Trying to stay sane despite rapid advances in scientific understanding and technology!

Monday, June 10, 2013

Ketamine and ketamines "cousin" GLYX-13 = suitable candidates for countering acute suicidality in affective disorders



Keatmines “cousin” [GLYX-13] rapidly lifts depression without side effects:
“Human clinical studies demonstrated that ketamine can ward off major and bipolar depressive symptoms within 2 hours of administration and last for several days. Ketamine is fraught with serious side effects including excessive sleepiness, hallucinations, and substance abuse behavior.”
"Our drug, GLYX-13, is very different. It does not block the receptor ion channel, which may account for why it doesn't have the same side effects."


“Previous electrophysiological and conditioning studies had suggested that GLYX-13, unlike ketamine, enhanced memory and learning in rats, particularly in the brain's memory hub or hippocampus. GLYX-13 also produced analgesic effects.”

“GLYX-13 and ketamine produced rapid acting (1 hour) and long-lasting (24 hour) antidepressant-like effects in the rats. Fluoxetine, an SSRI that typically takes from 2-4 weeks to show efficacy in humans, did not produce a rapid antidepressant effect in this study.”

“These results are consistent with data from a recent Phase 2 clinical trial, in which a single administration of GLYX-13 produced statistically significant reductions in depression scores in patients who had failed treatment with current antidepressants. The reductions were evident within 24 hours and persisted for an average of 7 days. After a single dose of GLYX-13, the drug's antidepressant efficacy nearly doubled that seen with most conventional antidepressants after 4-6 weeks of dosing. GLYX-13 was well tolerated and it did not produce any of the schizophrenia-like effects associated with other NMDA receptor modulating agents.”

“Moskal speculates that GLYX-13 either directly binds to the glycine site on the NMDA receptor or indirectly modulates how glycine works with the receptor. Resulting activation of more NMDA and AMPA receptors leads to an increase in memory, learning -- and antidepressant effects. By contrast, ketamine only blocks the NMDA receptor, but also increases the activity of the AMPA receptor. Knowledge of these mechanisms could lead to the development of more effective antidepressants.”
This reminds me of how SSRI’s are speculated to possibly work through their effects on increasing brain derived neuro factor (BDNF) which may in turn make one hypersusceptible to new learning, in turn allowing someone in a rut to quickly learn a way out of it…

People are always suprised when I say Ketamine, horse tranquiliser, or special K as it is known in drug circles has beneficial properties. It was also shown in another study to have neuroregenerative effects:
http://www.sciencedaily.com/releases/2012/10/121004141747.htm
"In their research, Duman and others show that in a series of steps ketamine triggers release of neurotransmitter glutamate, which in turn stimulates growth of synapses. Research at Yale has shown that damage of these synaptic connections caused by chronic stress is rapidly reversed by a single dose of ketamine."

Though I've never used it, so I can't attest to this personally, but i'm all for the open study of drugs and there effects, both positive and negative.

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