Literature DB >> 6696758

[3H] verapamil binding sites in skeletal muscle transverse tubule membranes.

J P Galizzi, M Fosset, M Lazdunski.   

Abstract

[3H]verapamil binding to muscle tubule membrane has the following properties. KD = 27 +/- 5 nM and maximum binding capacity Bmax = 50 +/- 5 pmol/mg of protein. A 1 = 1 stoichiometry of binding was found for the ratio of [3H]verapamil versus [3H] nitrendipine binding sites. The dissociation constant found at equilibrium is near that determined from the ratio of the rate constants for association (k1) and dissociation (k-1). Antiarrhythmic drugs like D600, diltiazem and bepridil are competitive inhibitors of [3H] verapamil binding with KD values between 40 and 200 nM. Dihydropyridine analogs are apparent non competitive inhibitors of [3H]verapamil binding with half-maximum inhibition values (K0.5) between 1 and 5 nM.

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Year:  1984        PMID: 6696758     DOI: 10.1016/0006-291x(84)91092-1

Source DB:  PubMed          Journal:  Biochem Biophys Res Commun        ISSN: 0006-291X            Impact factor:   3.575


  10 in total

1.  Pharmacological characterization of RP 62203, a novel 5-hydroxytryptamine 5-HT2 receptor antagonist.

Authors:  A Doble; D Girdlestone; O Piot; D Allam; J Betschart; A Boireau; A Dupuy; C Guérémy; J Ménager; J L Zundel
Journal:  Br J Pharmacol       Date:  1992-01       Impact factor: 8.739

2.  Ontogenesis and localization of Ca2+ channels in mammalian skeletal muscle in culture and role in excitation-contraction coupling.

Authors:  G Romey; L Garcia; V Dimitriadou; M Pincon-Raymond; F Rieger; M Lazdunski
Journal:  Proc Natl Acad Sci U S A       Date:  1989-04       Impact factor: 11.205

3.  Neuroleptics of the diphenylbutylpiperidine series are potent calcium channel inhibitors.

Authors:  J P Galizzi; M Fosset; G Romey; P Laduron; M Lazdunski
Journal:  Proc Natl Acad Sci U S A       Date:  1986-10       Impact factor: 11.205

4.  Calcium channel antagonists inhibit the acrosome reaction and bind to plasma membranes of sea urchin sperm.

Authors:  T Kazazoglou; R W Schackmann; M Fosset; B M Shapiro
Journal:  Proc Natl Acad Sci U S A       Date:  1985-03       Impact factor: 11.205

5.  Relationship between the stereoselective negative inotropic effects of verapamil enantiomers and their binding to putative calcium channels in human heart.

Authors:  D R Ferry; H Glossmann; A J Kaumann
Journal:  Br J Pharmacol       Date:  1985-04       Impact factor: 8.739

6.  [3H]-verapamil binding to rat cardiac sarcolemmal membrane fragments; an effect of ischaemia.

Authors:  J S Dillon; W G Nayler
Journal:  Br J Pharmacol       Date:  1987-01       Impact factor: 8.739

7.  Characteristics of the phenylalkylamine binding site in canine cardiac sarcolemmal membranes.

Authors:  L Dumont; J S Williams; P L Vaghy; A Schwartz
Journal:  Basic Res Cardiol       Date:  1988 Jul-Aug       Impact factor: 17.165

8.  The IVS6 segment of the L-type calcium channel is critical for the action of dihydropyridines and phenylalkylamines.

Authors:  A Schuster; L Lacinová; N Klugbauer; H Ito; L Birnbaumer; F Hofmann
Journal:  EMBO J       Date:  1996-05-15       Impact factor: 11.598

9.  Dihydropyridine-sensitive Ca2+ channels in mammalian skeletal muscle cells in culture: electrophysiological properties and interactions with Ca2+ channel activator (Bay K8644) and inhibitor (PN 200-110).

Authors:  C Cognard; G Romey; J P Galizzi; M Fosset; M Lazdunski
Journal:  Proc Natl Acad Sci U S A       Date:  1986-03       Impact factor: 11.205

10.  (-)-3H-desmethoxyverapamil labelling of putative calcium channels in brain: autoradiographic distribution and allosteric coupling to 1,4-dihydropyridine and diltiazem binding sites.

Authors:  D R Ferry; A Goll; C Gadow; H Glossmann
Journal:  Naunyn Schmiedebergs Arch Pharmacol       Date:  1984-09       Impact factor: 3.000

  10 in total

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