NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. ANTAGONISTS - Can inhibit the development of tolerance to Morphine

Memantine - Noncompetitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives., HT3, NACh antagonistA substance that interferes with or inhibits the physiological action of another. and D2 agonistA substance that initiates a physiological response when combined with a receptor.. For use in Alzheimer's patients,

Delucemine - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another., SRISerotonin Reuptake Inhibitor and has neuroprotective effects.

Alazocine - σ1 agonistA substance that initiates a physiological response when combined with a receptor., κ opioid agonistA substance that initiates a physiological response when combined with a receptor. & slight NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.

Caroverine - It acts as an N-type Ca+ blocker, competitive AMPA antagonistA substance that interferes with or inhibits the physiological action of another., and non-competitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. It also has potent antioxidant effects.

Lanicemine - Low affinity NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another., possible anti-depressant.

Dexoxadrol - Potent PCP analogue similar to Etoxadrol. Development discontinued due to side effects such as "nightmares and hallucinations"

Etoxadrol - potent PCP analogue ^^

Hodgkinsine - alkaloid found in Psychotria colorata plants. Has antiviral, antibacterial and antifungal properties. Also μ opioid agonistA substance that initiates a physiological response when combined with a receptor. & NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another..

Psychotridine - non-competitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. found in Psychotria colorata. Incredible structure!

Dexanabinol - Synthetic CannabinoidChemicals produced naturally that bind to cannabinoid receptors. They are involved in a variety of mental and physical processes, including pain regulation, food intake, and reward. which does not exhibit cannabinoidChemicals produced naturally that bind to cannabinoid receptors. They are involved in a variety of mental and physical processes, including pain regulation, food intake, and reward. agonism but instead NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonism.

Dextrallophan - Morphinan, σ1 agonistA substance that initiates a physiological response when combined with a receptor. & NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. 2x potency of DXM

Atomoxetine - Selective NRI & NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. Increases levels of NE & DA in prefrontal cortices by a factor of 3, however DA levels in striatum or nucleus accumbens are unaffected.

Levorphanol - μ, κ & δ agonistA substance that initiates a physiological response when combined with a receptor., 4-8x potency of M, long duration, no cross tolerance with morphine. NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. like it's dextro counterpart.

Neramexane - Related to Memantine, NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antag. and NACh antag. Has antidepressant, neuroprotective and nootropicNootropics, also referred to as smart drugs, memory enhancers, neuro enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that purportedly improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. They are generally neuroprotective, and non-toxic. properties

Rhynchophylline - Weak NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. found in certain Uncaria species of plant. Also present in Kratom.

Phencyclidine - PCP. NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antag., DRIDopamine Reuptake Inhibitor, HT2A agonistA substance that initiates a physiological response when combined with a receptor. etc.

Rolicyclidine - Sedative PCP analogue, similar to barbiturates

3-MeO-PCPy - 3-MeO version of PCPy

Tenocyclidine - Higher affinity to NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. than PCP, deeper experience

Gacyclidine - PCP analogue with similar characteristics. Derivative of TCP.

Eticyclidine - More potent PCP analogue with similar effects.

Dieticyclidine - Low potency prodrug for eticyclidine, however it exhibits NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistic effects in itself.

PCPr - Similar Potency to PCP

PCiPr - ^^

3-Fl 2-OH PCiPr - Similar to MXEMethoxetamine but less potent and maybe different effects?

Dimethicyclidine - PCM with a dimethyl bond.

NEFA - Moderate affinity NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. PCP analogue.

3-MeO-TCP - More balanced version of TCP

3-Fluoro-TCP - Similar to the above however slightly more potent?

2-Chloro-2-Oxo-TCM - Thiopyrrole Ketamine or Tenoketamine (S-iso)

3-HO, 2-Oxo-BCPy - Opiate stimulant

PCA - blank ketamine structure minus foliage

Diphenidine - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. with little information.

Sabeluzole - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antag. with neuroprotective and nootropicNootropics, also referred to as smart drugs, memory enhancers, neuro enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that purportedly improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. They are generally neuroprotective, and non-toxic. effects.

8A-PDHQ - High affinity NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another., potency similar to MK-801.

Amantadine - Weak NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another., NACh-a7 antagonistA substance that interferes with or inhibits the physiological action of another. and MAOMonoamine Oxidase, an enzyme that catalyses the metabolism of many drugs (e.g., DMT, dopamine and serotonin).-A inhibitor.

Indantadol - Acts as a reversible, non-competitive MAOIMonoamine oxidase inhibitor are drugs that inhibit the action of monoamine oxidase in the brain and so allow monoamines to accumulate. and a low affinity NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. NootropicNootropics, also referred to as smart drugs, memory enhancers, neuro enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that purportedly improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. They are generally neuroprotective, and non-toxic. potential.

Ketamine - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. ant. Gold Standard. Also DRIDopamine Reuptake Inhibitor, κ & μ opioid agonistA substance that initiates a physiological response when combined with a receptor.. S-IsomerEach of two or more compounds with the same formula but a different arrangement of atoms in the molecule and different properties. 50% more potent, R-IsomerEach of two or more compounds with the same formula but a different arrangement of atoms in the molecule and different properties. less potent, morelike alcohol

Methoxetamine - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. ant, DRIDopamine Reuptake Inhibitor, SERT, μ & κ opioid agonistA substance that initiates a physiological response when combined with a receptor.

2-MeO-PCP - Potent ketamine type drug. 2-MeO-PCM has effects identical to Ketamine.

3-MeO-PCP - PCP analogue with a more balanced effects profile. Smooth and relaxing.

4-MeO-PCP - Low potency PCP analogue with effects similar to low dose Ketamine.

Ketobemidone - μ opioid antagonistA substance that interferes with or inhibits the physiological action of another. & NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. More addictive than M

3-HO-PCP - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. ant, DRIDopamine Reuptake Inhibitor, μ opioid agonistA substance that initiates a physiological response when combined with a receptor. (sigma?)

Remacemide - Low affinity NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. with Sodium channel blocking properties.

MK-801 (Dizocilpine) - potent dissociative, DRIDopamine Reuptake Inhibitor and NAch antag. Mix between PCP, Tiletamine and Rohypnol. Used to simulate psychosis in animal models.

Huperzine A - acetylcholinesterase inhibitor, NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.

Kynurenic Acid - Product of metabolism of l-Tryptophan. AntagonistA substance that interferes with or inhibits the physiological action of another. at AMPA, NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives., Kainate glutamate and ligand for GPR35. Useful in neurological disorders

Tiletamine - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. similar to Ketamine and PCP but mainly used as an anaesthetic for large animals. Gets a bit nutty.

Flupirtine - Non-opioid, non-NSAID, non-steroidal painkiller. Selective neuronal potassium channel opener with NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonism.

Muscimol - Potent, selective GABAa agonistA substance that initiates a physiological response when combined with a receptor.. Although non-stated, theories towards MACh and NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonism are grounded due to it's effects as a hallucinogen.

PEAQX - Competitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another., 100-fold selective for GluN1/GluN2A receptors vs. GluN1/GluN2B receptors.

Midafotel - Potent, competitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another., non-toxic however unsuitable for epilepse trials due to lack of neuroprotection.

AP5 - Selective competitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. Useful in isolating the actions of AMPA and kianate receptors.

AP-7 - Selective, competitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. Antagonism of NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. causes GABAGamma aminobutyric acid an amino acid that is found in the central nervous system; acts as an inhibitory neurotransmitter. excitation to reach equilibrium in the brain. Is known to cause muscle rigidity.

LY-235,959 - Competitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. Has analgesic and neuroprotective properties as well as reducing tolerance to opioids.

2-MDP* - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. that produces similar effects to PCP in animals, it also has a stimulant effect 1/3 potency of Amp. Effects last around 24 hours.

Traxoprodil - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antag selective for the NR2B subunit. Neuroprotective, analgesic and antidepressant. Psychoactive side effects and abuse potential at high doses.

Magnesium - Essential to the human body. Mg deficiency causes cardiovascular disease, diabetes, high blood pressure, anxiety disorders, migraines, osteoporosis and cerebral infarction. A regular amount must be taken each day.

Aptiganel - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. with neuroprotective properties. Side effects such as hallucinations and sedation occurs.

Budipine - Effects not well understood. NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. and promotes the synthesis of dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system..

Perzinfotel - Potent NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. HasNeuroprotective effects but lacks analgesic effects.

Orphenadrine - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives., MACh, H1 antagonistA substance that interferes with or inhibits the physiological action of another. and NET, Na1.7, 1.8 & 1.9 and HERG Po blocker. Used against pain and muscle spasms.

Gavestinel - Selective NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. without PCP's behavioural effects. Neuroprotective.

Ifenprodil - Selective NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. inhibitor, specific to NR1 & NR2B subunits.

Acamprosate - Positive GABAa allosteric modulator and NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. inhibitor. Useful in alcohol dependance and has neuroprotective properties.

Agmatine - Amino acid metabolite, binds to a2 and imidazoline receptors and blocks NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. receptors. Has neuroprotective effects in animals with brain trauma.

Selfotel - Competitive NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another.. Has anticonvulsant, anxiolytic, analgesic and neuroprotective effects. PCP-esque effects and possible neurotoxicity.

7-Chlorokynurenic acid - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. with antidepressant effects

DCKA - Selective NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. at the glycine site.

Eliprodil - NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonistA substance that interferes with or inhibits the physiological action of another. without the sedative or amnesiatic effects of other NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antags. Does not substitute for PCP but shows neuroprotective effects.

METABOTROPIC GLUTAMATE RECEPTOR (MGluR) LIGANDS

MGluR I LIGANDS -> MGluR 1 & 5

Agonists:

Ro67-4853 - Lead compound used to investigate selective positive AM for MGluR1. Studies show that PAMs activate cAMP production, calcium mobilization and extracellular signal-regulated kinase 1/2 (ERK1/2) phosphorylation.

CDPPB - Selective positive AM for MGluR5. It has antipsychotic and nootropicNootropics, also referred to as smart drugs, memory enhancers, neuro enhancers, cognitive enhancers, and intelligence enhancers, are drugs, supplements, nutraceuticals, and functional foods that purportedly improve mental functions such as cognition, memory, intelligence, motivation, attention, and concentration. They are generally neuroprotective, and non-toxic. effects and is capable of directly potentiating the depolarization of hippocampal CA1 neurons induced through NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. administration. It also extinguishes drug-oriented memories hindering treatment and causing relapse.

Dihydroxyphenylglycine (DHGP) - Group selective (possibly) partial agonistA substance that initiates a physiological response when combined with a receptor. for MGluR I. Displays cognitive enhancing effects useful in the treatment of Alzheimers and neuronal injury. Another group agonistA substance that initiates a physiological response when combined with a receptor., ACPD, can induce convulsions in neonatal rats.

Antagonists:

CPCCOEt - High selectivity but moderate affinity antagonistA substance that interferes with or inhibits the physiological action of another. at MGluR1 used in research of the behavioural effects of addiction and memory. Impairs fear extinction 48hrs after conditioning but not at 2hrs implying MGluR1 is critical in long term memory.

CTEP - High potency and selectivity as an MGluR5 antagonistA substance that interferes with or inhibits the physiological action of another. with high BA and long duration (18hrs). Has anti-hyperalgesic (increased sensitivity to pain) effects and has been shown to be neuroprotective and hepatoprotective (prevents damage to liver).

SIB-1893 - Selective MGluR5 antagonistA substance that interferes with or inhibits the physiological action of another. and positive AM of MGluR4. Has anticonvulsant and neuroprotective effects, and reduces glutamate release.

Mavoglurant - Selective MGluR5 antagonistA substance that interferes with or inhibits the physiological action of another. currently in phase 2&3 trials to treat the underlying disorder behind Fragile X Syndrome (inherited autism and retardation among male South Americans).

MTEP - Potent, selective allosteric antagonistA substance that interferes with or inhibits the physiological action of another. at MGluR5. Produces neuroprotective, antidepressant, analgesic, and anxiolytic effects. Also reduces symptoms of morphine withdrawal and decreases the addictive effects of nicotine, cocaine and methamphetamine.

Fenobam - Potent, selective negative AM of mGluR5. Has anxiolytic effects comparable to benzos and also displays additional antidepressant, analgesic and anti-addictive effects.

MGluR II LIGANDS -> MGluR 2 & 3

Agonists:

Biphenylindanone A (BINA) - Potent & selective MGluR 2 positive AM. It displays anxiolytic and antipsychotic properties and decreases cocaine self administration.

LY-487,379 - Selective MGluR 2 positive AM similar to BINA.

DCG-IV - Group-selective agonistA substance that initiates a physiological response when combined with a receptor. at MGluR2&3. Displays potent neuroprotective and anticonvulsant effects as well as anti-Parkinsonian effects, but also impairs the formation of memories.

Eglumegad - Group selective agonistA substance that initiates a physiological response when combined with a receptor. for MGluR II with possible D2 interaction. As effective an anxiolytic as diazepam without sedation or memory impairment. Relieves the withdrawal symptoms from drugs like nicotine and morphine as well as inhibiting the development of tolerance to M. It is neuroprotective and synergistic with the neuroprotection induced by NMDAN-methyl-D-aspartate receptor. NMDA antagonists are often dissociatives. antagonists. Also reduces the effects of 5-HT2a agonists. Chronic oral admin. also markedly reduced baseline cortisol (steroidAnabolic steroids are drugs that are structurally related to the cyclic steroid ring system and have similar effects to testosterone in the body. They increase protein within cells, especially in skeletal muscles. Anabolic steroids also have androgenic and virilizing properties, including the development and maintenance of masculine characteristics such as the growth of the vocal cords, testicles (primary sexual characteristics) and body hair (secondary sexual characteristics). hormone released in response to stress) levels and diminished yohimbine induced stress response (fight or flight). However has low BA so the prodrug LY-544,344 is more likely to be used in trial.

LY-404,039 - Group selective agonistA substance that initiates a physiological response when combined with a receptor. for MGluR II with considerable affinity for the D2 receptor. It has anxiolytic and antipsychotic effects in animal studies.

Antagonists:

PCCG-4 - Group selective antagonistA substance that interferes with or inhibits the physiological action of another. for MGluR II with slight selectivity for MGluR2.

CECXG - Potent, group selective antagonistA substance that interferes with or inhibits the physiological action of another. for MGluR II with reasonable selectivity for mGluR3 at 38x higher affinity than mGluR2.

LY-341,495* - Potent, group selective antagonistA substance that interferes with or inhibits the physiological action of another. for MGluR II . Shows antidepressant effects while potentiating psychedelics and opioids, as well as modulating dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. receptor function. The 1-fluorocyclopropane analog has a superior pharmacokinetic profile and similar receptor affinities, making a prodrug from this with the heptyl ester increases BA even further.

MGS-0039 - Potent, group selective antagonistA substance that interferes with or inhibits the physiological action of another. for MGluR II. Produces antidepressant and anxiolytic effects, and boosts release of dopamineA neurotransmitter associated with movement, attention, learning, and the brain’s pleasure and reward system. and serotoninA monoamine neurotransmitter, biochemically derived from tryptophan, that is primarily found in the gastrointestinal (GI) tract, platelets, and central nervous system (CNS) of humans and animals. It is a well-known contributor to feelings of well-being. in specific brain areas possibly through a similar mechanism as ketamine.

RO4491533 - Potent, group selective negative AM for MGluR II, being equipotent at mGluR2 and mGluR3. Producing antidepressant effects and reversing the effects of group II agonistA substance that initiates a physiological response when combined with a receptor. LY-379,268 but at lower potency than LY-341,495.

MGluR III LIGANDS -> MGluR 4, 7 & 8

Agonists:

PHCCC - Positive allosteric modulator for MGluR4 (Receptor involved in tasting 'umami' or savory tastes), negative AM for MGluR1 (see Group I) and direct MGluR6 agonistA substance that initiates a physiological response when combined with a receptor. (?).

AMN082 - Selective MGluR7 allosteric agonistA substance that initiates a physiological response when combined with a receptor.. This produces and antidepressant type effect and rapid internallisation. At high doses hypo-locamotion increased significantly (shaking, flinching, general stimulated actions). Seems to also be linked to the PICK1 protein.

DCPG - MGluR8 agonistA substance that initiates a physiological response when combined with a receptor.. Has anti-convulsant and neuroprotective effects and could be used to treat hyperalgesia.

L-A4P - Non selective group III MGluR agonistA substance that initiates a physiological response when combined with a receptor.. Indicative of anti-parkinson effects by modulating GABAergic neurotransmission. Activation causes inhibition of GABAGamma aminobutyric acid an amino acid that is found in the central nervous system; acts as an inhibitory neurotransmitter. release in globus pallidus (involved in regulating voluntary movement) and anti-nociceptive effects.

Antagonists:

MMPIP - MGluR7 antagonistA substance that interferes with or inhibits the physiological action of another.. Seems to be involved in the downstream response to cocaine in the brain.

OTHER GLUTAMATERGIC LIGANDS

WAY-213,613 - Reuptake inhibitor for subtype EAAT2, highly selective over metabotropic and ionotropic glutamate receptors. Used for research into glutamate transporters.

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