theobromos Posted February 21, 2004 We now appear to have the full range of opioid agonists available from non-opium sources: Life Sci. 2004 Mar 12;74(17):2143-55. Antinociceptive effect of 7-hydroxymitragynine in mice: Discovery of an orally active opioid analgesic from the Thai medicinal herb Mitragyna speciosa. Matsumoto K, Horie S, Ishikawa H, Takayama H, Aimi N, Ponglux D, Watanabe K. Laboratory of Chemical Pharmacology, Graduate School of Pharmaceutical Sciences, Chiba University, 1-33 Yayoi-cho, Inage, Chiba 263-8522, Japan. Mitragynine is an indole alkaloid isolated from the Thai medicinal plant Mitragyna speciosa. We previously reported the morphine-like action of mitragynine and its related compounds in the in vitro assays. In the present study, we investigated the opioid effects of 7-hydroxymitragynine, which is isolated as its novel constituent, on contraction of isolated ileum, binding of the specific ligands to opioid receptors and nociceptive stimuli in mice. In guinea-pig ileum, 7-hydroxymitragynine inhibited electrically induced contraction through the opioid receptors. Receptor-binding assays revealed that 7-hydroxymitragynine has a higher affinity for mu-opioid receptors relative to the other opioid receptors. Administration of 7-hydroxymitragynine (2.5-10 mg/kg, s.c.) induced dose-dependent antinociceptive effects in tail-flick and hot-plate tests in mice. Its effect was more potent than that of morphine in both tests. When orally administered, 7-hydroxymitragynine (5-10 mg/kg) showed potent antinociceptive activities in tail-flick and hot-plate tests. In contrast, only weak antinociception was observed in the case of oral administration of morphine at a dose of 20 mg/kg. It was found that 7-hydroxymitragynine is a novel opioid agonist that is structurally different from the other opioid agonists, and has potent analgesic activity when orally administered. Share this post Link to post Share on other sites
friendly Posted February 22, 2004 Coming soon to a street corner near you... It's inevitable. For instance: I have been speaking with a person who wants me to prepare a Sceletium tortuosum 5x and 10x concentrate from pharmaceutical grade material. I have samples from the same person of another Sceletium t. 5x that has already been produced and marketed, but the manufacturer was inconstant. Seeing as the herb is orally active as an SSRI in doses of 50 mg and much lower when smoked or insufflated, to make an extract with an oral activity of 5mg would seem to be pushing the envelope and making it more likely that someone will show up at the emergency room in an ambulance, suffering from serotonin syndrome or overdose. At Mind States IV I saw a full spectrum Tansy (Tanecetum vulgare) extract which was purported to be 85% thujone. I asked the chemist what else was in it and he said "nothing." The phytochemical and ethnobotanical databases of James Duke (which I have URl'ed here before) list over 40 different compounds, some highly toxic and others carcinogenic in the Tansy flower. I notified his distributor by sending him the Duke chemical printout for Tansy and he stopped selling it. I have seen Voacanga africana and T. iboga full-spectrum extracts strong enough to scare the pants off anyone not fully ready. Not to mention the dangers inherent in making a full-spectrum T. iboga extract which would concentrate the toxics as well as the ibo. Many herbs have undesirable components that will be concentrated in full spectrum (the simplest to make) extracts. Share this post Link to post Share on other sites
Torsten Posted February 22, 2004 I don't have a problem with producing and selling extracts that overcome the 'is it placebo or is it not' effect. ie, with salvia this was the difference between plain herb and 5x. With argemone it is similar. With lily I presume it is about 5x or 10x as well. The there is the 'yuck' factor that sometimes requires some extraction or concentration. For example iboga rootbark, which is almost impossible to ingest at the required rate and certainly produces a very bad mindset caused by physical discomfort. I've also made tobacco 100x and several almost pure compounds for experimental reasons, but I would never sell them. So yeah, I don't mind extracts, especially because I don't like smoking (which is often the most efficient delivery method), but common sense needs to prevail. Friendly, I see that your extracts are along about the same lines as what I would do them.... purposeful, but not too strong. Share this post Link to post Share on other sites
mescalito Posted February 22, 2004 Mother Nature always packages her gear just right Share this post Link to post Share on other sites
Torsten Posted February 23, 2004 Originally posted by mescalito: Mother Nature always packages her gear just right Mother Nature packs in a hell of a lot of tar and other crap into many things. She also sometimes mixes outright toxic constituents with the desirable ones (eg Peganum harmala). I hate to say it, but she isn't perfect Share this post Link to post Share on other sites
Machine Elf Posted February 23, 2004 Hi Torsten, I think I remember some mention a while back of a possible Nymphaea extract at SAB. Is this still on the cards? Belfy Share this post Link to post Share on other sites
Torsten Posted February 24, 2004 Belfy - we are working hard at it. I think it hsould be ready wihtin about 10-14 days. Not sure if it will be 5x or 10x yet as we haven't experimented with the potency. Share this post Link to post Share on other sites
Machine Elf Posted February 24, 2004 Okay, thanks for the heads-up Torsten. Good luck with it all, and look forward to seeing the extract! Belfy Share this post Link to post Share on other sites
