Block of the lymphocyte K+ channel mKv1.3 by the phenylalkylamine verapamil: Kinetic aspects of block and disruption of accumulation of block by a single point mutation

British Journal of Pharmacology

Volumn 131, Issue 7, 2000, Pages 1275-1284

  Robe, R J ^a   Grissmer, S ^a  

^a UNIVERSITY OF ULM   (Germany)

Author keywords

Accumulation of block; Inactivation; Kinetic model; mKv1.3; Phenylalkylamine; Verapamil

Indexed keywords

CALCIUM CHANNEL; PHENYLALKYLAMINE; POTASSIUM CHANNEL; VERAPAMIL;

ANIMAL CELL; ARTICLE; BINDING SITE; CONTROLLED STUDY; DRUG ACCUMULATION; DRUG BINDING; DRUG INACTIVATION; DRUG MECHANISM; KINETICS; LYMPHOCYTE; NONHUMAN; POINT MUTATION; PRIORITY JOURNAL; RAT;

EID: 0033638022     PISSN: 00071188     EISSN: None     Source Type: Journal    
DOI: 10.1038/sj.bjp.0703723     Document Type: Article

References (37)

1. + channel revealed by the NMR-derived structures of scorpion toxins
2. +-induced anomalous rectification in squid giant axons
3. + channel
4. Ion channels in the immune system as targets for immunosuppression
5. A voltage-gated potassium channel in human T lymphocytes
6. Mechanism of verapamil block of a neuronal delayed rectifier K channel: Active form of the blocker and location of its binding domain
7. Voltage-gated potassium channels are required for human T lymphocyte activation
8. Physiological role, molecular structure and evolutionary relationships of voltage-gated potassium channels in T lymphocytes
9. + currents in rat type II alveolar epithelial cells
10. + channel block by verapamil and related compounds in rat alveolar epithelial cells
11. + channels in human T lymphocytes: A role in mitogenesis?
12. + channel
13. Basophilic leukaemia in the albino rat and a demonstration of the basopoietin
14. Divalent ion trapping inside potassium channels of human T lymphocytes
15. + channel gene
16. Improved patch-clamp techniques for high-resolution current recording from cells and cell-free membrane patches
17. Molecular mechanism of use-dependent calcium channel block by phenylalkylamines: Role of inactivation
18. 2+ channel block and inactivation: Common molecular determinants
19. Molecular determinants of high affinity phenylalkylamine block of L-type calcium channels in transmembrane segment IIIS6 and the pore region of the alpha l subunit
20. Molecular determinants of high affinity phenylalkylamine block of L-type calcium channels
21. Mechanisms of potassium channel block in rat alveolar epithelial cells
22. Distinct effects of mutations in transmembrane segment IVS6 on block of L-type calcium channels by structurally similar phenylalkylamines
23. Interaction between tetraethylammonium and amino acid residues in the pore of cloned voltage-dependent potassium channels
24. Multiple subunits of a voltage-dependent potassium channel contribute to the binding site for tetraethylammonium
25. Blockade of the voltage-gated potassium channel Kv1.3 inhibits immune responses in vivo
26. Functional messenger RNAs are produced by SP6 in vitro transcription of cloned cDNAs
27. Recovery from C-type inactivation is modulated by extracellular potassium
28. + in recovery from C-type inactivation
29. + channels
30. State-dependent inactivation of the Kv3 potassium channel
31. Kinetics and state-dependent effects of verapamil on cardiac L-type calcium channels
32. Evidence for an internal phenylalkylamine action on the voltage-gated potassium channel Kv1.3
33. The effect of deep pore mutations on the action of phenylalkylamines on the Kv1.3 potassium channel
34. The role of the intrinsic inactivation in the accumulation of phenylalkylamine block in mKv1.3
35. Detailed characterization of verapamil block of mKv1.3
36. 2+ channels
37. Verapamil block of the delayed rectifier K current in chick embryo dorsal root ganglion neurons