AN-132, a new class I anti-arrhythmic agent, depresses the acetylcholine-induced K+ current in atrial myocytes.
AN-132, a newly developed anti-arrhythmic agent, effectively depressed the acetylcholine (ACh)-induced K+ current (IK.ACh), as measured with the tight-seal, whole-cell clamp technique in single atrial cells of guinea-pig. When GTP-gamma S was loaded into the cell through a pipette, IK.ACh was activated persistently, probably due to irreversible activation of G proteins by GTP-gamma S. AN-132 was much less potent to depress IK.ACh in GTP-gamma S-loaded cells than in GTP-loaded cells. In conclusion, AN-132 may block mainly the cardiac muscarinic ACh receptors to suppress IK.ACh.
Kurachi
Y
Y
2nd Department of Internal Medicine, Faculty of Medicine, University of Tokyo, Japan.
Nakajima
T
T
Ito
H
H
Sugimoto
T
T
D000109:Acetylcholine / Q000037:antagonists & inhibitors*; D000813:Anilides / Q000494:pharmacology*; D000818:Animals; D000889:Anti-Arrhythmia Agents / Q000494:pharmacology*; D005029:Ethylenediamines / Q000494:pharmacology*; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D006160:Guanosine Triphosphate / Q000031:analogs & derivatives / Q000494:pharmacology; D006168:Guinea Pigs; D006321:Heart / Q000187:drug effects; D066298:In Vitro Techniques; D009206:Myocardium / Q000166:cytology / Q000378:metabolism*; D015221:Potassium Channels / Q000187:drug effects / Q000378:metabolism*; D013873:Thionucleotides / Q000494:pharmacology
C053205:3-(diisopropylaminoethylamino)-2',6'-dimethylpropionanilide, diphosphoric acid; D000813:Anilides; D000889:Anti-Arrhythmia Agents; D005029:Ethylenediamines; D015221:Potassium Channels; D013873:Thionucleotides; D016244:Guanosine 5'-O-(3-Thiotriphosphate); D006160:Guanosine Triphosphate; D000109:Acetylcholine