Atypical cardiostimulant β-adrenoceptor in the rat heart: Stereoselective antagonism by bupranolol but lack of effect by some bupranolol analogues

British Journal of Pharmacology

Volumn 139, Issue 8, 2003, Pages 1548-1554

  Malinowska, Barbara ^a   Kieć Kononowicz, Katarzyna ^b   Flau, Karsten ^c   Godlewski, Grzegorz ^a   Kozłowska, Hanna ^a   Kathmann, Markus ^c   Schlicker, Eberhard ^c  

^a MEDICAL UNIVERSITY OF BIALYSTOK   (Poland)

^b JAGIELLONIAN UNIVERSITY MEDICAL COLLEGE   (Poland)

^c UNIVERSITY OF BONN   (Germany)

Author keywords

1 Adrenoceptor; 3H CGP 12177 binding; Atypical cardiostimulant adrenoceptor; Bupranolol analogues; Bupranolol enantiomers; CGP 12177; CGP 20712; Pithed rat; Positive chronotropic effect

Indexed keywords

3 ISOPROPYLAMINO 1 (7 METHYL 4 INDANYLOXY) 2 BUTANOL; 4 (3 TERT BUTYLAMINO 2 HYDROXYPROPOXY) 2 BENZIMIDAZOLONE; 5 [2 [[2 HYDROXY 3 [4 (1 METHYL 4 TRIFLUOROMETHYL 2 IMIDAZOLYL)PHENOXY]PROPYL]AMINO]ETHOXY]SALICYLAMIDE; BETA 1 ADRENERGIC RECEPTOR BLOCKING AGENT; BETA 1 ADRENERGIC RECEPTOR STIMULATING AGENT; BETA 2 ADRENERGIC RECEPTOR BLOCKING AGENT; BETA ADRENERGIC RECEPTOR; BEVANTOLOL; BUPRANOLOL; DRUG DERIVATIVE; PRENALTEROL; TRITIUM;

ANIMAL EXPERIMENT; ANIMAL TISSUE; ARTICLE; BRAIN MEMBRANE; CHRONOTROPISM; CONTROLLED STUDY; DOSE RESPONSE; DRUG ANTAGONISM; DRUG BINDING SITE; DRUG EFFECT; DRUG POTENCY; DRUG PROTEIN BINDING; ENANTIOMER; HEART MUSCLE CONTRACTILITY; HEART RATE; IMMUNOHISTOCHEMISTRY; INTRINSIC SYMPATHOMIMETIC ACTIVITY; MALE; NONHUMAN; PRIORITY JOURNAL; RAT;

ADRENERGIC BETA-ANTAGONISTS; ANIMALS; BINDING SITES; BLOOD PRESSURE; BUPRANOLOL; DOSE-RESPONSE RELATIONSHIP, DRUG; HEART RATE; MALE; MYOCARDIAL CONTRACTION; MYOCARDIUM; RATS; RATS, WISTAR; RECEPTORS, ADRENERGIC, BETA; STEREOISOMERISM; STIMULATION, CHEMICAL; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 0141428761     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0705390     Document Type: Article

References (27)

1. ALEXANDER, S., PETERS, J. & MATHIE, A. (2001). TiPS nomenclature supplement. Trends Pharmacol. Sci. (Suppl.), 22, 1-146.
2. BRADFORD, M.M. (1976). A rapid and sensitive method for the quantitation of microgram quantities of protein utilizing the principle of protein-dye binding. Anal. Biochem., 72, 248-254.
3. 1-adrenoceptors in human myocardium. J. Pharmacol. Exp. Ther., 300, 794-801.
4. 3 receptors and rat atrial receptors mediating tachycardia. Br. J. Pharmacol., 126, 1018-1024.
5. 2+ transients in mouse ventricular myocytes. Naunyn-Schmiedeberg's Arch. Pharmacol., 360, 445-456.
6. GRAEFE, K.H. & BÖNISCH, H. (1988). The transport of amines across the axonal membranes of noradrenergic and dopaminergic neurones. In: Handbook of Experimental Pharmacology, ed. Trendelenburg, U. & Weiner, N. Vol. 90/I, pp. 193-245. Berlin: Springer.
7. HOEFLE, M.L., HASTINGS, S.G., MEYER, R.F., COREY, R.M., HOLMES, A. & STRATTON, C.D. (1975). Cardioselective β-adrenergic blocking agents. 1. 1-[(3,4-dimethoxyphenethyl)amino]-3-aryloxy-2-propanols. J. Med. Chem., 18, 148-152.
8. 1-adrenoceptor. Br. J. Pharmacol., 117, 93-98.
9. 4-adrenoceptor pharmacology. Naunyn-Schmiedeberg's Arch. Pharmacol., 363, 87-93.
10. 3-adrenoceptor in the rat. Br. J. Pharmacol., 118, 2085-2098.
11. KAUMANN, A.J. & MOLENAAR, P. (1997). Modulation of human cardiac function through 4 β-adrenoceptor populations. Naunyn-Schmiedeberg's Arch. Pharmacol., 355, 667-681.
12. 3-adrenoceptor knockout mice. Mol. Pharmacol., 53, 670-675.
13. 4-adrenoceptors mediated responses occur in parallel in a rat model of cardiac failure. Br. J. Pharmacol., 128, 1399-1406.
14. KUNZ, W., JACOBI, H. & KOCH, K. (1967). Verfahren zur Herstellung von basischen Phenyl- und Naphthyläthern und -thioäthern und deren Salzen. German Patent, DE, 1236523.
15. LEMOINE, H. & KAUMANN, A.J. (1982). A novel analysis of concentration-dependence of partial agonism. Ring-demethylation of bupranolol results in a high affinity partial agonist (K 105) for myocardial and tracheal β-adrenoceptors. Naunyn-Schmiedeberg's Arch. Pharmacol., 320, 130-144.
16. LEMOINE, H. & KAUMANN, A.J. (1983). A model for the interaction of competitive antagonists with two receptor-subtypes characterized by a Schild-plot with apparent slope unity. Agonist-dependent enantiomeric affinity ratios for bupranolol in tracheae but not in right atria of guinea pigs. Naunyn-Schmiedeberg's Arch. Pharmacol., 322, 111-120.
17. 2-Adrenoceptor antagonist activity of a series of para-substituted N-isopropylphenoxypropanolamines. Eur. J. Med. Chem., 34, 919-937.
18. 1-adrenoceptors by carvedilol in ferret myocardium. Naunyn-Schmiedeberg's Arch. Pharmacol., 359, 400-403.
19. 2-adrenoceptor-mediated effects. Br. J. Pharmacol., 124, 1341-1344.
20. 1-adrenoceptor in ferret ventricular myocardium. Br. J. Pharmacol., 135, 451-461.
21. 3-adrenoceptors. Br. J. Pharmacol., 117, 943-949.
22. 3-adrenoceptors in the pithed rat. Br. J. Pharmacol., 122, 1307-1314.
23. PHILLIPS, D.K. (1980). Chemistry of alpha- and beta-adrenoceptor agonists and antagonists. In: Handbook of Experimental Pharmacology, ed. Szekeres, L. Vol. 54/I, pp. 3-61. Berlin, Heidelberg, New York: Springer.
24. 3H]-CGP 12177 binding. Br. J. Pharmacol., 128, 1445-1460.
25. 1-adrenoceptor. Naunyn-Schmiedeberg's Arch. Pharmacol., 367, 10-21.
26. TADOKORO, C., KIUCHI, Y., YAMAZAKI, Y., NARA, K., OGUCHI, K. & KAMIJIAMA, K. (1997). Behavioral stimulation without alteration of β and 5-HT receptors and adenylate cyclase activity in rat brain after chronic sertraline administration. Psychopharmacology, 130, 124-130.
27. TODA, N. & OKAMURA, T. (1990). Beta adrenoceptor subtype in isolated human, monkey and dog epicardial coronary arteries. J. Pharmacol. Exp. Ther., 253, 518-524.