N&PD Moderators: Skorpio | thegreenhand
Philip Seaman reported that ketamine and PCP bind to D2 but no other labs have ever been able to replicate his findings.
I can't seem to find any studies about how NMDA antagonism leads to seizures (maybe Serotonin2A can enlighten us) but the other day I did find this study that would make me think twice about using NMDA antagonists long term http://www.ncbi.nlm.nih.gov/pmc/articles/PMC3856160/
After chronic of administration of ketamine to rats, there is a shift to proconvulsant effects, suggesting it may induce kindling:http://www.ncbi.nlm.nih.gov/pubmed/4674053
The glutamate system is very fast in adjusting.
Am very interested in these kappa agonists though. Would be so great if we had the possibility for a whole new generation of dissociatives..
Sophora flavescens, the shrubby sophora, is a species of plant in the genus Sophora a genus of the Fabaceae family, that contains about 52 species, nineteen varieties, and seven forms that are widely distributed in Asia, Oceanica, and the Pacific islands.About fifteen species in this genus have a long history of use in traditional Chinese medicines. The root is known as Ku shen. is a typical traditional Chinese medicine.
Oxymatrine (matrine oxide, matrine N-oxide, matrine 1-oxide) is one of many quinolizidine alkaloid compounds extracted from the root of Sophora flavescens, a Chinese herb. It is very similar in structure to matrine, which has one less oxygen atom. Oxymatrine has a variety of effects in vitro and in animal models, including protection against apoptosis, tumor and fibrotic tissue development, and inflammation. Furthermore, oxymatrine has been shown to decrease cardiac ischemia (decreased blood perfusion), myocardial injury, arrhythmias (irregular heartbeats), and improve heart failure by increasing cardiac function.
You can calculate the dose using allometric scaling. Note, however, that there can be pharmacokinetic and pharmacodynamic species differences that make allometric scaling inaccurate for some drugs.
For the less mathematically inclined can you say whether 10:1 ratio is an even somewhat accurate estimate from rats to humans?