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Dissociatives

Dissociatives are a category of hallucinogens which cause sensory deprivation, by reducing signals from certain parts of the brain (usually external stimuli) to the conscious mind.

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[top]Introduction to Dissociatives

Dissociative drugs are a category of hallucinogens which cause sensory deprivation, by reducing signals from certain parts of the brain (usually external stimuli) to the conscious mind. This usually means that a person under the influence of a dissociative has less connection to reality, sometimes completely losing this connection. The reduction of external stimuli can result in dream-like states, hallucinations, altered cognition and sometimes complete separation from reality and the own body (dissociation).

Most typical dissociatives (DXM, ketamine, PCP) are NMDA (N-methyl-D-aspartate) receptor antagonists, but their mechanism of action is usually more complex. Some dissociatives are also sigma-opioid and kappa-opioid agonists (PCP, salvinorin) and GABA (benzodiazepine receptor) agonists (muscimol).

Quote:
NMDA receptor antagonists are a class of anesthetics that work to antagonize, or inhibit the action of, the N-methyl d-aspartate receptor (NMDAR). They are used as anesthesia for animals and, less commonly, for humans; the state of anesthesia they induce is referred to as dissociative anesthesia. There is evidence that NMDA receptor antagonists can cause a certain type of neurotoxicity or brain damage referred to as Olney's Lesions in rodents, though such damage has never been observed in primates like humans.

Some NMDA receptor antagonists, including ketamine (K), dextromethorphan (DXM), phencyclidine (PCP), and nitrous oxide (N2O) are popular as recreational drugs for their dissociative, hallucinogenic, and/or euphoriant properties. When used recreationally, they are classified as dissociative drugs. Because some users use them for spiritual reasons, these recreational NMDA receptor antagonists are sometimes considered to be entheogens.

The NMDA receptor is an ionotropic receptor that allows for the transfer of electrical signals between neurons in the brain and in the spinal column. For electrical signals to pass, the NMDA receptor must be open. To remain open, an NMDA receptor must bind to glutamate and to glycine. An NMDA receptor that is bound to glycine and glutamate and has an open ion channel is called "activated."

Chemicals that deactivate the NMDA receptor are called antagonists. NMDAR antagonists fall into four categories: competitive antagonists, which bind to and block the binding site of the neurotransmitter glutamate; glycine antagonists, which bind to and block the glycine site; noncompetitive antagonists, which inhibit NMDARs by binding to allosteric sites; and uncompetitive antagonists, which block the ion channel by binding to a site within it. [source: Wikipedia]
Dissociatives differ from other hallucinogens by being much more intoxicating and producing more separation from reality than psychedelics, yet not causing delirium (total separation from reality, the user not being capable of separating hallucinations from reality) and anticholinergic side effects like deliriants do.

[top]Using Dissociatives

[top]Ways of administration

[top]Effects of Dissociatives

[top]Combinations with Dissociatives

[top]Different Uses for Dissociatives

[top]The dangers of Dissociatives

[top]Most Popular Forms of Dissociatives

[top]Other Dissociatives


Diethyl ether: once used as a general anaesthetic. Swiss physician and alchemist Theophrastus Bombastus von Hohenheim, better known as Paracelsus first discovers the hypnotic effects of ether in XVIth century.

Ethyl chloride (monochloroethane, chloroethane): a dissociative anaesthetic similar in actions and effects to diethyl ether and nitrous oxide. Extremely flammable hence same safety protocols as for diethyl ether are required.

Eticyclidine (PCE, CI-400): a dissociative anaesthetic drug in effects similar to phencyclidine, slightly more potent but its unpleasant taste and tendency to cause nausea made it less accepted by users. PCE was developed by Parke-Davis in the 1970s and evaluated for anaesthetic potential under the code name CI-400, but research into PCE was not continued after the development of ketamine, a similar drug with more favourable properties. PCE is slightly more potent than PCP and has similar effects. (source: Wikipedia)

Rolicyclidine (PCPy): a dissociative anaesthetic drug with sedative effects. It is similar in effects to phencyclidine but is slightly less potent and has less stimulant effects instead producing a sedative effect described as being somewhat similar to a barbiturate, but with additional PCP-like dissociative, anaesthetic and hallucinogenic effects. (source: Wikipedia)

Tenocyclidine (TCP): a dissociative anaesthetic drug with stimulant effects. It is similar in effects to phencyclidine (PCP) but is considerably more potent with more affinity for the NMDA receptors but less affinity for the sigma receptors. TCP acts primarily as an NMDA receptor antagonist which blocks the activity of the NMDA receptor, however its increased stimulant effects compared to PCP suggests it also has relatively greater activity as a dopamine reuptake inhibitor (DRI). (source: Wikipedia)

Tiletamine: a dissociative anaesthetic pharmacologically classified as an NMDA receptor antagonist, related chemically and pharmacologically to ketamine and phencyclidine. (source: Wikipedia)

Memantine: the first in a novel class of Alzheimer's disease medications acting on the glutamatergic system by blocking NMDA glutamate receptors. Memantine acts as a non-competitive antagonist at the 5HT3 receptor, with a potency similar to that for the NMDA receptor. Memantine acts as a non-competitive antagonist at different neuronal nicotinic acetylcholine receptors (nAChRs) at potencies possibly similar to the NMDA and 5-HT3 receptors. Memantine acts as an agonist at the dopamine D2 receptor. (source: Wikipedia)

Amantadine: antiviral used for treating Parkinson's, influenza and Alzhiemer's. Has many effects in the brain and has been associated with several central nervous system side effects, likely due to amantadine's dopaminergic and adrenergic activity (releases dopamine and norepinephrine from nerve endings). It appears to be a weak NMDA receptor antagonist as well as a weak anticholinergic. (source: Wikipedia)

Dizocilpine (MK-801): a strong non-competitive antagonist of the N-methyl-d-aspartate (NMDA) receptor and an experimental drug that mimics schizophrenia in animals, has a potential to treat stroke, traumatic brain injury, and neurodegenerative diseases such as Huntington's, Alzheimer's, and amyotrophic lateral sclerosis. May be effective as a recreational drug, and may have an active dose in the 50-100 μg range. Little is known in this context about its effects, dosage, and risks. (source: Wikipedia)

Dexanabinol (HU-211): a synthetic cannabinoid derivative, which is the "unnatural" enantiomer of the potent cannabinoid agonist HU-210. HU-211 does not act as a cannabinoid receptor agonist, but instead has NMDA antagonist effects. It therefore does not produce cannabis-like effects, but is anticonvulsant and neuroprotective. (source: Wikipedia)

Remacemide: low-affinity NMDA antagonist with sodium channel blocking properties. Principle metabolite is an uncompetitive antagonist with a low affinity for the binding site. (source: Wikipedia)

Riluzole: used to treat amyotrophic lateral sclerosis. The drug has has several actions: sodium channel blockade, high-voltage calcium channel blockade, N-methyl-D-aspartate (NMDA)/glutamate receptor blockade. [Związek organiczny związek chemiczny, lek będący pochodną benzotiazolu, o nie do końca wyjaśnionym mechanizmie działania.] (source: Wikipedia)

4-MeO-PCP: 1-(4-methoxy-1-phenylcyclohexyl)piperidine, somewhat less potent than PCP itself and with a decreased duration of effect.

Most noble gasses.
Quote:
http://en.wikipedia.org/wiki/Nitrogen_narcosis: seems to support the theory that certain noble gases can be classed as and indeed are dissociatives, as their mode of action are dissociative anaesthetic in nature; If N2O is regarded as a dissociative, then so should be Xe, as its dissociative anaesthetic action is extremely effective.
Pentazocine: synthetically-prepared prototypical mixed agonist-antagonist narcotic (opioid analgesic) drug of the benzomorphan class of opioids used to treat mild to moderately severe pain. This compound may exist as one of two enantiomers, named (+)-pentazocine and (-)-pentazocine. (-)-pentazocine is a kappa-opioid receptor agonist, while (+)-pentazocine is not, instead displaying a ten-fold greater affinity for the sigma receptor. Oprócz skutków ubocznych występujących przy leczeniu wszystkimi pochodnymi morfiny pentazocyna może powodować także zaburzenia nastroju, halucynacje i depersonalizację. (source: Wikipedia)

[can this one be called a dissociative at all? - Sushi]

AP5 or APV: (2R)-amino-5-phosphonovaleric acid; (2R)-amino-5-phosphonopentanoate is a selective NMDA receptor antagonist that competitively inhibits the ligand (glutamate) binding site of NMDA receptors. (source: Wikipedia)

[this is NMDA antagonist but has it got any known psychoactive properties? - Sushi]

[top]Legal status of Dissociatives

[top]United Nations

[top]USA

[top]EU

[top]History of Dissociatives


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Category: Hallucinogens

[top]References

[top]Pages in category "Dissociatives"


Contributors: NeuroChi , Alfa
Created by Alfa, 09-05-2007 at 00:40
Last edited by NeuroChi , 22-02-2011 at 17:36
Last comment by Joe-(5-HTP) on 15-09-2011 at 00:02
1 Comments, 28,704 Views

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