Abstract
N-Isopropyl-p-iodoamphetamine (IMP) receptors in normal human lung tissue were characterized using a radioligand binding assay with iodine-125 IMP as the ligand. Saturation binding studies revealed the presence of two binding sites with dissociation constant (K d) values of 53 ± 2 and 4687 ± 124 nM and maximum binding capacity (Bmax) values of 7 ± 1 and 133 ± 27 pmol/mg protein (n=5) respectively. The IC50 values of various amines were as follows: IMP, 9 × 10−5 M; propranolol, 5 × 10−4 M; haloperidol, 6 × 10−4 M; ketamine, 9 × 10−3 M; dopamine, 1 × 10−2 M. The IMP receptors of cancerous tissue obtained from human lung also had two binding sites with K d values of 54 ± 2 and 5277 ± 652 nM and Bmax values of 7±1 and 103 ± 21 pmol/mg protein (n = 3) respectively. There was no significant difference in binding parameters between normal and cancerous lung tissue. These results demonstrate the existence of IMP receptors and suggest that cancer does not affect the nature of IMP receptors in human lung tissue.
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Winchell HS, Baldwin RM, Lin TH. Development of I-123-labeled amines for brain studies. J Nucl Med 1980; 21:940–946.
Winchell HS, Horst WD, Braun L, Oldendorf WH, Hattner R, Parker H. N-Isopropyl-[123I]p-iodoamphetamine: single-pass brain uptake and washout; binding to brain synaptosomes; and localization in dog and monkey brain. J Nucl Med 1980; 21:947–952.
Touya JJ, Akber SF, Rahimian J, Benett LR. Metabolic lung scanning with N-isopropyl-I-123-p-iodoamphetamine. Nucl Med Biol 1982; 2554–2557.
Rahimian J, Glass EC, Touya JJ, Akber SF, Graham LS, Bennett LR. Measurement of metabolic extraction of tracers in the lung using a multiple indicator dilution technique. J Nucl Med 1984; 25:31–37.
Touya JJ, Rahimian J, Grubbs DE, Corbus HF. A noninvasive procedure for in vivo assay of a lung amine endothelial receptor. J Nucl Med 1985; 26:1302–1307.
Akber SF. Demonstration and quantitation of pharmacological inhibition of pulmonary uptake of N-isopropyl-123I-p-iodo-amphetamine by propranolol. Nucl Med 1989; 28:100–104.
Fowler JS, Gallagher BM, Macgregor RR. Radiopharmaceuticals XIX. 11C-labeled octylamine, a potential diagnostic agent for lung structure and function. J Nucl Med 1976; 17:752–754.
Moretti JL, Holman BL, Delmon L, Carmel A, Johnson D, Moingeon P, Blau M. Effect of anti-depressant and narcoleptic drugs on N-isopropyl-p-iodoamphetamine biodistribution in animals. J Nucl Med 1987; 28:354–359.
Touya JJ, Rahimian J, Corbus HF, Grubbs DE, Savala KM, Glass EC, Bennett LR. The lung as a metabolic organ. Semin Nucl Med 1986; 16:296–305.
Van Zandwijk N, Zwijnenburg A, Hoefnagel CA, Marcuse HR. N-Isopropyl-p[123I]iodoamphetamine, a new agent for lung imaging studies. Thorax 1986; 41:801–803.
Nakajo M, Uchiyama N, Hiraki Y, Miyata Y, Iriki A, Hirotsu Y, Wakimoto J, Norimatsu Y. Increased accumulation of iodine-123-IMP in the pulmonary inflammatory lesion surrounding a lung cancer. Ann Nucl Med 1988; 2:49–53.
Nakajo M, Uchiyama N, Shinohara J, Iriki A, Hiromatsu Y, Egawa K, Fukunaga H; Norimatsu Y. Differentiation of bronchogenic carcinoma from secondary changes, obstructive pneumonitis and/or collapse by I-123IMP lung imaging. Ann Nucl Med 1990; 4:1–13.
Bristow MR, Ginsburg R, Minobe W, Cubicciotti RS, Sageman WS, Lurie K, Billingham ME, Harrison DC, Stinson EB. Decreased catecholamine sensitivity and β-adrenergic-receptor density in failing human hearts. N Engl J Med 1982; 307:205–211.
Lowry OH, Rosebrough NJ, Farr AL, Randall RJ. Protein measurement with the Folin phenol reagent. J Biol Chem 1951; 193:265–275.
Olsen RW, Bergman MO, Van Ness PC, Lumis SC, Watkins AE, Napias C, Greenlee DV. r-Amino butyric acid receptor binding in mammalian brain: heterogeneity of binding sites. Mol Pharmacol 1981; 19:217–227.
Nishikawa H, Taniguchi T, Ninomiya H, Fujiwara M. Nicotinic acteylcholine receptors in the rat stomach: I. (−)-[3H]nicotine binding. Eur J Pharmacol 1988; 146:97–103.
Gallagher B, Christman D, Fowler J, MacGregor R, Wolf AP, Som P, Ansari AN, Atkins H. Radioisotope scintigraphy for the study of dynamics of amine regulation by the human lung. Chest 1977; 71 (2 Suppl):282–284.
Geddes DM, Nesbitt K, Traill T, Blackburn JP. First pass uptake of 14C-propranolol by the lung. Thorax 1979; 34:810–813.
Rahimian J, Bennett LR, Touya JJ, Akber SF. Metabolic lung scanning: demonstration of amine receptors with N-isopropyl-I-123-iodoamphetamine [abstract]. Clin Nucl Med 1981; 6:453.
Joulin Y, Moretti JL, Hoellinger H, Defer G. Fate of isopropyliodoamphetamine (IMP) in rat liver microsomes. Nucl Med Commun 1992; 13:99–105.
Moretti JL, Zini R, Morin D, Joulin Y, Desplanches G, Caillat-Vigneron N, Tillement JP. Interactions of phenylalkylamines with human lung membrane and microsome preparation. Nucl Med Commun 1987; 8:115–120.
Dollery CT, Junod AF. Concentration of (+−)propranolol in isolated, perfused lungs of rat. Br J Pharmacol 1976; 5:67–71.
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Tanaka, E., Mishima, M., Kawakami, K. et al. N-Isopropyl-p-iodoamphetamine receptors in normal and cancerous tissue of the human lung. Eur J Nucl Med 20, 293–296 (1993). https://doi.org/10.1007/BF00169803
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DOI: https://doi.org/10.1007/BF00169803