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STP : main ionotropic receptors MAIN IONOTROPIC RECEPTORS (5x)

Table of contents :


 
name
expressed on ...
ligand(s)
agonists
antagonists
... whose ligands induce channel opening :

Ca2+ channels (also permeable to Na+ (1 Na+ every 5 Ca2+) and K+)

NMDA receptor (NMDAR) (heteromer:  Clathrin-dependent NMDAR endocytosis requires both Gly and Glu site activation. hippocampus Glu + Gly

Asp + Gly

quinolinate 

taurine (antagonist)

 NMDA + Gly

homoquinolinate 

D-cycloserine (DCS) (Seromycin®) (partial agonist)

 noncompetitive antagonists :  competitive antagonists : 
  • D-AP-5 / (+/-)-2-amino-5-phosphonovaleric acid (APV)
  • D-AP-7 (partial agonist)
  • (+/-)-3-(2-carboxypiperazin-4-yl)-propyl-1-phosphonic acid (CPP)
  • a-methyl-carboxyphenylglycine
  • amantadine (Symmetrel®)
  • memantadine
  • memantine (Axura®, Akatinol®, Exiba®, Namenda®, Neuroplus®)
  • riluzole / 2-amino-6-[trifluoromethoxy]benzothiazole (Rilutek®)
  • metapramine (Timaxil®)
  • ketanserin (Sufrexal®, Aseranox®, Ketensin®, Ketenserina®, Perketan®, Serepress®, Sparfloxacine®)
antagonists at the polyamine site : 
  • eliprodil
drugs that may interfere with glutamate release by sodium channel blockade as well as having other actions 
  • 619C89
  • lubeluzole (Prosynap®) is a benzothiazole derivative that has shown neuroprotective properties in different experimental models inhibiting glutamate release, nitric oxide (NO) synthesis and blocking voltage-gated Na+ and Ca2+ ion channels
competitive antagonists of the glutamate recognition site of the NMDA receptor 
  • selfotel
noncompetitive blockers of the ion channel associated with the NMDA receptor : 
  • aptiganel (Cerestat®)
competitive antagonists of the glycine recognition site : 
  • ACEA 1021
  • GV150526
  • gavestinel
Na+ and K+ channels (also permeable to Ca2+)
kainate (heteromer : subunits 1, 2, 3, 4 and 5)  B lymphocytes Glu kainic acid 
domoic acid		 AP5 
MK801 
LY223053 
riluzole / 2-amino-6-[trifluoromethoxy]benzothiazole (Rilutek®)
AMPA receptor (AMPAR) (heteromer : subunits  granule and pyramidal cells in the hippocampal formation : active only upon depolarization (often mediated by AMPA receptors) and Gly costimulation Glu
  • a-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) 
  • 1,4-dihydroquinoxaline-2,3-dione (ANQX) (obtained from DNQX by replacing one of the nitro groups (NO2) with a highly photoreactive azido group (-N3); upon exposure to UV light, the azido group loses dinitrogen (-N2) to form a nighly reactive nitrene (:N), and this photoactivated antagonist then irreversibly binds to and inhibits AMPARsref)
  • quisqualic acid
    		•  6-cyano-7-nitroquinoxaline 
    -2,3-dione (CNQX) 
    LY215490 
    barbiturates (also GABAA agonists) 
    • 2-oxybarbiturates
      • long-acting barbiturates (5-phenyl substituent; anticonvulsant acitivity)
        • barbital (Barbital®, Calmine®, Neurinase®, Peralga®, Plexonal®, Veramon®, Veronal®)
        • mephobarbital (Mebaral®)
        • primidone (Mysoline®) => phenobarbital (PB) (also CAR agonist) (Adonal®, Alepsal®, Anirrit®, Barecal®, Corosedine®, Deriminal®, Dilatrane®, Dolviran®, Epanal®, Eupaco®, Gardenal®, Gardenale®, Hydantal®, Luminal®, Luminalettes®, Myocardon®, Natisedine®, Nunol®, Perphyllon®, Phenobarbital®, Plexonal®, Priscophene®, Quietal®, Tensedine®, Solfoton®, ..) and phenylethylmalonamide (PEMA)
        • methylphenobarbital (Prominal®)
      • medium-acting barbiturates
        • amobarbital (Amesec®, Amytal®, Dexamyl®, Eunoctal®, Tuinal®)
        • cyclobarbital (Cyclobartital®, Phanodorme®, Phanodorme calcium®, Proponal®, Quadronox®, Sanox®)
        • heptabarbital (Medomine®)
      • short-acting barbiturates
        • butabarbital / butobarbital (Butisol®)
        • hexobarbital (Evipan®, Tobinal®)
        • pentobarbital (Barecal®, Carbrital®, Nembutal®)
        • secobarbital (Immenoctal®, Secorbarbital®, Seconal®, Tuinal®; Vesparax® in combination with hydroxyzine and brallobarbital)
      • ultra-short acting barbiturates
        • methohexital (Brevital®)
      • allobarbital (Asmac®, Cibalgine®, Dial®, Somnocodal®)
      • alphenal (Efrodal®)
      • aprobarbital (Alurate®, Plexonal®, Somnifene®)
      • brallobarbital (Vesparax® in combination with  hydroxyzine and secobarbital)
      • cyclopentobarbital (Barecal®, Cyclopal®)
      • phethabarbital / N-phenylbarbital
      • propylbarbital (Proponal®)
      • talbutal
      • tetralobarbital (Sandoptal®)
    • 2-thiobarbiturates (more lipid-soluble => decreased duration of action, latency to onset, accelerated degradation)
      • thiamylal (Surital®)
      • thiopental sodium (Pentothal®; "Truth serum")
    5-HT3 / M receptor (heterodimer : a and b subunits) chemo-receptor trigger zone (CTZ; area postrema) ; 
    stomach ; 
    small intestine ; 
    nucleus tractus solitarius (NTS) ; peripheral nerves    		 5-HT a-methyl-5-HT 
    m-chlorophenylpiperazine (mCPP)     		 metoclopramide (Plasil®, Reglan®) 
    alosetron (Lotronex®) 
    dolasetron / hydroxydolasetron (Anzemet®) 
    granisetron (Kytril®) 
    ondansetron (Zofran®, Zophren®) 
    palonosetron (Aloxi® : > 30X higher affinity, half-life = 40 hours, single 0.25 mg IV dose) 
    tropisetron (Navoban®) 
    mianserin (Norval®)
    P2X1 (homo-trimer: it can heterodimerize with P2X5) B lymphocytes, urinary bladder alpha,beta-methyleneATP suramin; 
    PPADS
    P2X2 (homo-trimer : it can heterodimerize with P2X3) B lymphocytes alpha,beta-methyleneATP suramin; 
    PPADS
    P2X3 (homo-trimer: it can heterodimerize with P2X2) heart, spinal cord alpha,beta-methyleneATP suramin; 
    PPADS
    P2X4 (homo-trimer: it can heterodimerize with P2X6) B lymphocytes, brain alpha,beta-methyleneATP suramin; 
    PPADS
    P2X5 (homo-trimer : it can heterodimerize with P2X1) activated T-cells alpha,beta-methyleneATP suramin; 
    PPADS
    P2X6 (homo-trimer: it can heterodimerize with P2X4) placenta, spleen alpha,beta-methyleneATP suramin; 
    PPADS
    P2X7 / P2Z (homo-trimer) : upon brief exposure to ATP in the mM range, P2X7 functions as a nonselective cation channel, but upon prolonged exposure, channels rapidly transform into pores allowing passages of solutes up to 800 Da, leading to cell death by apoptosis. B lymphocytes alpha,beta-methyleneATP suramin; 
    PPADS
    OxATP
    salt molecules tongue
    Na+ channels (also permeable to K+, Ca2+, Rb+, Mg2+ and NH4+)
    N 
    • a 
    • b 
    • d
    • e 
    • g

      •  
    • skeletal muscle (NM) : 
      • (a1)2b1gd
      • (a1)2b2ed
    • postsynaptic neurons of autonomic ganglia and adrenal medulla (NN) : (a2-9)2(b2-4)3
    • NCNS : (a2-9)0-5(b2-4)5-0
    		 skeletal muscle cells, 
    postganglionic neurons in both 
    ortosympathetic and parasymphatetic systems, bronchial epithelial and endothelial cells, 
    electroplaque of Electrophorus spp. and Torpedo spp..    		 ACh homoanatoxin-a
    anatoxin-a
    a-conotoxin
    epibatidine
    cytisine 
    ganglionic stimulating drugs : 
    • nicotine (polacrilex gums (Nicorette®), trandermal patch (Nicoderm®, Habitrol®, ...), nasal spray (Nicotrol NS®), and vapor inhaler (Nicotrol Inhaler®))
    • lobeline
    • tetramethylammonium (TMA)
    • phenyltrimethylammonium (PTMA)
    • 1,1-dimethyl-4-phenylpiperazinium iodide (DMPP)
         		 Me-lycaconitine 
    ganglioplegics / ganglionic blocking agents
    • tetraetylammonium (TEA)
    • hexamethonium (C6)
    • trimethaphan (Arfonad®)
    • mecamylamine (Inversine®, Mevasine®, Prexion®)
    neuromuscular blocking agents
    • depolarizing agents
      • decamethonium (C10)
      • succinylcholine (Anectine®, ...)
      • suxamethonium (Scoline®)
    • competitive (stabilizing) agents
    Cl- channels
    GABAA receptor complex (GRC) : a2b2g presynaptic in spinal cord a-motoneurons; postsynaptic in cortical and cerebellar pyramidal cells, cuneate nucleus, substantia nigra, and thalamic relay neurons GABA (a subunit) 

    endozepin-4 (b subunit) 

    taurine

    		 pagoclone (partial agonist/modulator) 
    benzodiazepines (BDZ) (allosteric drugs on b subunit; binding requires g subunit, too) 
    • 2-ketobenzodiazepines (active catabolites)
      • short half-life
        • bromazepam (Lectopam®, Lexotan®, Lexotanil®)
      • long half-life (t > 40 hrs)
        • chlordiazepoxide (Librax®, Libritabs®,  Librium®, Tropium®; Limbitrol® in combination with amitriptyline)
        • chlordesmethyldiazepam / delorazepam (En®)
        • clobazam (Frisium®)
        • clorazepate (Tranxene®, Tranxilene®)
        • diazepam (DZP) (Dizac®, Noan®, Valium®)
        • flurazepam (Flunox®, Dalmane®)
        • halazepam (Paxipam®, Alapryl®, Pacinone®)
        • ketazolam (Anxon®)
        • medazepam (Nobrium®, Debrun®, Lerisum®, Rusedal®)
        • pinazepam (Domar®)
        • prazepam (Centrax®)
        • quazepam (Dormalin®, Doral®, Prosedar®, Quazium®, Selepam®, Temodal®)
    • 3-hydroxybenzodiazepines (t < 24 hrs)
      • comazepam
      • lorazepam (Ativan®, Tavor®, Alzapam®, Almazine®, Durazolam®, Loraz®, Temesta®)
      • lormetazepam (Noctamid®, Noctamide®, Ergocalm®)
      • oxazepam (Serenid®, Serpax®, Serax®, Adumbran®, Alepam®, Murelax®, Serepax®, Seresta®, Vaben®) 
      • temazepam (Eupnios®, Restoril®)
    • 7-nitrobenzodiazepines (24 < t < 48 hrs)
      • clonazepam (CZP) (Rivotril®, Klonopin®)
      • flunitrazepam (Hipnosedon®, Roipnol®, Rohypnol®) (drug of abuse)
      • nitrazepam (Mogadon®)
    • triazolobenzodiazepine (2 < t < 5 hrs)
      • adinazolam (Deracyn®)
      • alprazolam (Ansiopax®, Apotex®, Constan®, Mialin®, Pazolam®, Tafil®, Tranquinal®, Xanax®, Xanor®, Zanapam®)
      • estazolam (Prosom®, DEprinocte®, Domnamid®, Esilgan®, Kainever®, Nuctalon®) 
      • midazolam (Versed®, Dormicum®, Hypnovel®) 
      • triazolam (Halcion®, Songar®, Triazoral®, Alpralid®)
    • thienodiazepines (t > 24 hrs)
      • brotizolam (Lendormin®)
      • clotiazepam
    • loprazolam (Dormonoct®, Havlane®, Sonan®)
    • metaclazepam (Talis®)
    • zopiclone (Imovane®, Rhovane®, Zimovane®)
    imidazopyridines
    • alpidem (Anaxyl®)
    • zolpidem (Stilnox®, Ambien®)
    pyrazolopyrimidine
    • zaleplon (Sonata®)
    imidazopyrimidines
    imidazoquinolones
    cyclopyrrolones
    • eszopiclone (Lunesta®)
    barbiturates (complete agonists ; also AMPAR antagonists) 
    • 2-oxybarbiturates
      • long-acting barbiturates (5-phenyl substituent; anticonvulsant acitivity)
        • barbital (Barbital®, Calmine®, Neurinase®, Peralga®, Plexonal®, Veramon®, Veronal®)
        • mephobarbital (Mebaral®)
        • primidone (Mysoline®) => phenobarbital (also CAR agonist) (Adonal®, Alepsal®, Anirrit®, Barecal®, Corosedine®, Deriminal®, Dilatrane®, Dolviran®, Epanal®, Eupaco®, Gardenal®, Gardenale®, Hydantal®, Luminal®, Luminalettes®, Myocardon®, Natisedine®, Nunol®, Perphyllon®, Phenobarbital®, Plexonal®, Priscophene®, Quietal®, Tensedine®, Solfoton®, ..) and phenylethylmalonamide (PEMA)
        • methylphenobarbital (Prominal®)
      • medium-acting barbiturates
        • amobarbital (Amesec®, Amytal®, Dexamyl®, Eunoctal®, Tuinal®)
        • cyclobarbital (Cyclobartital®, Phanodorme®, Phanodorme calcium®, Proponal®, Quadronox®, Sanox®)
        • heptabarbital (Medomine®)
      • short-acting barbiturates
        • butabarbital / butobarbital (Butisol®)
        • hexobarbital (Evipan®, Tobinal®)
        • pentobarbital (Barecal®, Carbrital®, Nembutal®)
        • secobarbital (Immenoctal®, Secorbarbital®, Seconal®, Tuinal®; Vesparax® in combination with hydroxyzine and brallobarbital)
      • ultra-short acting barbiturates
        • methohexital (Brevital®)
      • allobarbital (Asmac®, Cibalgine®, Dial®, Somnocodal®)
      • alphenal (Efrodal®)
      • aprobarbital (Alurate®, Plexonal®, Somnifene®)
      • brallobarbital (Vesparax® in combination with  hydroxyzine and secobarbital)
      • cyclopentobarbital (Barecal®, Cyclopal®)
      • phethabarbital / N-phenylbarbital
      • propylbarbital (Proponal®)
      • talbutal
      • tetralobarbital (Cafergot®, Sandoptal®)
    • 2-thiobarbiturates (more lipid-soluble => decreased duration of action, latency to onset, accelerated degradation)
      • thiamylal (Surital®)
      • thiopental sodium (Pentothal®; "Truth serum")
    muscimol
    isoguvacine 
    THIP 
    halothane (Fluothane®) 
    enflurane (Ethrane®) 
    isoflurane (Forane®) 
    desflurane (Suprane®) 
    methoxyfluorane (Metofane®) 
    sevoflurane (Ultane®) 
    nitrous oxide / dinitrogen monoxide / N2O 
    propofol (Diprivan®) 
    etomidate (Amidate®) 
    neurosteroids : carbamates 
    • carisoprodol (Soma®) => meprobamate (Eubamate®, Meprobamatum®, Meprocalm®, Meprodil®, Meprolettes®, Miltown®, Oasil®, Pertranquil®, Probamyl®, Proponal®, Quaname®, Equanil®, Meprotabs®, Meprospan®, Meptran®, Novalm®, Promate®, Vio-Bamate®)
    chloral hydrate => trichloroethanol (CCl3CH2OH) 
    paraldehyde (Paral®) 
    ethchlorvynol (Placidyl®) 
    glutethimide (Doridene®, Ondasil®) 
    methyrprylon 
    ethinamate 
    etomidate (Amidate®) 
    clomethiazole 
    compound 4 (a2 subunit selectivity => anxiolytic activity without sedative liability)    		 b-carbolines (inverse agonists) ; 
    RO 15-4513 (inverse agonist on a6-containing GABAA) 
    SR 95531 
    bicucullin 
    picrotoxin
    pentamethylentetrazole 
    imidazobenzodiazepine 
    • flumazenil (Romazicon®)
    chlorinated cyclodiene insecticides : 
    • aldrin
    • chlordane
    • dieldrin
    • endrin
    • heptachlor
    hexachlorocyclohexane (HCH) / benzene hexachloride (BHC) is a mixture of 8 isomers 
    • CNS-stimulating isomers
      • a isomer
      • g isomer / lindane
    • CNS-depressing isomers
      • b isomer
      • d isomer
    • e
    • z / i
    • h
    • q
  • toxaphene is a complex mixture of > 175 C10 polychlorinated hydrocarbons, of which only ~ 20 are known (e.g. heptachlorobornane)
  • mirex
  • chlordecone (Kepone®)
  • tetramine (tetramethylene disulfotetramine)
  • fluoroquinolones
    		•
    GABACref retina, spinal cord, superior colliculus, pituitary and the gut and their involvement in vision, aspects of memory and sleep-waking behaviour GABA partial agonists :
    •  (+/-)-trans-2-(aminomethyl)cyclopropanoic acid ((+/-)-TAMP) and imidazole-4-acetic acid (I4AA) 
    • CACA
    		 P4PMA
    1,2,5,6-tetrahydropyridine-4-yl)methylphosphinic acid (TPMPA)
    4,5,6,7-tetrahydroisoxazole[4,5-c]pyridine-3-ol (THIP)
    2-methyl-TACA 
    picrotoxin
    Zn2+ > Ni2+ > Cu2+ > Cd2+ref
    Gly (heterodimer :  Gly
    taurine    		 b-alanine 
    D-serine 

    halothane (Fluothane®) 
    enflurane (Ethrane®) 
    isoflurane (Forane®) 
    desflurane (Suprane®) 
    sevoflurane (Ultane®) 
    nitrous oxide / dinitrogen monoxide / N2O 
    propofol (Diprivan®) 
    barbiturates
    neurosteroids 

    • alphaxalone (Althesin®)
    • pregnanolone
    		 strychnine
    H+ channels
    acidic molecules tongue
    ... whose ligands induce channel closing :

    K+ channels

    some bitter molecules tongue
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