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Dissociatives The Little & Dandy MK-801 Thread

emjay said:
Interesting. DXM more than anything else makes me feel absolutely refreshed the next morning and is almost guaranteed to leave me in a great mood.
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When I first started using DXM it was the same with me, where the morning after I would feel incredible, alert, and alive. But now, it makes me feel incredibly tired, lathargic, and somewhat ill. Oddly enough I still enjoy the day after and I also tie it to the trip experience, but sometimes it's too unpleasant for me to enjoy. Ketamine makes me feel great the next morning if I do it late at night before I go to sleep which I find interesting, but otherwise I don't notice any after effects. I've never done PCP, but I'm curious what the day after effects are.
 
im assuming mk-801 is no longer on the market, because all of the reports on this substance date back at least two years if not three or four. one thing about the substance (that really should not be underestimated) is the reports on it are fantastic, there is something to be said for any drug which provokes the user to write really engagingly about it effects.
this is the sort of thing i would like to have and file away so if forty years down the road things arent going to well, i will have the freedom to exparament with drugs which are likely to damage my brain. at this moment in time i could not take that risk.
 
emjay said:
Interesting. DXM more than anything else makes me feel absolutely refreshed the next morning and is almost guaranteed to leave me in a great mood.
Click to expand...

YEAH! I wake up with this great body high and I just feel nice and... well, the best word for it is JUICY!

egor, touché.


MK-801 is one of the weirder drugs out there. All the telepathy talk makes me think it may have some serious delusion-inducing properties.
 
It seems that to be enjoyable there needs to be a certain level of dopaminergic activity. Too little and it's like MK-801, too much and it's like tiletamine (the 2-thienyl group as the aromatic ring increses dopaminergic activity).

Personally I found PCP to have too much of a dopaminergic edge as I had muscle tension leading to pain for a couple of days after trying PCP (enough so I'd not consider trying it again)

MK-801 is one of the weirder drugs out there. All the telepathy talk makes me think it may have some serious delusion-inducing properties.
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That's putting it mildly! =D
 
Ever since the first time I found out that DXM was an OTC dissassociative I became very interested in them. I've probably tripped on DXM well over 20 times, and the amazing thing is, I believe that I am completely deficient in the enzyme that metabolizes it.

Ingesting DXM was at least a 48 hour endeavor, even with small doses. I believe that my body didn't produce any noticable levels of DXO because I never got any strong "stoning" or "flanging" effects from it, it just gave me the strangest buzz. I'm sure my DXM trips were very much unlike the average trip, as DXM itself has high affinity for sigma receptors, but low affinity for NMDA receptors. DXO seems to be responsible for most of the dissassociating effects. Another odd thing is that I've never been able to sleep on DXM, not now and not ever. A lot of people seem to get groggy from it, probably a result of DXO.

Low doses (100 - 250mg range) would result in an energetic, stimulating, and of course, long lasting high. I'd be extremely talkative and have a lot of muscle tension, very strange gait. No visual effect though.

At medium doses, several other effects would become evident. 354mg would not give me disassociation, but it would give me a strange visual effects in the dark. Objects looked like they were darting back and forth, shrinking around. But as I upped the dosage, the stimulating effects would become very strange and occasionally were profoundly unpleasant.

500mg and upwards gave me very engaging closed eye visuals, but I still was very anchored to reality. I'd close my eyes and suddenly, holy shit, I'd see my body laying out in front of me. Then I started floating from scene to scene, places I'd been before and others it seemed I made up. It was so strange, I was laying in bed and behind my closed eyes I was laying down on my friends floor in his house watching people walk by me. I would always pop my eyes back open and flip out with excitement after experiencing that.

I assume that I was still able to get some dissassociation from higher doses because DXM binds somewhat weakly there, so high doses would start to give me some NMDA blockage.

Unfortunately, my trips began to get more and more uncomfortable, it seems that DXM by itself is very rough on the body and it's effects have changed considerably. I used to enjoy the bizarre effects, but now it just makes me feel like I want to die anytime I take it, even tiny doses. So DXM gave me a taste of dissassociatives, but I've never had a chance to try ketamine, pcp, etc. I often wonder what a straight DXO trip would be like for me, probably nothing like the trip I'm used to.
 
Eventually one "loses the magic" with dextromethorphan after extended and/or frequent use. The only solution seems to be taking a long (and I mean long, at least 6 months) break before being reunited with it.
 
Mk-801

Since there seems to be a resurgance in interest in MK-801, we need a place to consolidate the small ammount of info available on it. I've been curious about this one for a long time, but the rumored temporary changes in brain structure (vacuoles) have at least for me shelved it for the time being; at least until more definitive info on its pharmacology is published. Heres a start>

Erowid trip reports> http://www.erowid.org/experiences/subs/exp_Dizocilpine.shtml

IUPAC> (+)-5-methyl-10,11- dihydro-5H-dibenzo[a,d] cyclohepten-5,10-imine maleate

A few pubmed links>
http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"RATIONALE: Non-competitive NMDA receptor antagonists markedly increase neuronal activity in medial prefrontal cortex (mPFC), an effect which partly underlies their schizomimetic actions. Projection pyramidal neurons and local GABAergic interneurons in mPFC express 5-HT(1A) receptors, whose activation modulates dopaminergic (DA) and serotonergic (5-HT) activity in midbrain and the cortical release of both monoamines. OBJECTIVE: To examine whether the presence of 5-HT(1A) receptors can modulate the effect of NMDA receptor blockade with MK-801 (dizocilpine) on DA and 5-HT release in mouse mPFC. MATERIALS AND METHODS: Brain microdialysis and locomotor activity measures in wild-type and 5-HT(1A) receptor knockout mice. RESULTS: Systemic MK-801 administration (0.125, 0.25, 0.50, and 1 mg/kg i.p.) induced a dose-dependent increase in mPFC 5-HT output, which was independent of the genotype. MK-801 increased DA output in a dose-dependent manner with a significant effect of genotype on low doses (0.125, 0.25 mg/kg). These differences were not paralleled by differences in gross locomotor activity. Overall, MK-801 increased more markedly DA than 5-HT output in both genotypes. Finally, the local perfusion of MK-801 in mPFC (30, 100, 300 muM) by reverse dialysis did not elevate dialysate DA or 5-HT concentrations in mPFC. CONCLUSION: 5-HT(1A) receptors partly modulate the increase in mPFC DA (but not 5-HT) release produced by NMDA receptor blockade. The lack of effect observed after the local MK-801 application suggests that the change in cortical monoamines is mainly driven by subcortical NMDA receptor blockade, without a significant involvement of PFC 5-HT(1A) receptors."

http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"Background: The glutamate system plays a major role in mediating EtOH's effects on brain and behavior, and is implicated in the pathophysiology of alcohol-related disorders. N-methyl-D-aspartate receptor (NMDAR) antagonists such as MK-801 (dizocilpine) interact with EtOH at the behavioral level, but the molecular basis of this interaction is unclear. Methods: We first characterized the effects of MK-801 treatment on responses to the ataxic (accelerating rotarod), hypothermic and sedative/hypnotic effects of acute EtOH administration in C57BL/6J and 129/SvImJ inbred mice. Effects of another NMDAR antagonist, phencyclidine, on EtOH-induced sedation/hypnosis were also assessed. Gene knockout of the NMDAR subunit NR2A or l-alpha-amino-3-hydroxy-5-methylisoxazole-4-propionate GluR1 or pharmacological antagonism of the NMDAR subunit NR2B (via Ro 25-6981) was employed to examine whether inactivating any one of these glutamate signaling molecules modified MK-801's effect on EtOH-related behaviors. Results: MK-801 markedly potentiated the ataxic effects of 1.75 g/kg EtOH and the sedative/hypnotic effects of 3.0 g/kg EtOH, but not the hypothermic effects of 3.0 g/kg EtOH, in C57BL/6J and 129/SvImJ mice. Phencyclidine potentiated EtOH-induced sedation/hypnosis in both inbred strains. Neither NR2A nor GluR1 KO significantly altered basal EtOH-induced ataxia, hypothermia, or sedation/hypnosis. Ro 25-6981 modestly increased EtOH-induced sedation/hypnosis. The ability of MK-801 to potentiate EtOH-induced ataxia and sedation/hypnosis was unaffected by GluR1 KO or NR2B antagonism. NR2A KO partially reduced MK-801 + EtOH-induced sedation/hypnosis, but not ataxia or hypothermia. Conclusions: Data confirm a robust and response-specific potentiating effect of MK-801 on sensitivity to EtOH's intoxicating effects. Inactivation of three major components of glutamate signaling had no or only partial impact on the ability of MK-801 to potentiate behavioral sensitivity to EtOH. Further work to elucidate the mechanisms underlying NMDAR x EtOH interactions could ultimately provide novel insight into the role of NMDARs in alcoholism and its treatment."

http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"The non-competitive NMDA receptor antagonist MK-801 elicits a behavioural syndrome in rodents characterized by hyperlocomotion and stereotypies, which is antagonized by antipsychotic drugs. NMDA receptor antagonists increase prefrontal cortex (PFC) activity in rodents, as assessed by electrophysiological and neurochemical measures. The increase in glutamate outflow induced by systemic MK-801 administration in the medial PFC (mPFC) is prevented by the local administration of clozapine (Clz). In the present study, we examine whether a PFC lesion alters the behavioural syndrome induced by MK-801 in rats and the Clz-induced antagonism of MK-801 actions. We evaluated the hyperlocomotion, stereotypies and other behavioural changes induced by MK-801 in the open field and the effect of electrolytic lesions of the mPFC, and of cortical transection on the behavioural syndrome induced by MK-801 and its reversal by Clz. MK-801 (0.1-0.2 mg/kg i.p.) reduced rearings but only the higher dose induced hyperlocomotion. At this dose, MK-801 also increased disorganized movements, head weavings, and induced ataxia signs. An electrolytic lesion of the mPFC markedly reduced the number of rearings pre-treatment but caused a very slight attenuation of MK-801-induced hyperlocomotion. Cortical transection did not significantly alter MK-801 effects. Clz administration (1 mg/kg s.c.) significantly attenuated hyperlocomotion, head weavings and ataxia signs induced by MK-801 but did not prevent the decrease in rearings. The effect of Clz was essentially unaffected by electrolytic lesions of the mPFC. These results show that MK-801-induced motor syndrome and its reversal by Clz are mostly independent on PFC integrity."

http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"There are experimental evidences indicating that the non-competitive NMDA receptor antagonist MK-801 impairs cognition and produces a series of schizophrenia-like symptoms in rodents (hypermotility, stereotypies and ataxia). The present study was designed to investigate the efficacy of the selective 5-HT(6) receptor antagonist Ro 04-6790 in counteracting these MK-801-induced behavioural effects in the rat. The effects of Ro 04-6790 in antagonizing MK-801-induced memory deficits were assessed using the object recognition task. The ability of this 5-HT(6) receptor antagonist in counteracting hypermotility, stereotypies and ataxia produced by MK-801 were evaluated in a motor activity cage. Post-training administration of Ro 04-6790 (10 and to some extent also 3mg/kg) antagonized MK-801-induced performance deficits in a recognition memory test. In a subsequent study, Ro 04-6790 (3 and 10 mg/kg) reversed hypermotility and ataxia produced by MK-801. This 5-HT(6) receptor antagonist also alleviated MK-801-induced certain stereotypies. Our findings indicate that Ro 04-6790 attenuates behavioural effects related to the hypofunction of the NMDA receptor suggesting that this compound might be involved in the psychotomimetic effects of non-competitive NMDA receptor antagonists."

http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"We analysed acute and long-term effects of the N-methyl-d-aspartate receptor antagonist MK-801 on long-term heterosynaptic population spike depression (LTHPSD) evoked by high-frequency stimulation of the direct cortical input in female rat hippocampal slices to understand disturbances in cognitive functions associated with an acute phencyclidine-induced psychosis. High-frequency stimulation (HFS) of the direct cortical input (dCI) to cornu ammonis area 1 (CA1) induced homosynaptic long-term potentiation (LTP) while simultaneously evoking LTHPSD at the Schaffer collateral input. Animals treated with a single intraperitoneal application of MK-801 (5 mg/kg body weight) showed severe behavioural alterations for 24 h, although histological examination of CA1 did not reveal any morphological changes. However, after application of MK-801, homosynaptic LTP of the dCI was suppressed for up to 7 days and recovered within 4 weeks. Likewise, LTHPSD in response to HFS of the dCI to CA1 was abolished for at least 1 week post-treatment, with partial recovery occurring after 4 weeks. Homosynaptic LTP, induced by HFS of Schaffer collaterals, was also disturbed for at least 24 h, with recovery after 7 days. Remarkably, bath application of MK-801 (50 microM) converted LTHPSD, induced by dCI HFS, into persistent heterosynaptic long-term enhancement of stratum radiatum-evoked responses. The acute effects of MK-801 on synaptic plasticity seen in this study may contribute to the observed severe behavioural alterations and long-term effects and may explain some of the long-lasting symptoms remaining after an acute psychotic episode in humans."

http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"Hypoxic exposure produces a consistent decrease of rectal temperature (Tb), which is recognized as a potent protective response. While some of the neural mechanisms underlying this response have recently been described, it remains poorly known how these mechanisms evolve during post-natal development. We recently reported that in rat pups NMDA glutamate receptor limits Tb drop upon hypoxic exposure, an effect that has not been reported by others in adult rats. Accordingly, we tested the hypothesis that the implication of NMDA receptors on temperature control during hypoxic exposure evolves during development. To this aim, we evaluated the hypoxic (30 min - 12% O(2)) responses of Tb, metabolic rate, and ventilation in rats after injection of vehicle, or the NMDA receptor antagonist MK-801, at different ages (post-natal days 4, 10, 20 and 2-3 month-old - P4, P10, P20 and P60). MK-801 amplified the magnitude of the hypoxic-induced Tb drop in P4, P10 and P20 rats, but this effect was not apparent in adults. In P20 rats MK-801 tripled the hypoxic induced Tb drop, which was 0.5 degrees C in control and 1.4 degrees C in treated rats (p<0.0001). This effect was specific to temperature regulation, and was not accompanied by similar changes of other recorded parameters. MK-801 induced a significant decrease of the hypoxic ventilatory response in adults only. We conclude that NMDA glutamate receptor acts as a counter-regulatory factor that limits the hypoxic-induced drop of rectal temperature during post-natal development in rats."





More to come.
Discuss:)
 
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More mk-801 abstracts>
http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"Schizophrenia is mostly a progressive psychiatric illness. Although cognitive changes in chronic schizophrenia have been investigated, little is known about the consequences of a single psychotic episode on memory mechanisms and formation. We investigated changes in hippocampal long-term potentiation (LTP) and spatial memory in a rat model of an acute psychotic episode. Application of NMDA receptor antagonists, such as MK801 (dizolcilpine) in rats, have been shown to give rise to an acute and short-lasting behavioral state, which mirrors many symptoms of schizophrenia. Furthermore, NMDA antagonist-intake in humans elicits symptoms of schizophrenia such as hallucinations, delusions, and affective blunting. We therefore treated animals with a single systemic injection of MK801 (5 mg/kg). Increased stereotypy, locomotion, and ataxia were evident immediately after MK801-treatment, with effects disappearing within 24 h. MK801-treatment caused a disruption of prepulse inhibition of the acoustic startle reflex, 1 day but not 7 or 28 days after treatment. These effects were consistent with the occurrence of an acute psychotic episode. LTP was profoundly impaired in freely moving rats 7 days after MK801 application. Four weeks after treatment, a slight recovery of LTP was seen, however marked deficits in long-term spatial memory were evident. These data suggest that treatment with MK801 to generate an acute psychotic episode in rats, gives rise to grave disturbances in synaptic plasticity and is associated with lasting impairments with the ability to form spatial memory. (c) 2007 Wiley-Liss, Inc."

http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"Over-stimulation of NMDA receptors (NMDARs) is involved in many neurodegenerative disorders. Thus, developing safe NMDAR antagonists is of high therapeutic interest. GK11 is a high affinity uncompetitive NMDAR antagonist with low intrinsic neurotoxicity, shown to be promising for treating CNS trauma. In the present study, we investigated the molecular basis of its interaction with NMDARs and compared this with the reference molecule MK801. We show, on primary cultures of hippocampal neurons, that GK11 exhibits neuroprotection properties similar to those of MK801, but in contrast with MK801, GK11 is not toxic to neurons. Using patch-clamp techniques, we also show that on NR1a/NR2B receptors, GK11 totally blocks the NMDA-mediated currents but has a six-fold lower IC(50) than MK801. On NR1a/NR2A receptors, it displays similar affinity but fails to totally prevent the currents. As NR2A is preferentially localized at synapses and NR2B at extrasynaptic sites, we investigated, using calcium imaging and patch-clamp approaches, the effects of GK11 on either synaptic or extrasynaptic NMDA-mediated responses. Here we demonstrate that in contrast with MK801, GK11 better preserve the synaptic NMDA-mediated currents. Our study supports that the selectivity of GK11 for NR2B containing receptors accounts contributes, at least partially, for its safer pharmacological profile.
"

http://www.ncbi.nlm.nih.gov/pubmed/...ez.Pubmed.Pubmed_ResultsPanel.Pubmed_RVDocSum
"Previous research has established that dopamine signals are crucial in orienting behavior to reward. Less is known, however, about the psychopharmacology of task performance under small-reward conditions as compared to large-reward conditions. The current study examined the effects of the noncompetitive N-methyl-D-aspartate (NMDA)-receptor antagonist dizocilpine (MK-801) on reaction time (RT) in a nose-poke task with rats completing an asymmetric reward schedule. In all trials, the rats were required to poke their nose in either the left or the right peripheral hole immediately adjacent to the centre hole when the corresponding light was illuminated. Depending on the stimulus-reward mapping, however, one position was associated with a large reward, while the alternative position was associated with a small reward. Correct performance was required in every trial; if the rat did not make a correct response within 20 s, the trial was aborted, and the same stimulus was presented again on the next trial. In this way, the rat was forced to perform the same visuo-spatial discrimination task under different reward conditions. Reaction times (ms) were faster for large-reward trials than for small-reward trials, replicating previous findings. At a dosage of MK-801 (0.04 mg/kg), there was no significant influence of on RT in large-reward trials. In contrast, the same dosage of MK-801 in small-reward trials produced a decrease in RT as compared to the control condition, implying an improvement of performance. Below 0.04 mg/kg of MK-801, a steady decrease of RT in small-trials was seen as a function of dosage. Above 0.04 mg/kg of MK-801, the majority of rats failed to perform the task at all, whereas the rats that did manage to perform the criterion of 80 correct trials in a session showed no difference in RT between large- and small-reward trials. These data indicate that the systemic administration of a relatively small dosage of MK-801 facilitates performance when reward is small. It is suggested that the facilitation may be due to the reinforcement of mechanisms that work in opposition to response bias. As a corollary, the study provides a useful paradigm to study the voluntary control of unavoidable action."
 
^ I will get these on the front page of this thread when I figure out a good way to do it ;)
 
Has anyone seen this around recently? I've heard rumors that it is out there...somewhere. I must admit that I've always been interested in this one. From the few reports about it that I've read it sounds like the DPT of dissos. I don't know why I find these oddball substances so interesting but I'll jump at the chance to take this if and when it makes it way to me. I had a chance to buy it once and passed on it because I hadn't gotten into dissos at that time, was really young, and back then the only information on it was related to lab animals. Now that more human reports have come in I'm more and more interested in adding it to my collection.

Is anyone here sitting on some by chance? Not attempting to source just curious if it's in the wild still. The only person I know personally that would have such a thing has never been able to source it himself. He has a large collection of rare things just sitting around so I figure if he doesn't have it then no one outside of proper labs doing studies currently does.

If I do ever come across it I'll make sure to write a proper trip report. I've recently found a proper sitter/someone that enjoys rare substances as much as me and we plan on taking turns and writing reports from both prescriptives. Given the nature of something like MK-801 I think that'd be the proper way to document it. It seems to cause massive loss of memory once a hole state is obtained.
 
Shadowmeister said:
I'm also insanely curious about this one. There are a handful of reports of people claiming it's immensely profound and beautiful. And others where it sounds kinda creepy.
Click to expand...

Yea, the mix of reports is very odd. I'm wondering if people are testing slightly different compounds similar to how Ket feels different depending on which type you get. The creepy sounding reports do not strike me as that bad honestly. I've mainly heard of folks seeing dark entities (shadow people) which doesn't sound too horrible. The positive reports seem to be more common than the bad ones but since they are so few reports it's hard to tell what experience is the most common. I've wondered if the creepy reports were just bad trips associated with taking something so unknown.

Are there any reports aside from the one here and the few on erowid? I haven't seen a new one in many years.
 
There are actually a good few on Bluelight now, and more on Erowid too. Using the new Trip Reports tagging system I've been working on (for years 8(), here is a link to all MK-801 reports on Bluelight.

By the way I generated it using the search engine beta version I created, check it out: http://9931080.byethost5.com/searchEngine.html. Probably some bugs still, it's just a simple javascript/HTML thing. Interested in your feedback/testing. I'm hand-tagging about 100 reports a day with a tagging tool I made that makes it point-and-click instead of copy/pasting a bunch of code. 2018 is done, 2017 is mostly done, and 2009 is done, all the other years still need to be tagged. My goal is to make the TR forum a resource to rival Erowid, with the added benefits of no wait til to publish a report, and being able to discuss with people.
 
Hey thanks man, I gotta run for a bit but I'll check that out when I return. I see a couple in there that I haven't read yet. I'll let you know if I find anything in the search engine that needs your attention. The tagging system will be very helpful once you get it up and running 100%. I know it's a thankless job sometimes but I do appreciate it.
 
Xorkoth that link to reports list doesnt work anymore i tried using regular site search but i kept getting issue like mk , 801 too common terms.

I remember reading about this stuff many years ago and getting super excited, i didnt even see that it was submiligram!! I did see somewhere some BS that it will cause blindness yeah right.
I frickin really want to try this if i ever got the chance!!
 
Ah yeah we upgraded site software. Check this thread for an updated list of links to tagged projects in Trip Reports... this does not mean it is every single report, as they must have been manually tagged. However we are working on a way to automate the tagging of reports and get that project back up and running.

⫸STICKY⫷ - The Trip Reports Directory

The Trip Reports Directory Dynamic Link Database **NOTE** This thread's links only return manually tagged reports. Currently we have 3 out of 21 years of back-logged reports tagged, plus most of 2020 and some of 2021 To use a custom search engine that lets you enter a search term and return...
www.bluelight.org www.bluelight.org

I clicked the MK801 link and only got one report, sadly.
 
I appreciate it thank you!
I'd love to see an accessible version of this! I wonder if it could maintain it's potency with a substitution somewhere...
Gosh it sounds fun it sounds economical!
 
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