High non-specific binding of the β1-selective radioligand 2-125I-ICI-H

NuklearMedizin

Volumn 42, Issue 4, 2003, Pages 173-180

  Riemann, Burkhard ^c   Law, M P ^a   Kopka, K ^c   Wagner, St ^c   Luthra, S ^a   Pike, V W ^b   Neumann, J ^c   Kirchhefer, U ^c   Schmitz, W ^c   Schober, O ^c   Schafers M ^c  

^a HAMMERSMITH HOSPITAL   (United Kingdom)

^b NATIONAL INSTITUTE OF MENTAL HEALTH   (United States)

^c NONE

Author keywords

Cordiac imaging; PFT; SPECT; 1 adrenoceptor radioligands

Indexed keywords

1 (2 CYANOPHENOXY) 3 [2 (3 PHENYLUREIDO)ETHYLAMINO] 2 PROPANOL; 4 (3 TERT BUTYLAMINO 2 HYDROXYPROPOXY) 2 BENZIMIDAZOLONE; BETA 1 ADRENERGIC RECEPTOR; CYANOPINDOLOL I 125; IODINE 125; N [2 [3 (2 IODOPHENOXY) 2 HYDROXYPROPYLAMINO]ETHYL] N' PHENYLUREA I 125; N [2 [3 (2 TRIMETHYLSILYLPHENOXY) 2 HYDROXYPROPYLAMINO]ETHYL N' PHENYLUREA; RADIOLIGAND; TRACER; TRITIUM; UNCLASSIFIED DRUG; 2 I ICI H; 2-I-ICI-H; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; BIPHENYL DERIVATIVE; PROPANOLAMINE DERIVATIVE; RADIOPHARMACEUTICAL AGENT;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BINDING COMPETITION; BINDING KINETICS; CONTROLLED STUDY; DRUG CLEARANCE; DRUG DISTRIBUTION; HEART DISEASE; HEART VENTRICLE; IN VITRO STUDY; IN VIVO STUDY; LIGAND BINDING; MALE; MOUSE; NONHUMAN; POSITRON EMISSION TOMOGRAPHY; RAT; RECEPTOR AFFINITY; SINGLE PHOTON EMISSION COMPUTER TOMOGRAPHY; ANIMAL; COMPUTER ASSISTED EMISSION TOMOGRAPHY; DBA MOUSE; HEART; METABOLISM; METHODOLOGY; PHYSIOLOGY; RADIOASSAY; REPRODUCIBILITY; SENSITIVITY AND SPECIFICITY;

ADRENERGIC BETA-ANTAGONISTS; ANIMALS; BINDING, COMPETITIVE; BIPHENYL COMPOUNDS; HEART; MICE; MICE, INBRED DBA; PROPANOLAMINES; RADIOLIGAND ASSAY; RADIOPHARMACEUTICALS; RATS; RECEPTORS, ADRENERGIC, BETA-1; REPRODUCIBILITY OF RESULTS; SENSITIVITY AND SPECIFICITY; TOMOGRAPHY, EMISSION-COMPUTED; TOMOGRAPHY, EMISSION-COMPUTED, SINGLE-PHOTON;

EID: 0042326745     PISSN: 00295566     EISSN: None     Source Type: Journal    
DOI: 10.1055/s-0038-1625187     Document Type: Article

References (39)

1. Arch JR, Ainsworth AT, Cawthorne MA et al. Atypical β-adrenoceptor on brown adipocytes as target for anti-obesity drugs. Nature 1984; 309: 163-5.
2. Bond RA, Clarke DE. Agonist and antagonist characterization of a putative adrenoceptor with distinct pharmacological properties from the alpha- and beta-subtypes. Br J Pharmacol 1988; 95: 723-34.
3. 2-adrenoceptors in the human heart: properties, function, and alteration in chronic heart failure. Pharmacol Rev 1991; 43: 203-42.
4. Brodde OE, Michel MC. Adrenergic and muscarinic receptors in the human heart. Pharmacol Rev 1999; 51: 651-90.
5. Cheng Y, Prusoff WH. Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition of an enzymatic reaction. Biochem Pharmacol 1973; 22: 3099-108.
6. DeLean A, Hancock AA, Lefkowitz RJ. Validation and statistical analysis of radioligand binding data for mixtures of pharmacological receptor subtypes. Mol Pharmacol 1982; 21: 5-16.
7. Dubois EA, Somsen GA, van den Bos JC et al. Development of radioligands for the imaging of cardiac beta-adrenoceptors using SPECT. Part II: Pharmacological characterization in vitro and in vivo of new n3I 1231-labelled beta-adrenoceptor antagonists. Nucl Med Biol 1997; 24: 9-13.
8. 18F]fluoro-CGP 12388) for visualization of beta-adrenoceptors with positron emission tomography. J Med Chem 1997; 40: 3829-35.
9. 11C]CGP12388 and positron emission tomography. Eur J Pharmacol 2001; 433: 173-6.
10. 125I]Iodocyanopindolol, a new ligand for β-adrenoceptors: identification and quantification of subclasses of β-adrenoceptors in guinea pig. Naunyn Schmiedeberg's Arch Pharmacol 1981; 317: 277-85.
11. Erhardt PW, Woo CM, Matier WL et al. Ultrashort-acting β-adrenergic receptor blocking agents. 3. Ethylendiamine derivatives of (aryloxy)propanolamines having esters on the aryl function. J Med Chem 1983; 26: 1109-12.
12. 123I]iodobenzylguanidine for myocardial scintigraphy. Eur J Nucl Med 2000; 27: 302-7.
13. Law MP. Demonstration of the suitability of CGP 12177 for in vivo studies of β-adrenoceptors. Br J Pharmacol 1993; 109: 1101-9.
14. Majid PA, Schreuder JE, de Feyter PJ et al. Clinical, electrocardiographic, and hemodynamic effects of ICI 89,406, a new cardioselective beta-adrenoceptor antagonist with intrinsic sympathomimetic activity, in patients with angina pectoris. J Cardiovasc Pharmacol 1980; 2: 435-44.
15. 2+-AT-Pase in mice lacking the CREM gene. FASEB J 2002 (published online 10.1096/fj.02-0486fje).
16. Mutschler E. Arzneimittelwirkungen. Stuttgart: Wissenschaftliche Verlagsgesellschaft mbH, 1996; 292.
17. Nelder JM, Mead RA. Simple algorithm for function minimization. Comput J 1965; 7: 308-13.
18. Patent CH 605666. Verfahren zur Herstellung von Alkanolaminderivaten. Imperial Chemical Industries Limited, London (UK).
19. Pike VW, Law MP, Osman S et al. Selection, design and evaluation of new radioligands for PET studies of cardiac adrenoceptors. Pharm Acta Helv 2000; 74: 191-200.
20. Pitha J, Milecki J, Czajkowska T et al. β-adrenergic antagonists with multiple pharmacophores: persistent blockade of receptors. J Med Chem 1983; 26: 7-11.
21. Quast U, Vollmer KO. Binding of beta-adrenoceptor antagonists to rat and rabbit lung: special reference to levobunolol. Arzneimittelforschung 1984; 34: 579-84.
22. Riemann B, Schäfers M, Law MP et al. Radioligands for imaging myocardial α- and β-adrenoceptors. Nuklearmedizin 2003; 42: 4-9.
23. Scatchard G. The attraction of proteins for small molecules and ions. Ann NY Acad Sci 1949; 51: 660-72.
24. Schäfers M, Dutka D, Rhodes CG et al. Myocardial presynaptic and postsynaptic autonomic dysfunction in hypertrophic cardiomyopathy. Circ Res 1998; 82: 57-62.
25. Schäfers M, Lerch H, Wichter T et al. Cardiac sympathetic innervation in patients with idiopathic right ventricular outflow tract tachycardia. J Am Coll Cardiol 1998; 32: 181-6.
26. Schäfers M, Riemann B, Levkau B et al. Current status and future applications of cardiac receptor imaging with positron emission tomography. Nucl Med Commun 2002; 23: 113-5.
27. 11C]bisoprolol, a putative beta1-selective adrenoceptor radioligand. Neurochem Int 2001; 38: 169-180.
28. 2-adrenoceptors in the failing and nonfailing human heart. Eur J Clin Pharamcol 1992; 42: 607-12.
29. 2 subtypes. J Cardiothorac Vasc Anesth 1993; 7: 668-73.
30. Tumer N, Houck WT, Boehm C et al. Cardiac beta-adrenoceptor binding and characteristics with age following adrenal demedullation. Br J Pharmacol 1990; 99: 87-90.
31. 3H)- quinazolinone ([+/-]HX-CH 44) as a selective betal-adrenoceptor ligand for PET. Nucl Med Biol 1999; 26: 105-109.
32. Van den Bos JC, van Doremalen PA, Dubois EA et al. Development of radioligands for the imaging of cardiac beta-adrenoceptors using SPECT Part I: Asymmetric synthesis and structural characterization of five new iodine-containing beta-adrenoceptor antagonist derivatives. Nucl Med Biol 1997; 24: 1-7.
33. Van Waarde A, Meeder JG, Blanksma PK et al. Suitability of CGP 12177 and CGP 26505 for quantitative imaging of beta-adrenoceptors. Int J Rad Appl Instrum B 1992; 19: 711-718.
34. Van Waarde A, Meeder JG, Blanksma PK et al. Uptake of radioligands by rat heart and lung in vivo: CGP 12177 does and CGP 26505 does not reflect binding to β-adrenoceptors. Eur J Pharmacol 1992; 222: 107-112.
35. 18F]fluorocarazolol in intact rats reflects radioligand binding to β-adrenoceptors. Eur J Pharmacol 1995; 272: 159-168.
36. 18F]fluorocarazolol. J Nucl Med 1997; 38: 934-939.
37. 11C]formoterol and positron emission tomography. Eur J Pharmacol 1998; 361: 35-41.
38. Wichter T, Schäfers M, Rhodes CG et al. Abnormalities of cardiac sympathetic innervation in arrhythmogenic right ventricular cardiomyopathy: quantitative assessment of presynaptic norepinephrine reuptake and postsynaptic beta-adrenergic receptor density with positron emission tomography. Circulation 2000; 101: 1552-1558.
39. Wilbur DS, Stone WE, Anderson KW. Regiospecific incorporation of bromine and iodine into phenols using (trimethylsilyl)phenols derivates. J Org Chem 1983; 48: 1542-1544.