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Pharmacological implications for neuroreceptor imaging

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Abstract

Neuroreceptor imaging is increasing in nuclear medicine. New generations of radioligands will be developed that will allow us to study neurotransmitter systems not studied before. In data interpretation, however, links will have to be made with the number of counts acquired in the image and the real radioactivity in the brain and then, via the specific activity (and known metabolic characteristics), with the concentration of the ligand. From this point, links will have to be made, via kinetic modelling, with receptor density and, if possible, with receptor affinity, with the final link with brain function at a neurophysiological level. In this article several properties of receptor pharmacology and function are discussed that might help with the interpretation. It is argued that there is a complex relationship between the data, as is apparent in the images recorded and the underlying pharmacology of the receptor. Caution should be exercised, however, when in drawing conclusions about the receptor status and the possible implications on pathyphysiology.

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References

  • Ali H, Rousseau J, Van Lier JE (1990) 7-Alpha-methyl and 11 beta-ethoxy derivatives of [125I]16 alpha-iodoestradiol: effect on estrogen receptor-mediated target tissue uptake. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29 1190, pp 451–453 (abstract)

    Google Scholar 

  • Autillo-Touati A, Chamak B, Araud D, Vuillet J, Seite R, Prochiantz A (1988) Region-specific neuro-astroglial interactions: ultrastructural study of the in vitro expression of neuronal polarity. J Neurosci Res 19:326–342

    Google Scholar 

  • Banks WR, Yamakita H, Digenis GA (1990) Investigations on the in vivo stability and the biodistribution of alprazolam; a benzodiazepine receptor agonist. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29 1990, pp 242–244(abstract)

    Google Scholar 

  • Baron JC, Maziere B, Loc'h C, Cambon H, Sgoutopoulos P, Bonnet AM, Agid Y (1986) Loss of striatal [76Br] bromospiperone binding sites demonstrated by positron emission tomography in progressive supranuclear palsy. J Cereb Blood Flow Metab 6:131–136

    Google Scholar 

  • Barre L, Lasne MC, Camsonne R, Baron JC (1990) Synthesis of [11C]MDL 72222 as a potential radiopharmaceutical for the study of the 5-hydroxytryptamine 3 (5-HT3) receptor. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eights International Symposium of Radipharmaceutical Chemistry. Princeton University, Princeton, New Jersey USA, June 24–29 1990, pp 354 (abstract)

    Google Scholar 

  • Beer HF, Bläuenstein PA, Hasler PH, Delaloye B, Riccabona G, Bangerl I, Hunkeler W, Bonetti EP, Pieri L, Richards JG, Schubiger PA (1990) In vitro and in vivo evaluation of iodine-123-Ro 16–0154: a new imaging agent for SPELT investigations of benzodiazepine receptors. J Nucl Med 31:1007–1014

    Google Scholar 

  • Benwell MEM, Balfour DJK, Anderson JM (1988) Evidence that tobacco smoking increases the density of (−)-(3H)nicotine binding sites in human brain. J Neurochem 50:1243–1247

    Google Scholar 

  • Berridge MS, Terris AH, Vesselle JM (1990) [C-11]-Carazolol: a new labeled beta-adrenergic ligand. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A, (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey USA, June 24–29 1990, pp 359–360 (abstract)

    Google Scholar 

  • Biggio G, Corda MG (1990) GABAa receptor regulation after repeated administration of negative and positive modulators. Eur J Pharmacol 183:3

    Google Scholar 

  • Birnbaumer L, Abramowitz J, Brown AM (1990) Receptor-effector coupling by G proteins. Biochem Biophys Acta 1031:163–224

    Google Scholar 

  • Blomqvist G, Pauli S, Farde L, Eriksson L, Persson A, Halldin C (1990) Maps of receptor binding parameters in the human brain — a kinetic analysis of PET measurements. Eur J Nucl Med 16:257–265

    Google Scholar 

  • Bouthenet ML, Ruat M, Sales N, Garbarg M, Schwartz JC (1988) A detailed mapping of histamine H1-receptors in guinea-pig central nervous system established by autoradiography with [125I]iodobolpyramine. Neuroscience 26:553–600

    Google Scholar 

  • Brady F, Luthra SK, Tochon-Danguy H, Landais PG, Waters SL, Law M, Jaeggi KA, Pike VW (1990) Towards a chiral precursor for the automated radiosynthesis of carbon-11 labelled S-CGP 12177. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 258–260 (abstract)

    Google Scholar 

  • Brenner NJ, Burns HD, Solomon HF, Kinks J, Eng WS, Fioravanti C, Frost JJ, Karr D, Walkow J, Dannals RF (1990) Use of planar imaging for the study of drug delivery: the biodistribution of intravenously injected [C-11]MK-329. Eur J Nucl Med 16: S72 (abstract)

    Google Scholar 

  • Brodde OE (1989) β-Adrenoceptors. In: Williams M, Glennon RA, Timmermans PBMWM (eds) Receptor pharmacology and function. Dekker, New York, pp 207–255

    Google Scholar 

  • Brodde OE, Brinkmann M, Schemuth R, O'Hara N, Daul A (1985) Terbutaline-induced desensitization of human β2-adrenoceptors. Accelerated restoration of β2-adrenoceptor responsiveness by prednisone and ketotifen. J Clin Invest 76:1096–1101

    Google Scholar 

  • Bunzow JR, Van Tel HHM, Grandy DK, Albert P, Salon J, Christie M, Machida CA, Neve KA, Civelli O (1988) Cloning and expression of rat D2 dopamine receptor cDNA. Nature 336:783–787

    Google Scholar 

  • Cameron DL, Crocker AD (1990) Increased dopamine agonist sensitivity is accompanied by a decrease in striatal dopamine D2 receptor concentration in the hypothyroid rat. Eur J Pharmacol 183:1410–1411

    Google Scholar 

  • Cantineau R, Damhaut P, Plevenaux A, Lemaire C, Guillaume M (1990) Synthesis and preliminary animal studies of [131I]iodotroprapride: a cerebral dopamine D2 receptor ligand. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaccutical Chemistry. Princeton University, Princeton, New Jersey USA, June 24–29 1990, pp 368–369 (abstract)

    Google Scholar 

  • Chan SM, Basmadjian GP, Marten DF, Sadek SA, Magarian RA, Grunder JR (1984) Synthesis and biodistribution of radioiodinated nicotine and nicotine analogs. J Lab Comp Radiopharmacol 21:1107–1109

    Google Scholar 

  • Channing MA, Dunn BB, Boring DL, Jacobson KA (1990) Development of a F-18 labeled antagonist for the A1 adenosine receptor. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey USA, June 24–29 1990, pp 251 (abstract)

    Google Scholar 

  • Chase CR, Melson GL, Aurbach GD (1969) Pseudohypoparathyroidism: defective secretion of 3′,5′-cAMP in response to parathyroid hormone. J Clin Invest 48:1832–1844

    Google Scholar 

  • Chase TN, Mann U (1989) Cerebral muscarinic receptors in primary degenerative dementia as evaluated by SPELT with iodine-123 labeled QNB. In: Wurtmann RJ, Corkin S, Growdon JH, Ritter-Walker E (eds) Proceedings of the Fifth Meeting of the International Study Group on the Pharmacology of Memory Disorders Associated with Aging. Zurich, Switzerland, January 20–22 1989, pp 491–495

  • Chen JJ, Finn RD, Kiesewetter DO, Schmall B, Adams R, Plascjak P, Meyer W, Chiueh CC (1990) Synthesis of labelled diphentlethylenetropane with F-18 of C-11. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29 1990, pp 257 (abstract)

    MATH  Google Scholar 

  • Chesis PL, Welch MJ (1989) Sex dependent differences in N-3-(F18)-propyl diprenorphine distribution and metabolism. J Nucl Med 30:732 (abstract)

    Google Scholar 

  • Chumpradit S, Billings J, Kung MP, Pan S, Kung HF (1989) An improved CNS D-1 dopamine receptor imaging ligand: [I-123](+−)FISCH. J Nucl Med 30:803 (abstract)

    Google Scholar 

  • Chumpradit S, Billings J, Kung MP, Kung H (1990) R(+) and S(−)TISCH: new CNS D-1 dopamine receptor ligands. J Nucl Med 31:899 (abstract)

    Google Scholar 

  • Clow A, Theodorou A, Jenner P, Marsden CD (1980) Cerebral dopamine function in rats following withdrawal from one year of continuous neuroleptic administration. Eur J Pharmacol 63:145–157

    Google Scholar 

  • Collins S, Caron MG, Lefkowitz RJ (1988) Beta2-adrenergic receptors in hamster smooth muscle cells are transcriptionally regulated by glucocorticoids. J Biol Chem 263:9067–9070

    Google Scholar 

  • Costa DC, Verhoeff NPLG, Cullum ID, Ell PJ, Syed GMS, Barrett J, Palazidou E, Toone B, Van Royen EA, Bebeldijk M (1990) In vivo characterisation of 3-iodo-6-methoxybenzamide 123I in humans. Eur J Nucl Med 16:813–186

    Google Scholar 

  • Costentin J, Protais P, Schwartz JC (1975) Rapid and dissociated changes in sensitivities of different dopamine receptors in mouse brain. Nature 257:405–407

    Google Scholar 

  • Crawley JCW, Crow TJ, Johnstone EC, Oldland SRD, Owen F, Owens DGC, Smith T, Veall N, Zanelli GD (1986) Uptake of 77Br-spiperone in the striata of schizophrenic patients and controls. Nucl Med Biol 7:599–607

    Google Scholar 

  • Creese I, Sibley DR (1981) Receptor adaptations to centrally acting drugs. Ann Rev Pharmacol Toxicol 21:357–391

    Google Scholar 

  • Cresse I, Van Tol HHM, Riva M, Civelli O (1990) Lack of effect of chronic dopamine receptor blockade on D2 dopamine receptor mRNA levels. Eur J Pharmacol 183:1404

    Google Scholar 

  • Crouzel C, Prenant C, Comar D (1990) 11C-Labelling of Ohmefentanyl: an agonist for Mu-opiate receptor. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29 1990, pp 261 (abstract)

    Google Scholar 

  • DaSilva JN, Crouzel C (1990) Synthesis of NCA 11,17beta-dihydroxy-6-methyl-17alpha-(3-[18F]fluoroprop-1-ynyl)androsta-1,4,6-trien-3-one as a potential glucocorticoid receptor ligand for neuro-PET studies. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29 1990:247 (abstract)

    Google Scholar 

  • Delforge J, Janier M, Syrota A, Crouzel C, Vallois JM, Cayla J, Lancon JP, Mazoyer BM (1990) Noninvasive quantification of muscarinic receptors in vivo with positron emission tomography in the dog heart. Circulation 82:1494–1504

    Google Scholar 

  • De Vries CP, Van Haeften TW, Wieringa TJ, Van der Veen EA (1989) The insulin receptor. Diabetes Res 11:155–165

    Google Scholar 

  • Dewey SL, Bendriem B, MacGregor R, King P, Fowler JS, Christian DR, Schlyer DJ, Wolf AP, Volkow N, Brodie JD (1989) PET studies using I IC-cogentin in baboon brain. J Cereb Blood Flow Metab 9:1–13

    Google Scholar 

  • Dewey SL, Brodie JD, McGregor RR, Schlyer D, Bendriem B, King PT, Volkow N, Fowler JS, Wolf AP (1990) Effects of dopaminergic and scrotonergic blockade on the incorporation of [N-C-11-methyl]-benztropine in the baboon brain. J Nucl Med 31:780 (abstract)

    Google Scholar 

  • Di Paolo T, Falardeau P, Morisette M (1988) Striatal D-2 dopamine agonist binding sites fluctuate during the rat estrous cycle. Life Sci 43:665–672

    Google Scholar 

  • Drukarch B (1991) Biochemical aspects of signal transduction via D-2 dopamine receptors in the rat central nervous system. Thesis. Centrale Huisdrukkerij Vrije Universiteit Amsterdam, pp 1168

    Google Scholar 

  • Elands J, Barberis C, De Kloet ER, Jard S, De Wied D (1989) Radio-iodinated analogs for vasopressin and oxytocin receptors. In: Mertens J, Bossuyt-Piron C, (eds) Radio iodinated molecules for in vivo receptor mapping with SPELT. VUB-Jette October 19–20

  • Engel G, Hoyer D (1981) [1251]BE 2254, a new high affinity radioligand for alpha-1-adrenoceptors. Eur J Pharmacol 73:221–224

    Google Scholar 

  • Farde L, Wiesel FA, Stone-Elander S, Halldin C, Nordström AL, Hall H, Sedvall G (1990) D2 Dopamine receptors in neuroleptic-naive schizophrenic patients. Arch Gen Psychiatry 47:213–219

    Google Scholar 

  • Ferrarese C, Appollonio I, Frigo M, Gaini SM, Piolti R, Frattola L (1989) Benzodiazepine receptors and diazepam-binding inhibitor in human cerebral tumors. Ann Neurol 26:564–568

    Google Scholar 

  • Filer C, Hurt S, Wan YP (1989) Radioligands, synthesis and handling. In: Williams M, Glennon RA, Timmermans PBMWM (eds) Receptor pharmacology and function. Dekker, New York, pp 105–135

    Google Scholar 

  • Florijn WJ, De Boer T, Tonnaer JADM, Van Nispen JW, Versteeg DHG (1990) The in vitro binding of dopaminergic ligands to dopamine D-2 receptors is inhibited by ACTH/MSH-like peptides. Eur J Pharmacol 183:1407–1408

    Google Scholar 

  • Frangin Y, Chalon S, Caillet M, Foulon C, Desplanches G, Guilloteau D, Besnard JC (1990) Convenient synthesis of iodoethyl radiotracers: application to spiperone and spirotraxine derivatives. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey USA, June 24–29, pp 379–380 (abstract)

    Google Scholar 

  • Frey Ka, Koeppe RA, Mulholland GK, Kuhl DE (1990) Quantification of regional muscarinic receptors with the use of [C-11]tropanyl benzilate and positron emission tomography. J Nucl Med 31:779 (abstract)

    Google Scholar 

  • Frost JJ, Mayberg HS, Fisher RS, Douglass KH, Dannals RF, Links JM, Wilson AA, Ravert HT, Rosenbaum AE, Snyder SH, Wagner HN Jr (1988) Mu-opiate receptors measured by position emission tomography are increased in temporal lobe epilepsy. Ann Neurol 23:231–237

    Google Scholar 

  • Frost JJ, Sazdot B, Price J, Mayberg HS, Douglass KH, Dannals RF, Lever J, Links JM, Wilson AA, Ravert H, Wagner HN Jr (1989) Measurement of opiate receptor density (Bmax) and ligand affinity (Kd) in man using PET and C-11 diprenorphine at high and low specific activities. J Nucl Med 30:740–741 (abstract)

    Google Scholar 

  • Gibson RE, Schneidau TA, Cohen VI, Sood V, Ruch J, Melograna J, Eckelman WC, Reba RC (1989) In vitro and in vivo characteristics of [iodine-125]3-(R)-quinuclidinyl(S)-4-iodobenzilate. J Nucl Med 30:1079–1087

    Google Scholar 

  • Gildersleeve DL, Lin TY, Wieland DM, Ciliax BJ, Olson JMM, Young AB (1989) Synthesis of a high specific activity 125I-labeled analog of PK 11195, potential agent for SPECT imaging of the peripheral benzodiazepine binding site. Nucl Med Biol 16:423–429

    Google Scholar 

  • Gitler MS, Zeeberg BR, Reba RC (1990) In vivo [125I]-iodomelatonin (IMEL) specific binding to melatonin receptor (MELR) in rat brain. J Nucl Med 31:883 (abstract)

    Google Scholar 

  • Glennon RA (1989) Central serotonin receptors. In: Williams M, Glennon RA, Timmermans PBMWM (eds) Receptor pharmacology and function. Dekker, New York, pp 257–292

    Google Scholar 

  • Gysemans M, Mertens J (1990) Synthesis of p-F-o-l-phenyl ketone compounds, substrates for radio bromination, by Cu(I) assisted nucleophilic exchange. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 372 (abstract)

    Google Scholar 

  • Haefely WE (1990) Agonists, inverse agonists, and antagonists of benzodiazepine receptors. Eur J Pharmacol 183:38

    Google Scholar 

  • Hall H, Hogberg T, Halldin C, Kohler C, Strom P, Ross SB, Larsson SA, Farde L (1991) NCQ 298, a new selective iodinated salicylamide ligand for the labelling of dopamine D2 receptors. Psychopharmacology 103:6–18

    Google Scholar 

  • Halldin C, Farde L, Barnett A, Sedvall G (1990a) Synthesis of [11C]SCH 39166, a new selective D-1 dopamine receptor ligand for PET. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey USA, June 24–29 1990, pp 357–358 (abstract)

    Google Scholar 

  • Halldin C, Hogberg T, Bengtsson S, Hall H, Farde L (1990b) Preparation of [F-18]NCQ 115, a new selective reversible D-2 dopamine receptor ligand for PET. J Nucl Med 31:902 (abstract)

    Google Scholar 

  • Harden TK (1983) Agonist-induced desensitization of the β-adrenergic receptor-linked adenylate cyclase. J Pharmacol Exp Ther 35:5–32

    Google Scholar 

  • Hatazawa J, Hatano K, Itoh M, Ishiwata K, Ido T, Watanuki S, Seo S (1990) D2-Dopamine receptor specific binding in canine brain measured with C-11 YM-09151–2 using PET. J Nucl Med 31:779 (abstract)

    Google Scholar 

  • Hemmings HC, Nairn AC, McGuinness TL, Huganir RL, Greengard P (1989) Role of protein phophorylation in neuronal signal transduction. FASEB J 3:2125–2131

    Google Scholar 

  • Hirata F, Notsu Y, Yamada R, et al. (1985) Isolation and characterization of lipocortin (lipomodulin). Agents Actions 17:263–266

    Google Scholar 

  • Hosking DJ, Kerr D (1988) Mechanisms of parathyroid hormone resistance in pseudohypoparathyroidism. Clin Sci 74:561–566

    Google Scholar 

  • Hunter DH, Strickland LA, Zabel PL (1990) Synthesis and evaluation of three iodinated haloperidol derivatives as potential dopamine receptor imaging agents. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 373–374 (abstract)

    Google Scholar 

  • Innis RB, Al-Tikriti M, Woods SW, Zoghbi S, Roth RH, Charney DS, Heninger GR, Smith EO, Zubal IG, Alavi A, Hoffer PB, Kung HF (1990) SPECT imaging of the dopamine D2 receptor in primate brain. J Nucl Med 31:883 (abstract)

    Google Scholar 

  • Johnson LK, Longenecker JP, Baxter JD, Dallman MF, Widmaier EP, Eberhardt NL (1982) Glucocorticoid action: a mechanism involving nuclear and non-nuclear pathways. Br J Dermatol 107 [Suppl 23]:6–23

    Google Scholar 

  • Junck L, Olson JMM, Cihax BJ, Koeppe RA, Watkins GL, Jewett DM, McKeever PE, Wieland DM, Kilbourn MR, Starosta-Rubinstein S, Mancini WR, Kuhl DE, Greenberg HS, Young AB (1989) PET imaging of human gliomas with ligands for the peripheral benzodiazepine binding site. Ann Neurol 26:752–758

    Google Scholar 

  • Kawai R, Carson RE, Rice KC, Blasberg RG (1990a) Evaluation of methods to determine nonspecific tissue binding on Kd and Bmax estimates using the opiate receptor antagonist (−)-cyclofoxy [(−)CF] and equilibrium studies. J Nucl Med 31:810 (abstract)

    Google Scholar 

  • Kawai R, Charming M, Newman AH, Blasberg R (1990 b) Nonspecific brain tissue binding of the opiate antagonist (−)cyclofoxy [(−)CF] : regional variation and time dependency. J Nucl Med 883 (abstract)

  • Kessler RM, Votaw JR, De Paulis T, Schmidt D, Clanton JA, Ansari MS, Holdeman KP, Pfeffer R, Manning RG (1990) [1123]Labelled epidepride SPECT studies of dopamine D2 receptors in man. J Nucl Med 31:779 (abstract)

    Google Scholar 

  • Kiesewetter DO, Kawai R, Chelliah M, Owens E, McLellan C, Blasberg RG (1990) Preparation and biological evaluation of 18F-labeled benzamide analogs as potential dopamine D2 receptor ligands. Nucl Med Biol 17:347–356

    Google Scholar 

  • Kimelberg HK, Norenberg MD (1989) Astrocytes. Sci Am 260:4452

    Google Scholar 

  • Kinnier WJ (1989) Receptor-linked second messenger systems. In: Williams M, Glennon RA, Timmermans PBMWM (eds) Receptor pharmacology and function. Dekker, New York, pp 85–104

    Google Scholar 

  • Kinsey BM, Tewson TJ (1990) Fluorine-18 fluoroalkyl derivatives of carazolol: potential ligands for the in vivo studies of the beta-adrenergic receptor. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaccutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29 1990, pp 381 (abstract)

    Google Scholar 

  • Knudsen PJ, Dinarello CA, Strom TB (1987) Glucocorticoids inhibit transcriptional and posttranscriptional expression of interleukin 1 in U937 cells. J Immunol 139:4129–4134

    Google Scholar 

  • Kochanny MJ, Pomper MG, Carlson KE, Mathias CJ, Van Brocklin HF (1990) Imaging agents for embrain corticosteroid receptors: synthesis and tissue distribution of 21-[18F]fluoro-deacylcortivazol. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 248–250 (abstract)

    Google Scholar 

  • Koob GF, Bloom FE (1988) Cellular and molecular mechanisms of drug dependence. Science 242:715–723

    CAS  PubMed  Google Scholar 

  • Krogsgaard-Larsen P (1989) GABA receptors. In: Williams M, Glennon RA, Timmermans PBMWM (eds) Receptor pharmacology and function. Dekker, New York, pp 349–383

    Google Scholar 

  • Kung HF, Alavi A, Chang W, Kung MP, Keyes JW Jr, Velchik MG, Bilings J, Pan S, Noto R, Rausch A, Reilley J (1990) In vivo SPELT imaging of CNS D-2 dopamine receptors: initial studies with iodine-123-IBZM in humans. J Nucl Med 31:573–579

    Google Scholar 

  • Kung MP, Kung HF, Billings J, Yang Y, Murphy RA, Alavi A (1990) the characterization of IBF as a new selective dopamine D-2 receptor/imaging agent. J Nucl Med 31:648–654

    Google Scholar 

  • Lamberts SJW, Barker WH, Reubi JC, Krenning EP (1990) Somatostatin-receptor imaging in the localization of endocrine tumors. N Engl J Med 323:1246–1249

    Google Scholar 

  • Lamoureux G, Dupont RM, Gillin JC, Ashburn WL, Halpern SE, De Sherbrooke U, Quebec P (1990) A geomorphological description of the absolute uptake, cortical distribution and washout of I-13 iodoamphetamine (IMP) in a group of normal subjects. Eur J Nucl Med 16: S144 (abstract)

    Google Scholar 

  • Larsson C, Nilsson L, Halen A, Nordberg A (1986) Subchronic treatment of rats with nicotine: effects on tolerance and on 3H-acetylcholine and 3H-nicotine binding in the brain. Drug Alcohol Depend 17:37–45

    Google Scholar 

  • Le Breton C, Crouzel C (1990) Synthesis of [11C]ranitidine: a potential PET imaging agent for H2 receptors in heart. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, p 263 (abstract)

    Google Scholar 

  • Lefkowitz RJ, Hausdorff WP, Caron MG (1990) Role of phosphorylation in desensitization of the beta-adrenoceptor. Trends Pharmacol Sci 11:190–194

    Google Scholar 

  • Levine Ma, Downs RW Jr, Moses AM, et al. (1983) Resistance to multiple hormones in patients with pseudohypoparathyroidism. Association with a deficient activity of guanine nucleotide regulatory protein. Am J Med 74:545–556

    Google Scholar 

  • Leysen JE (1990) Biogenic amine receptor regulation: rules and exceptions. Eur J Pharmacol 183:2

    Google Scholar 

  • Liu A, Carlson KE, Katzenellenbogen JA, VanBrocklin HF, Mathias CJ, Welch MJ (1990) Androgen receptor-based imaging agents for the prostate: synthesis and tissue distribution studies with tritium and fluorine-18 labeled androgens. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 445–448 (abstract)

    Google Scholar 

  • Loc'h C, Mazière B, Stulzaft O, Bourguignon M, Valette H, Syrota A (1990) A-123 Prenalterol: a potential radiotracer for myocardial beta-adrenergic receptor studies by SPELT. J Nucl Med 31:899

    Google Scholar 

  • Lundberg JM (1990) Pharmacology of cotransmission. Eur J Pharmacol 183:156–157

    Google Scholar 

  • Luthra SK, Pascall C, Pike VW, Price GW, Ahier RG, Hume SP, MYers R, Manjil L, Cremer JE (1990a) The radiosynthesis of [18F]PK 14105 as an alternative radioligand for peripheral benzodiazepine binding sites. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey USA, June 24–29, 1990, pp 235–236 (abstract)

    Google Scholar 

  • Luthra SK, Turton DR, Dowsett K, Bateman DM, Kensett MJ, Waters SL, Pike VW (1990b) Improved and automated “one-pot” radiosyntheses of [11C]diprenorphine and [11C]Buprenorphine. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 264–265 (abstract)

    Google Scholar 

  • Mach RH, Ehrenkaufer RL, Luedtke RR, Nicklaus K, Molinoff PB, Reivich M (1990) Synthesis of [F-18]N-(4-fluorobenzyl)spiperone, a novel D2 receptor ligand for PET. J Nucl Med 31: 901

    Google Scholar 

  • Majewska MD, Harrison NL, Schwartz RD, Barker JL, Paul SM (1986) Steroid hormone metabolites are barbiturate-like modulators of the GABA receptor. Science 23:1004–1007

    Google Scholar 

  • Malenka RC, Kauer JA, Perkel DJ, Nicoll RA (1989) The impact of postsynaptic calcium on synaptic transmission: its role in long-term potentiation. Trends Neurosci 12:444–450

    Google Scholar 

  • Mathis CA, Bishop JE, Gerdes JM, Faggin B, Mailman R (1990a) Synthesis of aryl-substituted 5-[18F]fluoroalkylbenzamides: high affinity ligands for dopamine D-2 studies. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 365–367 (abstract)

    Google Scholar 

  • Mathis CA, Gerdes JM, Shulgin AT, Hanrahan S, Faggin B, Mailman R (1990b) Synthesis and evaluation of (S)-5-[125I]iodo-2,3-methylenedioxybenzamide. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, p 370 (abstract)

    Google Scholar 

  • Matsui H, Horikawa S, Suzuki N, Tsukada K, Hosoya T (1987) Effects of glucocorticoids and cycloheximide upon transcription of ribosomal RNA gene in rat liver: application of quantitative S1 nuclease mapping analysis. Cell Biol Int Rep 11:273–277

    Google Scholar 

  • Matsumura K, Uno Y, Scheffel U, Wilson AA, Dannals RF, Wagner HN Jr (1991) In vitro and in vivo characterization of 4-[125I]iododexetimide binding to muscarinic cholinergic receptors in the rat heart. J Nucl Med 32:76–80

    Google Scholar 

  • Maus M, Bertrand P, Drouva S, Rasolonjanahary R, Kordon C, Glowinski J, Premont J, Enjalbert A (1989) Differential modulation of D1 and D2 dopamine-sensitive adenylate cyclases by 17 beta-estradiol in cultured striatal neurons and anterior pituitary cells. J Neurochem 52:410–418

    Google Scholar 

  • Mazière B, Loc'h C, Bourguignon M, Chabriat H, Raynaud C, Levasseur M, Syrota A (1990) Imaging D2 receptors with SPELT and I-123 iodolisuride. Eur J Nucl Med 16:5112 (abstract)

    Google Scholar 

  • Mazière B, Mazière M (1990) Where have we got to with neuroreceptor mapping of the human brain? Eur J Nucl Med 16:817–835

    Google Scholar 

  • McKenna DJ, Nazarili AJ, Hoofman AJ, Nichols DE, Mathis CA, Saavedra CA (1989) Common receptors for hallucinogens in rat brain: a comparative autoradiographic study using [1251]LSD and [125I]DOI, a new psychotomimetic radioligand. Brain Res476:45–56

    Google Scholar 

  • McPherson GA (1989) A mathematical approach to receptor characterization. In: Williams M, Glennon RA, Timmermans PBMWM (eds) Receptor pharmacology and function. Dekker, New York, pp 47–84

    Google Scholar 

  • Melloni E, Pontremoli S (1989) The calpains. Trends Neurosci 12:438–444

    Google Scholar 

  • Mertens J, Bossuyt-Piron C, Bossuyt A (1990) Influence of the specific activity on the brain uptake of 2-radioiodo-ketanserin related to log P. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University; Princeton, New Jersey, USA, June 24–29, 1990, p 375 (abstract)

    Google Scholar 

  • Miller JC, Friedhoff AJ (1988) Prenatal neurotransmitter programming of postnatal receptor function. Prog Brain Res 73:509–522

    Google Scholar 

  • Miller LG, Greenblatt DJ, Barnhill JG, Summer WR, Shader RI (1988) ‘GABA shift’ in vivo: enhancement of benzodiazepine binding in vivo by modulation of endogenous GABA. Eur J Pharmacol 148:123–130

    Google Scholar 

  • Moerlein SM (1990) N-omega-[F-18]fluoroalkylated flumazenil: potential agents for mapping cerebral benzodiazepine receptors with PET. J Nucl Med 31:902 (abstract)

    Google Scholar 

  • Moody TW, Perry DC (1989) Peptide receptors. In: Williams M, Glennon RA, Timmermans PBMWM (eds) Receptor pharmacology and function. Dekker, New York, pp 527–570

    Google Scholar 

  • Murphy S, Pearce B (1987) Functional receptors for neurotransmitters on astroglial cells. Neuroscience 22:381–394

    Google Scholar 

  • Numa S (1990) Structure and function of neurotransmitter receptors and ionic channels. Eur J Pharmacol 183:157–158

    Google Scholar 

  • Nybäck H, Nordberg A, Langström B, Halldin C, Hartvig P, Ahlin A, Swahn CG, Sedvall G (1989) Attempts to visualize nicotinic receptors in the brain of monkey and man by positron emission tomography. In: Nordberg A, Fuxe K, Holmstedt B, Sundwall A (eds) Nicotinic receptors in the CNS. Their role in synaptic transmission. Progress in Brain Research, vol 79. Elsevier Science (Biomedical Division), Amsterdam New York, pp 313–319

    Google Scholar 

  • Oswald RE, Freeman JA (1981) Alpha-bungarotoxin binding and central nervous system nicotinic acetylcholine receptors. Neuroscience 6:1–14

    Google Scholar 

  • Overstreet DH, Yamamura HI (1979) Receptor alterations and drug tolerance. Life Sci 25:1865–1878

    Google Scholar 

  • Persson A, Ehrin E, Eriksson L, Farde L, Hedstrom CG, Litton JE, Mindus P, Sedvall G (1985) Imaging of (11C)-labelled Ro 15–1788 binding to benzodiazepine receptors in the human brain by positron emission tomography. J Psychiat Res 19:609–622

    Google Scholar 

  • Potts J (1987) Pseudohypoparathyroidism. In: Harrison's Principles of Internal Medicine, XIth edn. McGraw-Hill, New York, pp 1886–1889

    Google Scholar 

  • Putney JW Jr, Takemura H, Hughes AR, Horstman DA, Thastrup O (1989) How do inositol phosphates regulate calcium signalling? FASEB J 3:1899–1905

    Google Scholar 

  • Quik M, Spokes EG, Mackay AVP, Bannister R (1979) Alterations in [3H]spiperone binding in human caudate nucleus, substantia nigra and frontal cortex in the Shy-Drager syndrome and Parkinson's disease. J Neurol Sci 43:429–437

    Google Scholar 

  • Quivy J, Zeicher M, Delcorde A, Henrot P, Deblaton M, Pirotte R, Verbist A, Fruhling J (1990) Z-11 beta-chloromethyl-127 alpha-iodovinyl estradiol, a very high affinity estrogen for radioimaging and targetted radiotherapy of estrogen receptor (ER) positive tumors. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 454–455 (abstract)

    Google Scholar 

  • Rasmussen CD, Means AR (1989) Calmodulin, cell growth and gene expression. Trends Neurosci 12:433–438

    Google Scholar 

  • Reisine T (1981) Adaptive changes in catecholamine receptors in the central nervous system. Neuroscience 6:1471–1502

    Google Scholar 

  • Reithmann C, Gierschik P, Müller U, Werdan K, Jakobs KH (1990) Pseudomonas exotoxin A prevents β-adrenoceptor-induced up-regulation of Gi protein α-subunits and adenylyl cyclase desensitization in rat heart muscle cells. Molec Pharmacol 37:631–638

    Google Scholar 

  • Rinne JO (1987) Muscarinic and dopaminergic receptors in the aging human brain. Brain Res 404:162–168

    Article  CAS  PubMed  Google Scholar 

  • Romanelli L, Ohman B, Adem A, Nordberg A (1988) Subchronic treatment of rats with nicotine: interconversion of nicotinic receptor subtypes in brain. Eur J Pharmacol 148:289–291

    Google Scholar 

  • Saito N, Guitart X, Hayward M, Tallman JF, Duman RS, Nestler EJ (1989) Corticosterone differentially regulates the expression of Gs alpha and Gi alpha messenger RNA and protein in rat cerebral cortex. Proc Natl Acad Sci USA 86:3906–3910

    Google Scholar 

  • Saji H, Nakatsuka I, Iida Y, Magata Y, Yoshitake Y, Konishi J, Yokoyama A (1989) Radioiodinated diazepam derivative for SPECT studies of benzodiazepine receptor. J Nucl Med 30:803–804 (abstract)

    Google Scholar 

  • Savič I, Roland P, Sedvall G, Persson A, Pauli S, Widen L (1988) In-vivo demonstration of reduced benzodiazepine receptor binding in human epileptic foci. Lancet 11: 863–866

    Google Scholar 

  • Seeman P (1980) Brain dopamine receptors. Pharmacol Rev 32:229–313

    Google Scholar 

  • Seeman P, Bzowej NH, Guan HC, Bergeron C, Becker LE, Reynolds GP, Bird ED, Riederer P, Jellinger K, Watanabe S, Tourtelotte WW (1987) Human brain dopamine receptors in children and aging adults. Synapse 1:399–404

    CAS  PubMed  Google Scholar 

  • Snyder SH (1990) Neural receptors and psychotropic drugs. Eur J Pharmacol 183:19–20

    Google Scholar 

  • Spiegel A (1989) Pseudohypoparathyroidism. In: Scriver CR (ed) The metabolic basis of inherited disease, pp 2021–2027

  • Suchiro M, Dannals RF, Scheffel U, Stathis M, Wilson AA, Ravert HT, Villemagne VL, Wagner HN Jr (1990) In vivo labeling of dopamine D2 receptors with N-11C-methyl-benperidol. J Nucl Med 31:882 (abstract)

    Google Scholar 

  • Suhara T, Fukada H, Inoue O, Itch T, Suzuki K, Tateno Y (1991) Age-related changes in human D1 dopamine receptors measured by positron emission tomography. Psychopharmacology 103:41–45

    CAS  PubMed  Google Scholar 

  • Tewson TJ, Kinsey BM, Franceschini MP (1990) Synthesis of fluorine-18 fluoroalkyl pindolol derivatives: ligands for the betaadrenergic receptor. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 394–395 (abstract)

    Google Scholar 

  • Thonoor CM, Couch MW, Greer DM, Thomas KD, Williams CM (1988) Biodistribution and radiation dosimetry of radioiodinated-SCH 23982, a potential dopamine D-1 receptor imaging agent. J Nucl Med 29:1668–1674

    Google Scholar 

  • Titeler M (1989) Receptor binding theory and methodology. In: Williams M, Glennon RA, Timmermans PBMWM (eds) Receptor pharmacology and function. Dekker, New York, pp 17–45

    Google Scholar 

  • VanBrocklin HF, Welch MJ, Brodack JW, Mathias CJ, Pomper Mg, Carlson KE, Katzenellenbogen JA (1990) Fluorine-18 labeled estrogens: synthesis and biological evaluation of 11beta and l7alpha substituted estradiols. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29, 1990, pp 438–440 (abstract)

    Google Scholar 

  • Van Tol HHM, Riva M, Civelli O, Creese I (1990) Lack of effect of chronic dopamine receptor blockade on D2 dopamine receptor mRNA level. Neurosci Lett 111:303–308

    Google Scholar 

  • Verhoeff NPLG, Van Royen EA, Overweg J, Limburg M, Hijdra A, Linszen D (1990) 123I-Iomazenil whole body distribution in human volunteers. Eur J Nucl Med 16:461 (abstract)

    Google Scholar 

  • Verhoeff NPLG, Costa DC, Ell PJ, Toone B, Palasidou E, Cullum ID, Bobeldijk M, Miller R, Syed GMS, Barrett JJ, Soricelli A, Van Royen EA (1991a) Dopamine D2-receptor imaging with dynamic 123I-IBZM SPET in patients with schizophrenia or HIV encephalopathy. In: Schmidt HAE, Van der Schoot JB (eds) Nuclear medicine. The state of the art of nuclear medicine in Europe. European Nuclear Medicine Congress, Amsterdam, May 20–24, 1990. Schattauer, Stuttgart New York, pp 207–212

    Google Scholar 

  • Verhoeff NPLG, Van Royen EA, Ell PJ, Costa DC, Hasler PH, Schubiger PA (1991b) Benzodiazepine receptor density in human brain measured in vivo with.123I-Iomazenil SPELT. n: Schmidt HAE, Van der Schoot JB (eds) Nuclear medicine. The state of the art of nuclear medicine in Europe. European Nuclear Medicine Congress, Amsterdam, May 20–24, 1990. Schattauer, Stuttgart New York, pp 203–206

    Google Scholar 

  • Villemagne V, Dannals RF, Sanchez Roa P, Ravert HT, Vazquez S, Wilson AA, Natarajan TK, Murrell M, Wong DF, Yanai K, Wagner HN Jr (1989) Imaging histamine H1 receptors in the baboon brain by positron emission tomography (PET). J Nucl Med 30:741 (abstract)

    Google Scholar 

  • Vogt PK, Bos TJ (1989) The oncogene jun and nuclear signalling. TIBS 14:172–175

    Google Scholar 

  • Vos PE, Bleumink GJ, Van Ree JM (1990) The ACTH-(4–9) analogue ORG 2766 and supersensitivity after a unilateral 6-OHDA lesion of the corpus striatum in rats. Eur J Pharmacol 183:1419–1420

    Google Scholar 

  • Wieland DM, Kilbourn MR, Yang DJ, Laborde E, Gildersleeve DL, Van Dort ME, Pirat JL, Ciliax BJ, Young AB (1988) NMDA receptor channels: labeling of MK-801 with iodine-125 and fluorine-18. Appl Rad Isot 39:1219–1225

    Google Scholar 

  • Wilkström AC, Bakke O, Okret S, et al. (1987) Intracellular localization of the glucocorticoid receptor: evidence for cytoplasmic and nuclear localization. Endocrinology 120:1232–1242

    Google Scholar 

  • Wilson AA, Dannals RF, Ravert HT, Wagner HN Jr (1990a) 1-(4[11C]-methoxyphenyl)-3-(1-adamantyl)guanidine: a potential radiotracer for PET imaging of sigma receptors. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29 1990, pp 266–268 (abstract)

    Google Scholar 

  • Wilson AA, Scheffel U, Stathis M, Dannals RE, Ravert HT, Wagner HN Jr (1990b) Synthesis and biodistribution of two I-125 labelled sigma receptor ligands. J Nucl Med 31:797

    Google Scholar 

  • Wong DF, Wagner HN Jr, Dannals RF, Links JM, Frost JJ, Ravert HT, Wilson AA, Rosenbaum AE, Gjedde A, Douglass KH, Petronis JD, Folstein MF, Tung JKT, Burns D, Kuhar MJ (1984) Effects of age on dopamine and serotonin receptors measured by positron tomography in living human brain. Science 226:1393–1396

    Google Scholar 

  • Wong DF, Wagner HN Jr, Tune LE, Dannals RF, Pearlsson GD, Links JM, Tamminga CA, Broussole EP, Ravert HT, Wilson AA, Toung JKT, Malat J, Williams JA, O'Tuama LA, Snyder SH, Kuhar MJ, Gjedde A (1986) Positron emission tomography reveals elevated D2 dopamine receptors in drug-naive schizophrenics. Science 234:1558–1563

    Google Scholar 

  • Wong DF, Minkin E, Wilson AA, Young LT, Dannals RF, Ravert HT, Wagner HN Jr (1990) In vivo studies of D2 dopamine receptors with C-11 and I-125 iodobenzamide. J Nucl Med 31:882 (abstract)

    Google Scholar 

  • Yang D, Emran A, Tansey W, Tilbury R, Kasi L, Wright K, Kuang L, Walace S, Kim E (1990) Radiosynthesis of fluorotamoxifen analogs. J Nucl Med 31:903 (abstract)

    Google Scholar 

  • Yonekura Y, Iwasaki Y, Saji H, Iida Y, Tamaki N, Fujita T, Matoba N, Konishi J, Yokoyama A (1990) SPELT imaging of dopamine D-2 receptor: kinetics of I-123 2′-iodospiperone in normal subjects. J Nucl Med 31:885 (abstract)

    Google Scholar 

  • Yorke JC, Prenant C, Crouzel C (1990) Synthesis of carbon-11 labelled cyclopentyltheophylline: a radioligand for PET studies of adenosine receptors. In: Eckelman WC, Kseniak D, Kuczynski B, Nunn A (eds) Eighth International Symposium of Radiopharmaceutical Chemistry. Princeton University, Princeton, New Jersey, USA, June 24–29 1990, p 269 (abstract)

    Google Scholar 

  • Zhengpin G, Tianzhi T (1990) Radioiodinated alpha-butylhydroxybenzyl alcohol as a potential agent for benzodiazepine receptor imaging. Eur J Nucl Med 16:103 (abstract)

    Google Scholar 

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Verhoeff, N.P.L.G. Pharmacological implications for neuroreceptor imaging. Eur J Nucl Med 18, 482–502 (1991). https://doi.org/10.1007/BF00181287

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