Increased rigidity of the chiral centre of tocainide favours stereoselectivity and use-dependent block of skeletal muscle Na+ channels enhancing the antimyotonic activity in vivo

British Journal of Pharmacology

Volumn 134, Issue 7, 2001, Pages 1523-1531

  Talon, Sophie ^a   De Luca, Annamaria ^a   De Bellis, Michela ^a   Desaphy, Jean François ^a   Lentini, Giovanni ^a   Scilimati, Antonio ^a   Corbo, Filomena ^a   Franchini, Carlo ^a   Tortorella, Paolo ^a   Jockusch, Harald ^b   Conte Camerino, Diana ^a  

^a UNIVERSITY OF BARI   (Italy)

^b BIELEFELD UNIVERSITY   (Germany)

Author keywords

adr adr mice; Antimyotonic activity; Native frog skeletal muscle fibres; Stereoselectivity; Tocainide derivatives; Use dependent block; Vaseline gap voltage clamp

Indexed keywords

N (2,6 DIMETHYLPHENYL) 1 METHYL 2 PYRROLIDINECARBOXAMIDE; N (2,6 DIMETHYLPHENYL) 2 PYRROLIDINECARBOXAMIDE; PROLINE DERIVATIVE; SODIUM CHANNEL; TO 5; TO 6; TOCAINIDE; UNCLASSIFIED DRUG;

ANIMAL TISSUE; ANTIMYOTONIC ACTIVITY; ARTICLE; CHANNEL GATING; CONCENTRATION RESPONSE; DRUG ACTIVITY; DRUG CONFORMATION; DRUG POTENCY; FROG; NONHUMAN; PRIORITY JOURNAL; STEREOCHEMISTRY;

EID: 0035206715     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0704366     Document Type: Article

References (33)

1. On the repetitive discharge in myotonic muscle fibers
2. Ion-channel detects and aberrant excitability in myotonia and periodic paralysis
3. From mutation to myotonia in sodium channel disorders
4. + channels: Local anesthesics, antiarrhythmics and anticonvulsants
5. Antimyotonic effects of tocainide enantiomers on skeletal muscle fibers of congenitally myotonic goats
6. Ion channel genes and human neurological disease: Recent progress, prospects, and challenges
7. Molecular determinants of mexiletine structure for potent and use-dependent block of skeletal muscle sodium channels
8. Inhibition of frog skeletal muscle sodium channels by newly synthesized chiraI derivatives of mexiletine and tocainide
9. Stereoselective effects of mexiletine enantiomers on sodium currents and excitability characteristics of adult skeletal muscle fibers
10. Evaluation of the antimyotonic activity of mexiletine and some new analogs on sodium currents of single muscle fibers and on the abnormal excitability of the myotonic ADR mouse
11. The different use dependences of tocainide and benzocaine are correlated with different effects on sodium channel inactivation
12. + channels in a model of myotonia induced by ATX
13. AMI: A new general purpose quantum mechanical molecular model
14. Inactivation of human sodium channels and the effect of tocainide
15. + channel with increased potency and improved use-dependent activity
16. Nonsense and missense mutations in the muscular chloride channel gene Clc-1 of myotonic mice
17. An improved vaseline-gap voltage-clamp for skeletal muscle fibers
18. Treatment of myotonia with antiarrhythmic drugs
19. Molecular pathophysiology of voltage-gated ion channels
20. A molecular basis for different local anesthesic affinities of resting versus open and inactivated states of the sodium channels
21. - complexed aromatic fluoride
22. + channels modulate binding affinity and stereoselectivity of local anesthesic enantiomers
23. The familial periodic paralyses and nondystrophic myotonias
24. Tocainide therapy in muscle cramps and spasms due to neuromuscular disease
25. + channels by local anesthesics
26. + channels
27. Drug therapy: Tocainide
28. The nondystrophic myotonias
29. Successful treatment with tocainide of recessive generalized congenital myotonia
30. Stereoselective interaction of tocainide and its chiral analogs with the sodium channels in human myoballs
31. + channel D3-S6 segment modulates both batrachotoxin and local anesthetic affinities
32. + channel D4-S6 reduce inactivated channel block by local anesthesics
33. + channel α subunit