Hallucinogen Hallucinogens are a general group of pharmacological agents that can be divided into three broad categories: psychedelics, dissociatives, and deliriants. These classes of psychoactive drugs have in common that they can cause subjective changes in perception, thought, emotion and consciousness. Unlike other psychoactive drugs, such as stimulants and opioids, these drugs do not merely amplify familiar states of mind, but rather induce experiences that are qualitatively different from those of ordinary consciousness. These experiences are often compared to non-ordinary forms of consciousness such as trance, meditation, dreams, or insanity. L. E.
Classes of dissociatives NMDA receptor antagonists κ-opioid receptor agonists Effects The effects of dissociatives can include sensory dissociation, hallucinations, mania, catalepsy, analgesia and amnesia. The characteristic features of dissociative anesthesia were described as catalepsy, amnesia and analgesia. According to Pender (1972), "the state has been designated as dissociative anesthesia since the patient truly seems disassociated from his environment Dissociative
Opioid An opioid is any psychoactive chemical that resembles morphine or other opiates in its pharmacological effects. Opioids work by binding to opioid receptors, which are found principally in the central and peripheral nervous system and the gastrointestinal tract. The receptors in these organ systems mediate both the beneficial effects and the side effects of opioids. Although the term opiate is often used as a synonym for opioid, the term opiate is properly limited to the natural alkaloids found in the resin of the opium poppy (Papaver somniferum), while opioid refers to both opiates and synthetic substances, as well as to opioid peptides.
Salvinorin A is the main active psychotropic molecule in Salvia divinorum, a Mexican plant which has a long history of use as an entheogen by indigenous Mazatec shamans. Salvinorin A is considered a dissociative exhibiting atypically psychedelic effects. Salvinorin A can produce psychoactive experiences in humans with a typical duration of action being several minutes to an hour or so, depending on the method of ingestion. History Salvinorin A
Ibotenic acid Ibotenic acid is a chemical compound that is naturally occurring in the mushrooms Amanita muscaria and Amanita pantherina, among others. Ibotenic acid is a powerful neurotoxin that is used as a "brain-lesioning agent" and has shown to be highly neurotoxic when injected directly into the brains of mice and rats. Psychopharmacology
Ketamine, one of the most common NMDA receptor antagonists. 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 anesthetics for animals and 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, although such damage has never been conclusively observed in primates like humans. However, adolescent cynomolgus monkeys that were injected daily for six months with the non-competitive NMDA antagonist ketamine showed decreased locomotor activity and increased apoptosis of cells in their prefrontal cortices. Several synthetic opioids function additionally as NMDAR-antagonists, such as Meperidine, Methadone, Dextropropoxyphene, Tramadol and Ketobemidone. NMDA receptor antagonist
Morphinan Morphinan is the base chemical structure of a large chemical class of psychoactive drugs, consisting of opioid analgesics, cough suppressants, and dissociative hallucinogens, among others. Morphinan has the phenanthrene backbone. Chemical derivatives Immediate derivatives of morphinan include: More distant of derivatives include:
Levomethorphan Levomethorphan is the l-stereoisomer of methorphan. The effects of the two isomers are quite different. Dextromethorphan is an antitussive at low doses and a dissociative at much higher doses, whereas levomethorphan is an opioid analgesic.
Dimemorfan Dimemorfan is an antitussive or cough suppressant which acts as a sigma receptor agonist. It is an analogue of dextromethorphan and dextrorphan, but lacks significant NMDA receptor antagonistic action and dissociative effects, thereby having reduced abuse potential and adverse effects in comparison. See also References Jump up ^ Wang, H. H.; Chien, J. W.; Chou, Y.
Dextrorphan Dextrorphan (DXO) is a psychoactive drug of the morphinan chemical class which acts as an antitussive or cough suppressant and dissociative hallucinogen. It is the dextro-stereoisomer of racemorphan, the levo-half being levorphanol. Dextrorphan is produced by O-demethylation of dextromethorphan by CYP2D6. Dextrorphan is an NMDA antagonist and contributes to the psychoactive effects of dextromethorphan.
Dextromethorphan Dextromethorphan (DXM or DM) is an antitussive (cough suppressant) drug. It is one of the active ingredients in many over-the-counter cold and cough medicines, including generic labels and store brands, Benylin DM, Mucinex DM, Robitussin, NyQuil, Dimetapp, Vicks, Coricidin, Delsym, TheraFlu, and others. Dextromethorphan has also found other uses in medicine, ranging from pain relief to psychological applications. It is sold in syrup, tablet, spray, and lozenge forms. In its pure form, dextromethorphan occurs as a white powder.
2-MDP 2-MDP (U-23807A) is a dissociative anaesthetic drug which has been found to be an NMDA antagonist and produces similar effects to PCP in animals. The levo or (-) isomer is the active form of the drug. It also has stimulant effects, having only around one third the potency of amphetamine by weight, but with a long duration of action, lasting more than 24 hours from a single oral dose. Jump up ^ Tang AH, Cangelosi AA, Code RA, Franklin SR. Phencyclidine-like behavioral effects of 2-methyl-3,3-diphenyl-3-propanolamine (2-MDP). Pharmacology, Biochemistry and Behaviour. 1984 Feb;20(2):209-13.Jump up ^ Blake JC, Davies SN, Church J, Martin D, Lodge D. 2-Methyl-3,3-diphenyl-3-propanolamine (2-MDP) selectively antagonises N-methyl-aspartate (NMA).
8A-PDHQ 8a-Phenyldecahydroquinoline (8A-PDHQ) is a high affinity NMDA antagonist developed by a team at Parke Davis in the 1950s. It is a structural analog of Phencyclidine with slightly lower binding affinity than the parent compound. (-)-8a-Phenyldecahydroquinoline has an in vivo potency comparable to that of (+)-MK-801. Jump up ^ US Patent 3035059Jump up ^ Chen C, Kozikowski AP, Wood PL, Reynolds IJ, Ball RG, Pang YP (1992). "Synthesis and biological activity of 8a-phenyldecahydroquinolines as probes of PCP's binding conformation.
Aptiganel (Cerestat; CNS-1102) is a drug which acts as a noncompetitive NMDA antagonist. It has neuroprotective effects and was researched for potential use in the treatment of stroke, but despite positive results in animal studies, human trials showed limited efficacy, as well as undesirable side effects such as sedation and hallucinations, and clinical development was ultimately not continued. Synthesis See also Ditolylguanidine References Jump up ^ Reddy NL, Hu LY, Cotter RE, Fischer JB, Wong WJ, McBurney RN, Weber E, Holmes DL, Wong ST, Prasad R, et al. Aptiganel