Characterization of binding sites for the ω3 receptor ligands [3H]PK11195 and [3H]RO5-4864 in human brain

European Journal of Pharmacology

Volumn 340, Issue 1, 1997, Pages 89-99

  Rao, V L Raghavendra ^a   Butterworth, Roger F ^a  

^a UNIVERSITY OF MONTREAL   (Canada)

Author keywords

3H PK11195; 3H RO5 4864; Benzodiazepine receptor, peripheral type; Brain, human

Indexed keywords

4' CHLORODIAZEPAM; ALCOHOL DERIVATIVE; BENZODIAZEPINE RECEPTOR; CLONAZEPAM; DIAZEPAM; DIETHYL PYROCARBONATE; N SEC BUTYL 1 (2 CHLOROPHENYL) N METHYL 3 ISOQUINOLINECARBOXAMIDE; PREGNENOLONE; RECEPTOR SUBTYPE;

AMINO ACID COMPOSITION; ARTICLE; AUTOPSY; BINDING SITE; BRAIN; BRAIN REGION; CEREBELLUM; CONTROLLED STUDY; DRUG RECEPTOR BINDING; HISTOCHEMISTRY; HUMAN; HUMAN TISSUE; IN VITRO STUDY; MUTATION; NORMAL HUMAN; OCCIPITAL CORTEX; PRIORITY JOURNAL; RECEPTOR DENSITY;

ALLOSTERIC REGULATION; BENZODIAZEPINES; BENZODIAZEPINONES; BINDING SITES; BINDING, COMPETITIVE; CLONAZEPAM; CONVULSANTS; DETERGENTS; DIAZEPAM; DITHIOTHREITOL; FEMALE; HISTIDINE; HUMANS; ISOQUINOLINES; LIGANDS; MALE; OCCIPITAL LOBE; RECEPTORS, GABA-A; SULFHYDRYL REAGENTS; TRITIUM;

EID: 0031553386     PISSN: 00142999     EISSN: None     Source Type: Journal    
DOI: 10.1016/S0014-2999(97)01395-2     Document Type: Article

References (43)

1. Anholt R.R.H., Pedersen P.L., DeSouza E.B., Snyder S.H. The peripheral-type benzodiazepine receptor: Localization to the mitochondrial outer membrane. J. Biol. Chem. 261:1986;576-583.
2. Antkiewicz-Michaluk L., Guidotti A., Krueger K.E. Molecular characterization and mitochondrial density of a recognition site for peripheral-type benzodiazepine ligands. Pharmacology. 34:1988;272-278.
3. 3H ]PK11195 to cerebral cortex and peripheral tissues of various species: Species differences and heterogeneity in peripheral benzodiazepine binding sites J. Neurochem. 49:1987;1407-1414.
4. 3H ]PK11195 binding to peripheral-type benzodiazepine-binding sites Life Sci. 43:1988;167-175.
5. Awad M., Gavish M. Peripheral-type benzodiazepine receptors in human cerebral cortex, kidney and colon. Life Sci. 49:1991;1155-1161.
6. Barnard E.A., Bible G., Houamed K., Moss S.J., Van Renterghem C., Smart T.G. Functional expression in the Xenopus oocyte of messenger ribonucleic acids encoding brain neurotransmitter receptors: Further characterization of the implanted GABA receptors. Neuropharmacology. 26:1987;837-844.
7. 3H -PK11195, an isoquinoline carboxamide derivative: Kinetic studies and autoradiographic localization J. Neurochem. 41:1983;1744-1750.
8. Benavides J., Begassat F., Phan T., Tur C., Uzan A., Renault C., Dubroeucq M.C., Gueremy C., LeFur G. Histidine modification with diethylpyrocarbonate induces a decrease in the binding of an antagonist, PK11195, but not of an agonist, RO5-4864, of the peripheral benzodiazepine receptors. Life Sci. 35:1984;1249-1256.
9. 3 site ligand: a critical analysis of animal models of cerebral ischemia and neurodegeneration. Brain Res. 522:1990;275-289.
10. Bernassau J.M., Reversat J.L., Ferrara P., Caput D., LeFur G. A 3D model of the peripheral benzodiazepine receptor and its implication in intramitochondrial cholesterol transport. J. Mol. Graphics. 11:1993;236-244.
11. Blahos II J., Whalin M.E., Krueger K.E. Identification and purification of a 10 kDa protein associated with mitochondrial benzodiazepine receptors. J. Biol. Chem. 270:1995;20285-20291.
12. Braestrup C., Nielsen M. Multiple benzodiazepine receptors. Trends Neurosci. 3:1980;301-303.
13. Chang Y.J., McCabe R.T., Rennert H., Budarf M.L., Sayegh R., Emanuel B.S., Skolnick P., Strauss J.F. III The human 'peripheral-type' benzodiazepine receptor: regional mapping of the gene and characterization of the receptor expressed from cDNA. DNA Cell Biol. 11:1992;471-480.
14. 11C ]PK11195 in vivo after induction of a cortical ischemic lesion Int. J. Radiol. Appl. Instr. Part B Nucl. Med. and Biol. 19:1992;159-166.
15. Cymerman U., Pazo S.A., Palacios J.M. Evidence for species differences in 'peripheral' benzodiazepine receptors: An autoradiographic study. Neurosci. Lett. 66:1986;153-158.
16. Desjardins P., Bandeira P., Rao V.L.R., Ledoux S., Butterworth R.F. Increased expression of the peripheral-type benzodiazepine receptor-isoquinoline carboxamide binding protein in mRNA brain following portacaval anastomosis. Brain Res. 758:1997;255-258.
17. Doble A., Benavides J., Ferris O., Bertrand P., Menager J., Vaucher N., Burgevin M.-C., Uzan A., Gueremy C., LeFur G. Dihydropyridine and peripheral-type benzodiazepine binding sites: Subcellular distribution and molecular size determination. Eur. J. Pharmacol. 119:1985;153-167.
18. 3H ]PK11195: Anatomical and subcellular distribution Brain Res. Bull. 18:1987;49-61.
19. De Armond, S.J., Fusco, M.M., Dewey, M.M., 1976. Structure of human brain: A photographic atlas., 2nd ed. Oxford University Press, New York.
20. Ducis I., Norenberg L.-O.B., Norenberg M.D. The benzodiazepine receptor in the cultured astrocytes from genetically epilepsy-prone rats. Brain Res. 531:1990;318-321.
21. Earley B., Canney M., Clune B., Caldwell M., Leonard B., Junien J.-L. The effects of MK-801, ifenprodil, JO1784, JO1994 and JO1997 on PK11195 receptor binding, nitric oxide synthase (NO synthase) activity and infarct volume in a mouse model of focal cerebral ischemia. Neurochem. Int. 28:1996;509-521.
22. 3H ]RO5-4864 in trout and mouse brain membranes J. Neurochem. 53:1989;494-502.
23. Garnier M., Boujrad N., Ogwuegbu S.O., Hudson J.R., Papadopoulos V. The polypeptide diazepam-binding inhibitor and a higher affinity mitochondrial peripheral-type benzodiazepine receptor sustain constitutive steroidogenesis in the R2C Leydig tumor cell line. J. Biol. Chem. 269:1994;22105-22112.
24. Gavish M., Katz Y., Bar-Ami S., Weizman R. Biochemical, physiological and pathological aspects of the peripheral benzodiazepine receptors. J. Neurochem. 58:1992;1589-1601.
25. 3H ]PK11195 in rat brain following portacaval anastomosis Brain Res. 585:1992;295-298.
26. 2. J. Neurochem. 46:1986;804-811.
27. Itzhak Y., Norenberg M.D. Regulation of peripheral-type benzodiazepine receptors in cultured astrocytes by monoamines and amino acid neurotransmitters. Brain Res. 660:1994;346-348.
28. Itzhak Y., Baker L., Norenberg M.D. Characterization of the peripheral-type benzodiazepine receptors in cultured astrocytes: Evidence for multiplicity. Glia. 9:1993;211-218.
29. Itzhak Y., Roig-Cantisano A., Norenberg M.D. Ontogeny of peripheral-type benzodiazepine receptors in cultured astrocytes and brain from rat. Dev. Brain Res. 84:1995;62-66.
30. Junck L., Olson J.M.M., Ciliax B.S., Koeppe R.A., Watkins G.L., Jewett D.M., McKeever P.E., Wieland D.M., Kilbourn M.R., Starosta-Rubinstein S., Manoni W.R., Kuhl D.E., Greenberg H.S., Young A.B. PET imaging of human gliomas with ligands for the peripheral benzodiazepine binding sites. Ann. Neurol. 26:1989;752-758.
31. Lavoie J., Pomier Layrargues G., Butterworth R.F. Increased densities of peripheral-type benzodiazepine receptors in brain autopsy samples from cirrhotic patients with hepatic encephalopathy. Hepatology. 11:1990;874-878.
32. 3H ]PK11195 in vulnerable regions of the rat brain in thiamine deficiency encephalopathy J. Cerebr. Blood Flow Metab. 14:1994;100-105.
33. Lueddens H.W.M., Skolnick P. 'Peripheral-type' benzodiazepine receptors in the kidney: regulation of radioligand binding by anions and DIDS. Eur. J. Pharmacol. 133:1987;205-214.
34. Lowry O.H., Rosebrough N.J., Farr A.L., Randall R.J. Protein measurement with the Folin phenol reagent. J. Biol. Chem. 193:1951;265-275.
35. Möhler H., Okada T. Benzodiazepine receptor: Demonstration in central nervous system. Science. 198:1977;849-851.
36. Papadopoulos V., Amiri H., Boujrad N., Cascio C., Culty M., Garnier M., Hardwich M., Li H., Vidic B., Brown A.S., Reversa J.L., Bernassau J.M., Drieu K. Peripheral benzodiazepine receptor in cholesterol transport and steroidogenesis. Steroids. 62:1997;21-28.
37. 3H ]PK11195 in congenital ornithine transcarbamylase-deficient sparse fur mouse Pediatr. Res. 34:1993;777-780.
38. 3H ]PK11195 in rats following portacaval anastomosis Dig. Dis. Sci. 39:1994;1055-1063.
39. 3H ]nitroarginine binding sites in rat brain cerebellum J. Neurochem. 66:1996;701-709.
40. Sprengel R., Werner P., Seebury P.H., Mukhin A.G., Santi M.R., Grayson D.R., Guidotti A., Krueger K.E. Molecular cloning and expression of cDNA encoding a peripheral-type benzodiazepine receptor. J. Biol. Chem. 264:1989;20415-20421.
41. Stocco D.M., Clark B.J. Regulation of the acute production of steroids in steroidogenic cells. Endocrine Rev. 17:1996;221-244.
42. Skowronski R., Beaumont K., Fanestil D.D. Modification of the peripheral-type benzodiazepine receptor by arachidonate, diethylpyrocarbonate and thiol reagents. Eur. J. Pharmacol. 143:1987;305-314.
43. Wang J.K., Morgan J.I., Spector S. Benzodiazepines that bind at peripheral sites inhibit cell proliferation. Proc. Natl. Acad. Sci. 81:1984;753-756.