Literature DB >> 6092973

Different steric characteristics of beta 1- and beta 2-adrenoceptors.

T H Morris, A J Kaumann.   

Abstract

beta-Adrenoceptors of lung (75% beta 2) and heart (95% beta 1) of calf were labelled with 3H-(-)-propranolol. The stereoisomers of 10 ligands were used to inhibit the binding of 3H-(-)-propranolol to membrane particles. The affinity ratio of stereoisomers is consistently greater for beta 1-adrenoceptors than for beta 2-adrenoceptors, regardless of whether the ligands are agonists, partial agonists or antagonists. The beta 1-adrenoceptor appears to possess stricter steric requirements than the beta 2-adrenoceptor. This property may prove helpful in differentiating the beta-adrenoceptor subtypes during receptor solubilization and purification.

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Year:  1984        PMID： 6092973     DOI： 10.1007/bf00500913

Source DB:  PubMed          Journal:  Naunyn Schmiedebergs Arch Pharmacol        ISSN： 0028-1298            Impact factor:   3.000


  16 in total

1.  On spare beta-adrenoceptors of inotropic effect of catecholamines in kitten ventricle.

Authors:  A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1978-11       Impact factor: 3.000

2.  Studies on the relationship between chemical constitution and physiological action: Molecular dissymmetry and physiological activity.

Authors:  L H Easson; E Stedman
Journal:  Biochem J       Date:  1933       Impact factor: 3.857

3.  Coexistence of beta1 and beta2 adrenoceptors in mammalian lung: evidence from direct binding studies.

Authors:  E L Rugg; D B Barnett; S R Nahorski
Journal:  Mol Pharmacol       Date:  1978-11       Impact factor: 4.436

4.  Simultaneous determination of beta-1 and beta-2-adrenergic receptors in tissues containing both receptor subtypes.

Authors:  K P Minneman; L R Hegstrand; P B Molinoff
Journal:  Mol Pharmacol       Date:  1979-07       Impact factor: 4.436

Review 5.  Adenylate cyclase-coupled beta-adrenergic receptors: structure and mechanisms of activation and desensitization.

Authors:  R J Lefkowitz; J M Stadel; M G Caron
Journal:  Annu Rev Biochem       Date:  1983       Impact factor: 23.643

6.  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.

Authors:  H Lemoine; A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1983-03       Impact factor: 3.000

7.  Comparative assessment of beta-adrenoceptor blocking agents as simple competitive antagonists in isolated heart muscle: similarity of inotropic and chronotropic blocking potencies against isoproterenol.

Authors:  A J Kaumann; T K McInerny; D P Gilmour; J R Blinks
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1980-04       Impact factor: 3.000

8.  Relationship between the inhibition constant (K1) and the concentration of inhibitor which causes 50 per cent inhibition (I50) of an enzymatic reaction.

Authors:  Y Cheng; W H Prusoff
Journal:  Biochem Pharmacol       Date:  1973-12-01       Impact factor: 5.858

9.  Evidence that (+)-bupranolol interacts directly with myocardial beta-adrenoceptors. Control of optical purity with differential thermal analysis.

Authors:  W Wächter; U Münch; H Lemoine; A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1980-08       Impact factor: 3.000

10.  Stimulant and blocking effects of optical isomers of pindolol on the sinoatrial node and trachea of guinea pig. Role of beta-adrenoceptor subtypes in the dissociation between blockade and stimulation.

Authors:  M Walter; H Lemoine; A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1984-09       Impact factor: 3.000
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  15 in total

1.  The beta 1- and beta 2-adrenoceptor affinity and beta 1-blocking potency of S- and R-metoprolol.

Authors:  G Wahlund; V Nerme; T Abrahamsson; P O Sjöquist
Journal:  Br J Pharmacol       Date:  1990-03       Impact factor: 8.739

2.  The beta-adrenoceptor-adenylate cyclase complex. From model to biochemical reality.

Authors:  A P Ijzerman; H Timmerman
Journal:  Pharm Weekbl Sci       Date:  1986-08-22

3.  Molecular modeling of a putative antagonist binding site on helix III of the beta-adrenoceptor.

Authors:  H W van Vlijmen; A P IJzerman
Journal:  J Comput Aided Mol Des       Date:  1989-06       Impact factor: 3.686

4.  Chiral muscarinic agonists possessing a 1,3-oxathiolane nucleus: enantio- and tissue-selectivity on isolated preparations of guinea-pig ileum and atria and of rat urinary bladder.

Authors:  P Angeli; L Brasili; M Giannella; F Gualtieri; M T Picchio; E Teodori
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1988-03       Impact factor: 3.000

5.  Direct labelling of myocardial beta 1-adrenoceptors. Comparison of binding affinity of 3H-(-)-bisoprolol with its blocking potency.

Authors:  A J Kaumann; H Lemoine
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1985-10       Impact factor: 3.000

Review 6.  Some aspects of heart beta adrenoceptor function.

Authors:  A J Kaumann
Journal:  Cardiovasc Drugs Ther       Date:  1991-06       Impact factor: 3.727

7.  Stimulant and blocking effects of optical isomers of pindolol on the sinoatrial node and trachea of guinea pig. Role of beta-adrenoceptor subtypes in the dissociation between blockade and stimulation.

Authors:  M Walter; H Lemoine; A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1984-09       Impact factor: 3.000

8.  Intrinsic sympathomimetic activity of (-)-pindolol mediated through a (-)-propranolol-resistant site of the beta1-adrenoceptor in human atrium and recombinant receptors.

Authors:  Shirin S Joseph; James A Lynham; Peter Molenaar; Andrew A Grace; William H Colledge; Alberto J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  2003-11-08       Impact factor: 3.000

9.  Contribution of beta 1- and beta 2-adrenoceptors of human atrium and ventricle to the effects of noradrenaline and adrenaline as assessed with (-)-atenolol.

Authors:  H Lemoine; H Schönell; A J Kaumann
Journal:  Br J Pharmacol       Date:  1988-09       Impact factor: 8.739

10.  The affinity of (-)-propranolol for beta 1- and beta 2-adrenoceptors of human heart. Differential antagonism of the positive inotropic effects and adenylate cyclase stimulation by (-)-noradrenaline and (-)-adrenaline.

Authors:  E Gille; H Lemoine; B Ehle; A J Kaumann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1985-10       Impact factor: 3.000
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