Les benzodiazépines (BZD) produisent leurs effets cliniques en se liant à des récepteurs spécifiques du système nerveux central. Le récepteur BZD fait partie d'un complexe supramoléculaire qui possède également des sites allostériques pour les barbituriques et le GABA. En facilitant l'unité de couplage GABA-canal à CL-, les BZD potentialisent l'inhibition neuronale. Les recherches actuelles visent à préciser le fonctionnement moléculaire des récepteurs et à identifier leurs ligands endogènes.
References
1.
IversenL.L., BloomF.E.Studies of the uptake of 3H-GABA and 3H- glycine in slices and homogenates of rat brain and spinal cord by electron microscopic autoradiography.Brain Res1972; 41: 131–143.
2.
SchonF., IversenL.L.The use of autoradiographic techniques for the identification and mapping of transmitter-specific neurones in the brain.Life Sci1974; 15: 157–175.
3.
TallmanJ.F., PaulS.M., SkolnickP.Receptors for the age of anxiety: pharmacology of the benzodiazepines.Science1980; 207: 274–812.
4.
SternbackL.H.The benzodiazepines story.J Med Chem1979; 22: 1–7.
5.
SternbackL.H.Chemistry of 1,4-benzodiazepines and some aspects of the structure-activity relationship. In: GarattiniS., MussiniE., RandallL.O., eds. The benzodiazepines.New York: Raven Press, 1973: 1–26.
6.
BraestrupC., NielsenM.GABA reduces binding of 3H-methyl-bcarboline-3-carboxylate to brain benzodiazepine receptors.Nature1981; 294: 472–474.
7.
BraestrupC., SquiresR.F.Specific benzodiazepine receptors in rat brain characterized by high affinity 3H-diazepam binding.Proc Natl Acad Sci USA1977; 74: 3805–3809.
8.
MohlerH., OkadaT.Benzodiazepine receptors: demonstration in the central nervous system.Science1977; 198: 848–851.
9.
BraestrupC., SquiresR.F.Brain specific benzodiazepine receptors.Br J Psychiatry1978; 133: 249–260.
10.
MohlerH., OkadaT.The benzodiazepine receptor in normal and pathological human brain.Br J Psychiatry1978; 133: 261–268.
11.
BraestrupC., SquiresR.F., BockE.Benzodiazepine receptors: cellular and sub cellular localisation in brain. In: Tillement JP, ed. Advances in pharmacology and therapeutics.Pergamon Press,1978; 7: 173–185.
12.
MohlerH., OkadaT.Benzodiazepine receptor: demonstration in the central nervous system.Science1977; 198: 848–851.
13.
BosmannH.B., PennyD.P., CaseK.R.Diazepam receptor, specific binding of 3H-diazepam and 3H-flunitrazepam to rat brain sub-fraction.FEBS Lett1978; 82(3): 68–72.
14.
BrownC.L., MartinI.L.Photoaffinity labelling of the benzodiazepine receptor cannot be used to predict ligand efficacy.Neurosci Lett1983; 35: 37–40.
15.
MarangosP.J., DatelJ., BoulengerJ.P.Characterization of peripheral type benzodiazepine binding sites in brain using 3H-RO5–4864.Mol Pharmacol1982; 22: 26–32.
16.
SnyderS.H.Drug and neurotransmitter receptors.JAMA1989; 26(1): 3126–3129.
17.
SquiresR.F., BraestrupC.Benzodiazepine receptors in rat brain.Nature1977; 266: 732–734.
18.
MohlerH.The benzodiazepine today: mechanisms of action of the benzodiazepines.Medicine North America (Suppl 1)1987; 3–7.
19.
BiscoeT.J., FryJ.P., RicketsC.Autoradiography of benzodiazepine receptor binding in the central nervous system of the normal C57BL6J mouse.J Physiol1984; 352: 495–508.
20.
YoungW.S., KuharM.Radiohistochemical localization of benzodiazepine receptors in rat brain.J Pharmacol Exp Ther1980; 212: 337–346.
21.
EnnaS.J., AndreeT.GABA receptor heterogeneity: relationship to benzodiazepines. In: PaulS.M., SkolnickP., TallmanJ., eds. Pharmacology of benzodiazepine.New York: MacMillan,1983;: 121–132.
22.
HillD.R., BoweryN.G.3H-baclofen and 3H-GABA binding to bicuculline in sensitive GABA-B sites in rat brain.Nature1981; 290: 149–152.
23.
HoltzmanS.G.Phencyclidine-like discriminative stimulus properties of Opioids in the squirrel monkey.Psychopharmacology1982; 77: 295–300.
24.
BoweryN.G., DobleA., HillD.R.GABA facilitates or inhibits the evoked release of 3H-noradrenaline from rat cerebellar cortex slices by an action at separate receptors.Br J Pharmacol1980; 70: 77.
25.
BoweryN.G., HillD.R., HudsonA.L.Characteristics of GABA-B receptor binding sites on rat whole brain synaptic membranes.Br J Pharmacol1983; 78: 191–206.
26.
KarbonE.W., EnnaS.J.Characterization of the relationship between gamma-aminobutyric acid B agonists and transmitter-coupled cyclic nucleotide-generating systems in rat brain.Mol Pharmacol1985; 27: 53–59.
27.
EnnaS.J., MohlerH.Gamma-aminobutyric acid (GABA) receptors and their association with benzodiazepine recognition sites. In: MeltzerH.Y., ed. Psychopharmacology: the third generation of progress.New York: Raven Press,1987; 266.
28.
EnnaS.J.Gamma-aminobutyric acid (GABA), pharmacology and neuropsychiatric illness. In: HalesE.R., FrancesJ.A., eds. Annual review, volume 4. Washington DC: American Psychiatric Press, Inc., 1985: 67–82.
29.
EnnaS.J., KarbonE.W., DumanR.S.GABA-B agonists and imipramine-induced modifications in rat brain B-adrenergic receptor binding and function. In: MorselliP.O., LloydK.G., eds. GABA and mood disorders.New York: Raven Press, 1985: 23–31.
30.
FahnS.Regional distribution studies of GABA and other putative neurotransmitters and their enzymes. In: RobertsE., ChaseT., TowerD., eds. GABA in nervous system function.New York: Raven Press, 1976: 169–188.
31.
HillD.R., DolphinA.C.Modulation of adenylate cyclase activity by GABA-B receptors.Neuropharmacology1984; 23: 829–830.
32.
CalneD.B.The pharmacology of spasticity. In: KlawansH.L., ed. Clinical neuropharmacology, volume 1. New York: Raven Press, 1976: 137–145.
33.
SquiresR.F., BraestrupC.Benzodiazepine receptor in rat brain.Nature1977; 266(5604): 732–734.
34.
EnnaS.J., MohlerH.Gamma-aminobutyric acid (GABA) receptors and their association with benzodiazepine recognition sites. In: MeltzerH.Y., ed. Psychopharmacology: the third generation of progress.New York: Raven Press, 1987: 269
35.
SkolnickP., PaulS.M.Molecular pharmacology of the benzodiazepines.International Review of Neurobiology1982; 23: 103–140.
ArakiT., ItôM., OscarssonO.Anion permeability of the synaptic and non synaptic moto neurone membrane.J Physiol1961; 159: 410–435.
38.
CurtisD.R., HosliL., JohnstonG.A.The hyperpolarization of spinal motoneurones by glycine and related amino acids.Exp Brain Res1968; 5: 235–258.
39.
BruggencateG.T., EngbergI.Effects of GABA and related amino acids on neurones in Deiters' nucleus.Brain Res1969; 14: 533–653.
40.
StudyR.E., BarkerD.F.Diazepam and pentobarbital fluctuation analysis reveals different mechanisms for potentiation of GABA responses in cultured central nervous.Proc Natl Acad Sci USA1981; 78: 7180–7184.
41.
StudyR.E., BarkerJ.F.Cellular mechanisms of benzodiazepine action.J Amer Med Assoc1982; 247: 2147–2151.
42.
BraestrupC., SchmeichenR., NeegG.Interaction of convulsive ligands with benzodiazepine receptors.Science1982; 216: 1241–1243.
43.
StephensonF.A., OlsenR.W.Solubilization by chaps detergent of barbiturate-enhanced benzodiazepine. GABA receptor complex.J Neurochem1982; 39: 1579–1586.
OlsenR.W., FischerJ.B., KingR.G.Purification of the GABA/benzodiazepine/barbiturate receptor complex.Neuropharmacology1984; 23: 853–854.
46.
MartiniC., LucacchiniA., RoncaG.Isolation of putative benzodiazepine receptors from rat brain membranes by affinity chromatography.J Neurochem1982; 38: 15–19.
47.
PolcP., BonettiE.P., SchaffnerR.A three-state model of the benzodiazepine receptor explains the interactions between the benzodiazepine antagonist RO 15–1788, benzodiazepine tranquilizers, β-carbolines, and phenobarbitone.Naunyn-Schmiedeberg's Arch Pharmacol1982; 321: 260–264.
48.
MohlerH., RichardsJ.G.Agonist and antagonist benzodiazepine receptor interaction in vitro.Nature1971; 294: 763–765.
49.
GeeK.W., HorstW.D., O'BrienR.High affinity inhibition of [3H]-flunitrazepam bindinto brain benzodiazepine receptors by CGS 9896, a novel pyrazologuinoline.Biochem Biophys Res Commun1982; 105: 457–461.
50.
MeinersB.A., SalamaA.Enhancement of GABA binding by the benzodiazepine partial agonist CGS 9896.Eur J Pharmacol1985; 119: 61–65.
51.
Paldi-HarisP., GrafL., KenessyA.Enhancement of low affinity [3H] GABA binding by diazepam and a new 2,3-benzodiazepine.Eur J Pharmacol1985; 109: 305–306.
52.
SkerrittJ.H., JohnstonG.Diazepam stimulates the binding of GABA and muscimol but not THIP to rat brain membranes.Neurosci Lett1983; 38: 315–320.
53.
KaijimaM., Le Gal La SalleG., RossierJ.The partial benzodiazepine agonist properties of RO 15–1788 in pentyle-metrazol-induced seizures in cats.Eur J Pharmacol1983; 93: 113–115.
HonoréT., NielsenM., BraestrupC.Barbiturate shift as a tool for determination of efficacy of benzodiazepine receptor ligands.Eur J Pharmacol1984; 100: 103–107.
59.
TickuM.K.Interaction of dePressant, convulsant, and anticonvulsant barbiturates with the [3H] diazepam binding site of the benzodiazepine-receptor-GABA-ionophore complex.Biochem Pharmacol1981; 30: 1573–1579.
60.
MaksayG., SimonyM.Benzodiazepine anticonvulsants accelerate and β-carboline convulsants decelerate the kinetics of [35S] TBPS binding at the chloride ionophore.Eur J Pharmacol1985; 117: 275–278.
61.
MaksayG., TickuM.K.Dissociation of [35S] T-butylbicyclophosphorothionate binding differentiates convulsant and depressant drugs that modulate GABAergic transmission.J Neurochem1985; 44: 480–486.
62.
EnnaS.J., MohlerH.Gamma-aminobutyric acid (GABA) receptor and their association with benzodiazepine recognition sites. In: MeltzerH.Y., ed. Psychopharmacology: the third generation of progress.New York: Raven Press, 1987: 268.
63.
MohlerH., SchochP., RichardsJ.G.Monoclonal antibodies: probes for structure and location of the GABA receptor/benzodiazepine receptor/chloride channel complex. In: OlsenR.W., VenterJ.C., eds. Benzodiazepine/GABA receptors and chloride channels.New York: Alan R Liss, 1986: 285–298.
EnnaS.J., MohlerH.Gamma-aminobutyric acid (GABA) receptors and thin association with benzodiazepine recognition sites. In: MeltzerH.Y., ed. Psychopharmacology: the third generation of progress.New York: Raven Press, 1987: 265–272.
66.
HaringP., StahliC., SchochP.Monoclonal antibodies reveal structural homogeneity of gamma-aminobutyric/benzodiazepine receptors in different brain areas.Proc Natl Acad Sci U S A1985; 82: 4837–4841.
67.
SchochP., RichardsJ.G., HaringP.Co-localisation of GABA A receptors and benzodiazepine receptors in the brain shown by monoclonal antibodies.Nature1985; 314: 168–171.
68.
HamonM.Les récepteurs du GABA dans le système nerveux central. Aspects biochimiques et pharmacologiques.L'Encéphale1987; XIII: 159–163.
69.
VillarH.O., UyenoE.T., TollL.Molecular determinants of benzodiazepines receptor affinities and anticonvulsant activities.Mol Pharmacol1990; 36: 589–600.
