids and appears less likely than morphine to cause physical dependence in rats and mice. ==================================================================== From: randall.braun@gecits.ge.com (epibatidine) Subject: Re: Dermorphin Date: 1997/08/08 Newsgroups: alt.drugs.chemistry,alt.drugs.hard,alt.drugs,rec.drugs.chemistry, rec.drugs.misc,sci.med.pharmacy On Wed, 06 Aug 1997 16:15:37 -0500, BME wrote: >=snip= The dermorphins (most are potent mu agonists) and deltorphins (most are potent delta agonists) were originally isolated from alcoholic extracts of the skin secretions of certain species of rare frogs (some of the 'poison arrow'-type frogs in Ecuador?) found in South America by a group of Italian researchers, which include some of the authors mentioned in the abstract. Some of the natural peptides are somewhat unique in vertebrates, as they contain a D-amino acid in the 2-position, which gives them resistence to many endogenous proteases, thus endowing them with longer T1/2's. It's also interesting that the (frog) gene for these peptides codes for the L-amino acid, and it's apparently enzymatically converted to a D-amino acid during or after translation. There is also some evidence (immunochemical) that a related peptide is also produced in low quantities in mammalian brain (rat). Numerous synthetic modified peptides have also been studied, leading to some extremely potent analogs. -Randall Braun, MS Pharmacology, specialty area: opioids & opioid receptors; drugs of abuse. ==================================================================== From: "3.4-MethyleneDioxyMethaAmphetamine" Newsgroups: alt.drugs.hard Subject: Dermorphin Report Date: Mon, 3 May 1999 11:43:48 -0700 Well Guys, After being what we think were the first humans to use this peptide recreationally, here is my report on it (just so you know what to expect in case you ever decide to partake in it): Anyone who has done an opiate of any form already knows what to expect. Having never done Morphine myself, I cannot comapare it to Dermorphin, however it is supposedly 30-60x the potency when taken orally, and 200-300x the potency when taken I.V. We purchased 1mg for $20. Expensive, you say? Not really considering that 1mg is apporx. 5-7 oral doses and 10 I.V. doses. If you decided to inject the entire 1mg, you would die faster than instantaneously. The high that Dermorphin gave me was just like any other opiate I have ever done...warm, fuzzy, well-being, euphoria (hic-ups, in my case), slightly itchy at times (I'm sure you know what I mean). If you want me to compare it to something, I would say think of a Hydrocodone or Oxycodone high and multilply that by 500 or so...then you should have an idea. We each took about 100-150mcg initially sublingualy. I felt the first effects within 10 minutes...I was trying to figure out if it was placebo or not, but after 30 minutes I knew my body had just been ravaged by opiates. We all finished off the vile, so I would assume that by the end up the night I ended up taking 200-259mcg total. The high lasted for appoximately 4-6 hours. It wouldn't be foreign territory for the users of any opiate drug. I'll tell you right now that it does not compare to H, so don't expect that. But then again, I didn't take it I.V. The day after I did Dermorphin, I decided to snort half a hit of H, and it's definately more potent (nothing I would ruin my life over, mind you. H takes you away from all your problems, which is why I can see people getting [mentally and physically] addicted. But what happens when you are off it? You're problems are still right there. But it DOES feel frighteningly good ;) Anyway, that's about all I can tell you about Dermorphin...typical opiate high....VERY potent...unscheduled by the DEA...available for order from many research companies (although most of them don't sell to individuals). I won't tell you any companies on here, because the the last thing I want is for tons of people to order it and O.D., as it is VERY potent. Then you would have ABC and Hard Copy at your door with some horseshit like "New Designer Drug-Dermorphin...the Legal Killer!" Heheh, sorry about that. Besides, like I told you, 99% of the companies won't sell to the public. Well, now you guys know about this particular peptide...it IS orally active, it DOES pass the blood brain barrier, and it is, basically, an opiate (although technically it's not). That's about it for my report. Hope this quenched your curiosity. Like anything else, be careful when trying it, and enjoy! On a final note, it makes people (myself included) feel so stupid for trying to hookup Vicodin, Percodan, MS Contin, etc...we had this shit staring us in the face the entire time. Ack. Oh well, later for now.... -Atrox