22-01-2009, 19:47
|
 |
0utrider
is is singing in the rain
|
|
Join Date: 06-06-2007
Location: here and there...
Posts: 1,383
|
|
|
Re: opiate Research Chemicals?
possibly not atual opioid RCs, but rather working like kratom (i.e. different group, same receptors=similar effects)
these are said to be both available and cheap as well as tested Nigella sativa
Quote:
Title of Thesis
ROLE OF NIGELLA SATIVA IN OPIOID DEPENDENCE
Keywords (Extracted from title, table of contents and abstract of thesis)
nigella sativa, opioid dependence, detoxification, hyper-tension, arrhythmias, ischaemic heart disease, calcium channel blockers,
Abstract
Opioid dependence is a chronic disorder that produces changes in brain pathways that remain long after the patient stops taking the drug. These protracted brain changes put the dependent person at greater risk of relapse. Detoxification can be successful in cleansing the person of drugs and withdrawal symptoms; it does not address the underlying disorder, and thus is not the adequate treatment. Maintenance with methadone or naltrexone is the usual practice in the long-term management of opioid dependence but both drugs have their own disadvantages because no single medication is appropriate for every individual for treating their opioid dependence, it is important that clinicians have a variety of the therapeutic agents available to them.
Calcium channel blockers, such as verapamil, diltiazem, nifedipine, nimodipine, and felodipine are useful drugs being used in cardiovascular disorders, such as hyper-tension, arrhythmias, and ischaemic heart disease. Research on calcium channel blockers has proved their therapeutic potential in a variety of disorders such as asthma, diarrhoea, premature labour, and diseases of central nervous system such as epilepsy, and opioid dependence. Modern drugs are not only expensive and beyond the reach of majority of the population of world but also have multiple side effects. Hence there is a need to explore such drugs from indigenous sources and to observe if combination of desired therapeutic efficacy exists in nature.
Nigella Sativa is in use for the treatment of variety of ailments since ancient times. Research has based its many effects on their efficacy of blocking calcium channels. As calcium channels have been tried for the treatment of opioid dependence, so Nigella Sativa was used in this study. This study was carried out on 50 patients who were divided into two groups. Patients were admitted for 12 days and then weekly followed up for 12 weeks.
Each patient received placebo orally during day-1 and day-2 of admission. Thereafter Nigella Sativa was given to the patients from day-3 of admission to eighth week. Then the dose of each drug was tapered off during 9th and 10th weeks and then no treatment was given during last two weeks.
It was observed that Nigella Sativa showed a rapid improvement in signs and symptoms of acute opioid abstinence. It was also observed that Nigella Sativa prevented the development of significant craving and relapse. It is concluded that Nigella Sativa is effective in long term management of opioid dependence and it is suggested that further long term follow up studies may be designed with greater number of patients.
|
similar to what kratom was said to be
as well as Picrilima nitida
Quote:
the major compound is reported of having agonist / antagonist activity
"akuammine also showed highest affinity for mu-opioid binding sites (Ki 0.5 microM) but was an antagonist at mu-opioid receptors with a pK(B) of 5.7 against the selective mu-opioid receptor agonist"
I would caution people to think about the possibility that certian people might have dysphoric reaction to certian opioid compounds....also people who are using opiates daily, especially methadone or buprenorphine should consider being careful with mixed agonist/antagonist type compounds.
I have taken other compounds known to have agonist activity, and had primarily dysphoriic effects...and these were reported mu agonists...in the plant dalea purpurea..
I have hoped that someone would eventually get to seperating the alkaloids of this picralima nitida plant.
what I am interested in finding out, and have sent in questions to one supplier, is if the primarily kappa opioid agonist in this blend of alkaloids
akuammicine...has been taken out of the blend.
"Akuammicine has the highest affinity for kappa-opioid binding sites (Ki 0.2 microM) and was a full agonist at kappa-opioid receptors in the guinea pig ileum preparation but a partial kappa-opioid receptor agonist in the vasa deferentia of the mouse and the rabbit."
perhaps this kappa agonist compound was negating some of the mu potency.
if so, I would be real interested to have that fraction of the isolation that contains the akuammicine. even a kappa agonist has potential!
as well, I think further seperation of primarily the compound Akuammidine
might be interesting. a compound with delta and kappa activity as well as mu activity might have potential for less tolerance building effects...that is just my uninformed opinion....
"Akuammidine showed a preference for mu-opioid binding sites with Ki values of 0.6, 2.4 and 8.6 microM at mu-, delta- and kappa-opioid binding sites, respectively. The agonist actions of akuammidine in the mouse-isolated vas deferens were antagonised by naloxone and the mu-opioid receptor selective antagonist D-Phe-Cys-Tyr-D-Trp-Orn-Thr-Pen-Thr-NH2 (CTOP) confirming an action at mu-opioid receptors. "
even though I am broke as hell. I decided to order a small amount of this material.
I have definitely paid my dues with this plants seeds.
consuming over 20 grams of the raw ground seed is an experience that I will never face again...unless stranded in africa with nothing but picralima seeds for relief.
people interested in picralima nitida might also be interested in
similiarly opioid active compounds that occur in smaller amounts in the tabernaemontana pachysiphon and t. holstii plants.
I have two nice specimen of t. holstii that I am hoping to culture into cuttings this spring.
taberaemontana pachysiphon is commercially avialable. I tried that plant in raw leaf form. and got no toxic effects...but also no psychoactivity.
a chemist extracted alkaloids for me..but the yeild is much less than the picralima seeds.
still an interesting couple of plants.
also of interest in trachelopspermum jasminoides
"The leaves and stems of T. JASMINOIDES have been found to contain indole alkaloids. Five indole alkaloids, coronaridine, voacangine, apparicine, conoflorine, and 19-epi-voacangarine have been isolated. The (13)C-NMR spectra of apparicine and 19-epi-voacangarine are also reported."
there was a website that had some personal reports on using this chinese medicinal to support an opiate ween program. apparently small amounts were taken for weeks at a time, while weening down.
I have taken the plants extracts in the suggested doses, and had no negative effects. but I didnt push the dose up to increase any effects. and I didnt take this for more than a day at a time.
this recent picralima nitida extract with augmented levels of alkaloid %'s could be an important discovery for especially people in africa. if the product can be made over there for cheap. these seeds are not too expensive. if the analgesic activity can be increased, and lower side effects, this formula could boost the potential.
if this augmentation of alkaloid balance doesnt mess with this plants anti malarial benefits...that would be even better.
it interesting to me that cats claw, kratom and other mitragyna species, and this picralima nitida plant all have potential for research into treating malaria.
having two benefits of pain relief and anti malarial support in the bush is a good thing.
|
yet it seems in the right dosage to have similar to opioid effects
|
Similar Threads
-agonist effects. The peripherally selective antagonist quaternary naltrexone (1 mg/kg, s.c.) caused approximately 70% reduction in the peak effect of herkinorin (0.32 mg/kg) in females, indicating this effect of herkinorin is prominently mediated outside the blood-brain barrier.
Hybrid Mode
