Effects of(-)-RO363 at human atrial β-adrenoceptor subtypes, the human cloned β3-adrenoceptor and rodent intestinal β3-adrenoceptors

British Journal of Pharmacology

Volumn 120, Issue 2, 1997, Pages 165-176

  Molenaar, Peter ^a   Sarsero, Doreen ^a   Arch, Jonathan R S ^b   Kelly, John ^b   Henson, Sian M ^b   Kaumann, Alberto J ^c  

^a UNIVERSITY OF MELBOURNE   (Australia)

^b GLAXOSMITHKLINE   (United Kingdom)

^c BABRAHAM INSTITUTE   (United Kingdom)

Author keywords

3 and atypical adrenoceptors; ( ) RO363; Chronic 1 adrenoceptor blockade; Cloned human 3 adrenoceptors; Guinea pig ileum; Human atrium; Rat colon

Indexed keywords

1 (3,4 DIHYDROXYPHENOXY) 3 (3,4 DIMETHOXYPHENETHYLAMINO) 2 PROPANOL; 3 ISOPROPYLAMINO 1 (7 METHYL 4 INDANYLOXY) 2 BUTANOL; 5 [2 [[2 HYDROXY 3 [4 (1 METHYL 4 TRIFLUOROMETHYL 2 IMIDAZOLYL)PHENOXY]PROPYL]AMINO]ETHOXY]SALICYLAMIDE; ADENYLATE CYCLASE; BETA 2 ADRENERGIC RECEPTOR; BETA 3 ADRENERGIC RECEPTOR; BETA ADRENERGIC RECEPTOR; BETA ADRENERGIC RECEPTOR BLOCKING AGENT; CALCIUM ION; CYANOPINDOLOL I 125; HISTAMINE; HISTAMINE H2 RECEPTOR; ISOPRENALINE; PARTIAL AGONIST; POTASSIUM CHLORIDE; PROPRANOLOL; RECEPTOR SUBTYPE; SEROTONIN 4 RECEPTOR;

ADULT; ANIMAL TISSUE; ARTICLE; AUTORADIOGRAPHY; CELL STIMULATION; CHO CELL; CLINICAL ARTICLE; COLON; CONCENTRATION RESPONSE; CONTROLLED STUDY; DRUG POTENCY; FEMALE; GUINEA PIG; HEART ATRIUM; HOMOGENATE; HUMAN TISSUE; ILEUM; INOTROPISM; INTESTINE; LONG TERM CARE; MALE; MOLECULAR CLONING; NONHUMAN; PRIORITY JOURNAL; PROTEIN EXPRESSION; RAT; RECEPTOR BINDING; RECEPTOR DENSITY; SMOOTH MUSCLE RELAXATION;

ADENYLATE CYCLASE; ADRENERGIC BETA-AGONISTS; AGED; ANIMALS; AUTORADIOGRAPHY; CATECHOLS; CHO CELLS; COLON; CRICETINAE; DOSE-RESPONSE RELATIONSHIP, DRUG; FEMALE; GUINEA PIGS; HUMANS; MALE; MIDDLE AGED; PROPANOLAMINES; RADIOLIGAND ASSAY; RATS; RATS, SPRAGUE-DAWLEY; RECEPTORS, ADRENERGIC, BETA; RECEPTORS, ADRENERGIC, BETA-1; RECEPTORS, ADRENERGIC, BETA-3;

EID: 0031016767     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0700850     Document Type: Article

References (46)

1. ARUNLAKSHANA, O. & SCHILD, H.O. (1959). Some quantitative uses of drug antagonists. Br. J. Pharmacol., 14, 48-58.
2. 3-Adrenoceptors and atypical β-adrenoceptors. Med. Res. Rev., 48, 663-729.
3. 2-selective adrenoceptor antagonist (ICI 118,551). J. Cardiovasc. Pharmacol., 5, 430-437.
4. BLINKS, J.R. (1965). Convenient apparatus for recording contractions of isolated muscle. J. Appl. Physiol., 20, 755-757.
5. BOND, R.A. & CLARKE, D.E. (1988). Agoinst and antagonist characterization of a putative adrenoceptor with distinct pharmacological properties from the α- and β-subtypes. Br. J. Pharmacol., 95, 723-734.
6. BUXTON, B.F., JONES, C.R., MOLENAAR, P. & SUMMERS, R.J. (1987). Characterization and autoradiographic localization of β-adrenoceptor subtypes in human cardiac tissues. Br. J. Pharmacol., 92, 299-310.
7. 3-adrenoceptor refractory to down-regulation. Biochem. J., 303, 973-978.
8. 2-adrenoceptors. Eur. J. Pharmacol., 130, 137-139.
9. 2-adrenoceptors in the human atrioventricular conducting system: A comparison of patients with idiopathic dilated cardiomyopathy and ischemic heart disease. J. Mol. Cell. Cardiol., 26, 313-323.
10. 3-adrenoceptor. Science, 245, 1118-1121.
11. 2-adrenoceptors of human heart. Differential antagonism of the positive inotropic effects and adenylate cyclase stimulation by (-)-noradrenaline and (-)-adrenaline. Naunyn-Schmiedeberg's Arch. Pharmacol., 331, 60-70.
12. 2-adrenoceptors in human atrial myocardium. Circ. Res., 66, 1610-1623.
13. 1-antagonist treatment. Circ. Res., 69, 959-964.
14. KAUFMAN, R.J. & SHARP, P.A. (1982). Amplification and expression of sequences cotransfected with a modular dihydrofolate reductase complementary DNA gene. J. Mol. Biol., 159, 601-621.
15. 2-adrenoceptors activated by (-)-adrenaline in rat sinoatrial node. Naunyn-Schmiedeberg's Arch. Pharmacol., 332, 406-409.
16. KAUMANN, A.J. (1989). Is there a third heart β-adrenoceptor? Trends Pharmacol. Sci., 10, 316-320.
17. 4-like receptors. Naunyn-Schmiedeberg's Arch. Pharmacol., 342, 619-622.
18. KAUMANN, A.J. (1991). Some aspects of heart beta adrenoceptor function. Cardiovasc. Drugs Ther., 5, 549-560.
19. KAUMANN, A.J. (1996). (-)-CGP 12177-induced increase of human atrial contraction through a putative third β-adrenoceptor. Br. J. Pharmacol., 117, 93-98.
20. 2-adrenoceptors in the stimulation of adenylate cyclase and contractile force. Eur. Heart J., 10, (Supplement B) 29-37.
21. 2-Adrenoceptor-mediated positive inotropic effects of adrenaline in human ventricular myocardium. Quantitative discrepancies with binding and adenylate cyclase stimulation. Naunyn-Schmiedeberg's Arch. Pharmacol., 335, 403-411.
22. KAUMANN, A.J., LEMOINE, H., SCHWEDERSKI-MENKE, U. & EHLE, B. (1989b). Relations between β-adrenoceptor occupancy and increases of contractile force and adenylate cyclase activity induced by catecholamines in human ventricular myocardium. Acute desensitization and comparison with feline ventricle. Naunyn-Schmiedeberg's Arch. Pharmacol., 339, 99-112.
23. 2-adrenoceptors. Pharmacol. Commun., 6, 215-222.
24. 3-adrenoceptor in the rat. Br. J. Pharmacol., 118, 2085-2098.
25. 2-adrenoceptors mediate catecholamine-evoked arrhythmias in isolated human right atrium. Naunyn-Schmiedeberg's Arch. Pharmacol., 348, 536-540.
26. 4 receptors in human atrium: facilitation by chronic β-adrenoceptor blockade. Naunyn-Schmiedeberg's Arch. Pharmacol., 349, 331-337.
27. LEATHERBARROW, R.J. (1992). GRAFIT VERSION 3.0. Staines, U.K.: Erithacus Software Ltd.
28. 3H-ICI 118,551 and blocking potency of ICI 118,551. Naunyn-Schmiedeberg's Arch. Pharmacol., 331, 40-51.
29. 2-adrenoceptors of human atrium and ventricle to the effects of noradrenaline and adrenaline as assessed with (-)-atenolol. Br. J. Pharmacol., 95, 55-66.
30. 3-adrenergic receptors: differential agonist activation of recombinant receptors in chinese hamster ovary cells. Mol. Pharmacol., 42, 634-637.
31. LOWRY, O.H., ROSENBROUGH, N.J., FARR, A.L. & RANDALL, R.J. (1951). Protein measurement with the folin phenol reagent. J. Biol. Chem., 193, 265-275.
32. 3-adrenoceptor) mediating relaxation in the rat distal colon in vitro. Br. J. Pharmacol., 101, 569-574.
33. MCPHERSON, G.A. (1983). A practical computer-based approach to the analysis of radioligand binding experiments. Comp. Prog. Biomed., 17, 107-114.
34. 2-adrenoceptor sites. Br. J. Pharmacol., 82, 897-904.
35. 2-adrenoceptors in the human heart by chronic β-adrenoceptor antagonist treatment. Br. J. Pharmacol., 94, 685-692.
36. MILLER, J.A., CURELLA, P. & ZAHNISER, N.R (1988). A new densitometric procedure to measure protein levels in tissue slices in quantitative autoradiography. Brain Res., 447, 60-66.
37. MOLENAAR. P., CANALE, E. & SUMMERS, R.J. (1987). Autoradiographic localization of beta-1 and beta-2 adrenoceptors in guinea pig atrium and regions of the conducting system. J. Pharmacol. Exp. Ther., 241, 1048-1064.
38. 2-adrenoceptors in guinea-pig atrioventricular conducting system. J. Mol. Cell. Cordiol., 22, 483-495.
39. MOLENAAR, P., SMOLICH, J.J., RUSSELL, F.D., MCMARTIN, L.R. & SUMMERS, R.J. (1990b). Differential regulation of beta-1 and beta-2 adrenoceptors in guinea-pig atrioventricular conducting system after chronic (-)-isoprenaline infusion. J. Pharmacol. Exp. Ther., 255, 393-400.
40. 2-muscarinic receptors in the human right atrium. Br. J. Pharmacol., 101, 363-369.
41. MUNSON, P.J. & RODBARD, D. (1980). LIGAND: A versatile computerised approach for the characterisation of ligand binding systems. Anal. Biochem., 107, 220-239.
42. MURPHREE, S.S. & SAFFITZ, J.E. (1988). Delineation of the distribution of β-adrenergic receptor subtypes in canine myocardium. Circ. Res., 63, 117-125.
43. NEVE, K.A., MCGONIGLE, P. & MOLINOFF, P.B. (1986). Quantitative analysis of the selectivity of radioligands for subtypes of beta adrenergic receptors. J. Pharmacol. Exp. Ther., 238, 46-53.
44. 4 receptors by chronic β blocker treatment. Circulation, 92, 2526-2539.
45. 2 receptor systems in human atrium: role of cyclic nucleotides. Naunyn-Schmiedeberg's Arch. Pharmacol., 353, 661-670.
46. WILLIAMS, D.W. & SUMMERS, R.J. (1990). SIMUL: an accurate method for the determination of receptor subtype proportions using a personal computer. Comput. Meth. Prog. Biomed., 32, 137-139.