Literature DB >> 6096722

The relation between ionization and affinity of beta-adrenoceptor ligands.

A P IJzerman, T Bultsma, H Timmerman, J Zaagsma.   

Abstract

The displacement by some beta-adrenoceptor ligands of the specific (-)-[3H]dihydroalprenolol binding to membranes of the bovine musculus trapezius, a rich and homogeneous source of beta 2-adrenoceptors, appeared to be pH-dependent. This phenomenon was in contrast to the pH-dependency of the (-)-[3H]dihydroalprenolol receptor-binding and could be related to the ionization characteristics of the compounds. It was shown quantitatively that of the four ionic species of the ligands commonly present at physiological pH, the cation governs beta 2-adrenoceptor affinity.

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Year:  1984        PMID： 6096722     DOI： 10.1007/bf00506239

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


  16 in total

1.  Structure-basicity and structure-affinity relationships of beta-adrenergic blocking agents.

Authors:  B Fernández; A J Kaumann
Journal:  Acta Physiol Lat Am       Date:  1975

2.  Comparison of beta adrenergic receptor subtypes in mammalian tissues.

Authors:  K P Minneman; A Hedberg; P B Molinoff
Journal:  J Pharmacol Exp Ther       Date:  1979-12       Impact factor: 4.030

3.  NMR studies of catecholamines, Acid dissociation equilibria in aqueous solutions.

Authors:  J Granot
Journal:  FEBS Lett       Date:  1976-09-01       Impact factor: 4.124

4.  The influence of temperature increase, elevation of extracellular h+-concentration, and of triiodothyronine on the actions of phenylephrine, histamine, and beta-sympathomimetic drugs on rabbit aortic strips.

Authors:  J Wagner; D Reinhardt; W Huppertz
Journal:  Arch Int Pharmacodyn Ther       Date:  1975-11

5.  The pharmacolgy of 5-(2-t-butylamino-1-hydroxyethyl) salicylamide (ah 3474), a beta-adrenoreceptor blocking agent.

Authors:  C H Blackburn; L J Byrne; V A Cullum; J B Farmer; G P Levy
Journal:  J Pharm Pharmacol       Date:  1969-08       Impact factor: 3.765

6.  The effect of pH changes and ionization on the action of epinephrine upon the isolated rabbit ileum.

Authors:  R C Reynolds; H F Hardman
Journal:  Eur J Pharmacol       Date:  1972-12       Impact factor: 4.432

7.  The ionization of beta-adrenoceptor agonists: a method for unravelling ionization schemes.

Authors:  A P Ijzerman; T Bultsma; H Timmerman; J Zaagsma
Journal:  J Pharm Pharmacol       Date:  1984-01       Impact factor: 3.765

8.  A quantitative analysis of beta-adrenergic receptor interactions: resolution of high and low affinity states of the receptor by computer modeling of ligand binding data.

Authors:  R S Kent; A De Lean; R J Lefkowitz
Journal:  Mol Pharmacol       Date:  1980-01       Impact factor: 4.436

9.  Adrenergic beta 1- and beta 2-receptors in the isolated rabbit jejunum and ileum.

Authors:  N Nakahata; Y Takagi; E Watanabe; T Suzuki
Journal:  Fukushima J Med Sci       Date:  1978

10.  Validation and statistical analysis of a computer modeling method for quantitative analysis of radioligand binding data for mixtures of pharmacological receptor subtypes.

Authors:  A De Lean; A A Hancock; R J Lefkowitz
Journal:  Mol Pharmacol       Date:  1982-01       Impact factor: 4.436
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  10 in total

1.  Agonist-mediated conformational changes of beta-adrenoceptors could occur independent of functional coupling to Ns.

Authors:  Y Severne; L Kanarek; G Vauquelin
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1986-03       Impact factor: 3.000

2.  Affinity of clenbuterol analogues for beta 2-adrenoceptors in bovine skeletal muscle and the effect of these compounds on urinary nitrogen excretion in female rats.

Authors:  M N Sillence; G G Pegg; D B Lindsay
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1991-10       Impact factor: 3.000

3.  A molecular graphics study exploring a putative ligand binding site of the beta-adrenoceptor.

Authors:  A P IJzerman; H W van Vlijmen
Journal:  J Comput Aided Mol Des       Date:  1988-04       Impact factor: 3.686

4.  Beta-adrenoceptors and human skeletal muscle characterisation of receptor subtype and effect of age.

Authors:  M S Elfellah; R Dalling; I M Kantola; J L Reid
Journal:  Br J Clin Pharmacol       Date:  1989-01       Impact factor: 4.335

5.  Suramin analogs, divalent cations and ATP gamma S as inhibitors of ecto-ATPase.

Authors:  M W Beukers; C J Kerkhof; M A van Rhee; U Ardanuy; C Gurgel; H Widjaja; P Nickel; A P IJzerman; W Soudijn
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1995-05       Impact factor: 3.000

6.  [3H]R75231--a new radioligand for the nitrobenzylthioinosine sensitive nucleoside transport proteins. Characterization of (+/-)-[3H]R75231 binding to calf lung membranes, stereospecificity of its two stereoisomers, and comparison with [3H]nitrobenzylthioinosine binding.

Authors:  A P IJzerman; M Kruidering; A van Weert; H van Belle; C Janssen
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1992-05       Impact factor: 3.000

7.  The relationship between ionization and affinity of nucleoside transport inhibitors.

Authors:  A P IJzerman; A H Voorschuur
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1990-09       Impact factor: 3.000

8.  Assessment of the enantiomeric purity of R- and S-N6-phenylisopropyladenosine (PIA): implications for adenosine receptor subclassification.

Authors:  R A Mathôt; B C Van den Aarsen; J K von Frijtag Drabble Künzel; M Danhof; A P Ijzerman
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1994-07       Impact factor: 3.000

9.  Classical and atypical binding sites for beta-adrenoceptor ligands and activation of adenylyl cyclase in bovine skeletal muscle and adipose tissue membranes.

Authors:  M N Sillence; M L Matthews
Journal:  Br J Pharmacol       Date:  1994-03       Impact factor: 8.739

10.  Involvement of Asn-293 in stereospecific agonist recognition and in activation of the beta 2-adrenergic receptor.

Authors:  K Wieland; H M Zuurmond; C Krasel; A P Ijzerman; M J Lohse
Journal:  Proc Natl Acad Sci U S A       Date:  1996-08-20       Impact factor: 11.205
  10 in total

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